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R., Shyamsunder 1. G. Kalpana 2. K. Bhavanasindhu 3. *. "FORMULATION AND EVALUATION OF ORAL HERBAL TABLETS CONTAINING METHANOLIC EXTRACT OF ALTERNANTHERA PUNGENS WITH CYTOTOXIC ACTIVITY." Journal of Pharma Research 7, no. 4 (2018): 56–62. https://doi.org/10.5281/zenodo.1228682.
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<strong><em>ABSTRACT</em></strong> <strong><em>T</em></strong><em>he purpose of the present study is to prepare methanolic extract of the whole plant Alternanthera pungens (MEAP), to perform phytochemical analysis, screening of cytotoxic activity using MCF-7 cell lines and to develop herbal tablets using various polymers. The methanolic extract was prepared by maceration method and by performing qualitative analysis of extract MEAP, it was found to contain alkaloids, steroidal and triterpenoids and flavonoids. The extract MEAP has exhibited significant cytotoxic activity by performing In-vitro studies by using MTT assay on MCF-7 cancer cells. The 9 herbal oral formulations were prepared using various polymers such as Eudragit L 100, HPMC E50 premium, HPMC K 100 LVCR. Among 9 prepared herbal formulations, the blend of all the herbal tablets have exhibited good flow properties such as angle of repose, bulk density, tapped density and also exhibited significant post compression parameters and evaluated for the quality control parameters as per I.P limits. FT-IR analysis of all 9 herbal tablets shown that there is no interaction between the MEAP and the polymers employed. For conclusion, the whole plant Alternanthera pungens is rich in flavonoids and triterpenoids and exhibited cytotoxic activity with the methanolic extract and their herbal formulations were exhibited significant values. Hence the presence of cytotoxic phytoconstituents, the extension of the isolation of bioactive compounds from the plant Alternanthera pungens may be the promising study to obtain lead molecules for future.</em> <strong><em>KEYWORDS:</em></strong><em> Alternanthera pungens, herbal tablets, cytotoxic activity, Eudragit L 100, HPMC E50 premium, HPMC K 100 LVCR.</em>
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Witowski, Janusz, Andrzej Breborowicz, Nicholas Topley, Leo Martis, Jan Knapowski, and Dimitrios G. Oreopoulos. "Insulin Stimulates the Activity of Na+/K+-Atpase in Human Peritoneal Mesothelial Cells." Peritoneal Dialysis International: Journal of the International Society for Peritoneal Dialysis 17, no. 2 (1997): 186–93. http://dx.doi.org/10.1177/089686089701700215.
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Objective To assess the effect of insulin on the Na+/ K+-ATPase expression and activity in human peritoneal mesothelial cells (HPMC). Methods HPMC were isolated from the omental tissue of non-uremic patients, grown to confluence and rendered quiescent by serum deprivation for 24 hours. The activity of Na+/K+-ATPase was determined by measuring the ouabain-sensitive86Rb uptake. To assess whether the effect of insulin was related to changes in [Na+]i the sodium influx was measured with 22Na and the activity of Na+/K+ -A TPase was assessed in the presence of amiloride. Expression of Na+/K+ -A TPaseα1’ α2 and β1-subunit mRNAs was determined by RT/PCR. Results Exposure of HPMC to insulin resulted in a time and dose-dependent increase in the Na+/K+-ATPase activity. After 60 minutes the ouabain-sensitive 86Rb up take (cpm/104 cells) was increased from 6650±796 in control cells to 9763±1212 in HPMC exposed to 100 mU/ mL insulin (1.5-fold increase; n=4, P<0.05). In addition, incubation of HPMC with 100 mU/mL insulin resulted in a time-dependent increase in the 22Na influx. Pre-exposure of HPMC to 1 mM amiloride reduced the activity of Na+/K+-A TPase but did not block the stimulatory effect of insulin. RT/PCR analysis revealed that HPMC constitutively expressed α1 and β1-subunit mRNAs while the α2-subunit mRNA was barely detectable. Exposure of HPMC to insulin for up to 24 hours was not associated with any changes in the expression of either α1’ α2 or B1-subunit. Conclusion Insulin stimulates the Na+/K+-ATPase activity in HPMC in a time and dose-dependent manner. This effect appears to mediated by an increase in [Na+]i and is not related to alterations in Na+/K+-ATPase subunit mRNAs expression.
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Ramarao, Ch Taraka, J. Vijaya Ratna, and R. B. Srinivasa. "DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M." INDIAN DRUGS 55, no. 11 (2018): 71–73. http://dx.doi.org/10.53879/id.55.11.10741.
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The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.
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Shaik, Salma, Sudhir Maddela, and Buchi N. Nalluri. "Development of Capecitabine Floating Tablet Dosage Forms for Treating Stomach Cancer." Journal of Drug Delivery and Therapeutics 10, no. 3-s (2020): 199–205. http://dx.doi.org/10.22270/jddt.v10i3-s.4171.
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Objective: In the present research work, oral gastro retentive dosage forms (GRDFs) of capecitabine (CPC) were formulated using floating concept.
 Methods: GRDFs were formulated using hydroxypropyl methyl cellulose (HPMC K4M and K15M) as drug release retardant, sodium bicarbonate (NaHCO3) and calcium carbonate (CaCO3) as gas generating agents, and micro crystalline cellulose (MCC), dicalcium phosphate (DCP), spray dried lactose (SDL), and pre gelatinized starch (PGS) as fillers. The tablets were prepared by direct compression method and evaluated for various parameters. The GRDFs were also characterized by Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC).
 Results and Discussion: All the formulations were subjected for pre and post compression parameters, shows all the data within the limits. The lag times of GRDFs has decreased significantly for formulations containing calcium carbonate when compared to sodium bicarbonate as gas generating agent. In vitro drug release studies indicate that higher polymer concentration delayed the CPC release, and the sustaining effect was in the order K4M > K15M > LVCR 100. Addition of MCC, DCP, SDL, and PGS as fillers further affected the lag time and in turn the CPC release rates.
 Conclusion: The formulation (F9) containing 10%w/w HPMC K4M as the release retardant, microcrystalline cellulose as filler and 20%w/w CaCO3 as gas generating agent fulfilled regulatory requirements in terms of percent drug release at the end of 24h.
 Keywords: Capecitabine, Gastro retentive floating tablets, floating drug delivery systems, FTIR, DSC.
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Bhumi, Patel* Dr. Chainesh Shah. "FABRICATION AND IN-VITRO CHARACTERIZATION OF TRANSDERMAL MATRIX PATCH OF KETOPROFEN FOR TRANSDERMAL THERAPEUTIC SYSTEM." Indo American Journal of Pharmaceutical Sciences (IAJPS) 03, no. 09 (2016): 960–73. https://doi.org/10.5281/zenodo.153859.
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Objective: The objective of research work was to improve the permeability of Ketoprofen and to provide controlled release of drug to provide maximum effective concentration. Experimental work: Transdermal drug delivery systems are polymeric patches containing dissolved or dispersed drugs that deliver therapeutic agents at a constant rate to the human skin. Matrix type transdermal patches containing Ketoprofen were prepared by solvent casting method employing aluminium foil method. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as penetration enhancer. Polymers were selected on the basis of the their adhering and non-toxic property. Result and discussion Drug polymer interactions determine by FTIR and standard calibration curve of Ketoprofen were determine by using UV estimation. Transdermal patch was prepared by using HPMC K-4 M: PVP K-30, HPMC K-15 M: PVP K-30, HPMC K-100 M: PVP K-30, Eudragit RS-100:PVP K-30 showed good physical properties. All prepared formulations indicated good physical stability. In-vitro drug permeation studies of formulations were performed by using Franz diffusion cells using abdomen skin of Wistar albino rat. Result, showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations prepared with hydrophilic polymer containing permeation enhancer. The permeability of Ketoprofen was increased with increase in PVP content. The burst effect due to the incorporation of PVP was because of the rapid dissolution of the surface hydrophilic drug which gets swell and thus leads to the decrease of mean diffusional path length of the drug molecules to permeate into dissolution medium and higher permeation rates. Conclusion: It was observed that the formulation containing HPMC K-4 M: PVP K-30 (2:3) showed ideal higuchi release kinetics. Key words: Trasdermal drug delivery system, Polymers, Ketoprofen, Matrix type, Permiation
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Prusty, Amaresh, Sanjit Senapati, and Gyanaranjan Behera. "BOX-BEHNKEN DESIGN APPROACH (BBDA) IN DEVELOPMENT AND OPTIMIZATION OF METFORMIN EXTENDED RELEASE TABLETS (MERT)." Ankara Universitesi Eczacilik Fakultesi Dergisi 49, no. 2 (2025): 11. https://doi.org/10.33483/jfpau.1539651.
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Objective: The present research outlines the use of quality by design (QbD) method to formulate MERT using Box-Behnken Design approach (BBDA). Based on quality target product profile (QTPP) to achieve tablets hardness and % cumulative Drug Release (% CDR) (at 2 hour and 10 hour), Critical quality attribute (CQA)were identified and selected as independent variable. In this present work, HPMC K 100M, Eudragit RL 100, and excipients MCC are selected as independent variables at their high and low levels in development of MERT. Material and Method: As per Design-Expert® prediction, total 19 formulations are prepared where each tablets of weight of 850 mg prepared by direct compression method. For each formulation, responses are determined and analyzed to find most optimized concentration. Result and Discussion: HPMC K 100 M, Eudragit RL 100 and MCC have antagonistic effects on the % CDR after 2 hour and 10 hours. From diagnostic plot it has been observed normal distribution of all data points near to straight line for normal plot of residuals, and predicted vs. actual. The desirability cube and the contour graph showing maximum desirability for optimized values of 76.75 mg, 203 mg and 58 mg for HPMC K 100M, Eudragit RL 100 and MCC respectively which are selected as independent factors in formulation of MERT. Prepared optimized tablets of MERT releases drug for more than 10 hr.
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Abhishek, Bhosale*1 Priti Shinde2. "Formulation and Evaluation of Metformin HCL Gastroretentive Floating Sustained Released Tablet." International Journal of Scientific Research and Technology 2, no. 6 (2025): 06–16. https://doi.org/10.5281/zenodo.15566055.
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The Metformin HCl Gastroretentive Floating Sustained Release Tablet was formulated using the Wet Granulation method. This tablet incorporates an effervescent system, where Hydroxypropyl Methylcellulose (HPMC) K 100, a swellable polymer, facilitates the floating mechanism. Sodium bicarbonate is employed to create the effervescent system. A synergistic combination of HPMC K 100 and Xanthan Gum enhances the sustained release profile of the formulation. The prepared gastroretentive floating tablets were evaluated for various pharmaceutical parameters, including bulk density, tapped density, angle of repose, Carr’s index, weight variation, friability, and in vitro dissolution studies, along with the total floating time. The results from the optimized batch were satisfactory, indicating favorable flow properties. Both weight variation and friability were within the pharmacopoeial limits. In vitro dissolution testing revealed a maximum drug release of 99.10% within 8 hours.
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Anepu, Sarada, Lohithasu Duppala, and Soma Sundari M. "FORMULATION DEVELOPMENT, CHARACTERIZATION AND IN- VITRO EVALUATION OF FLOATING MATRIX DOSAGE FORM OF TRAMADOL HYDROCHLORIDE USING VARIOUS POLYMERS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 2 (2017): 281. http://dx.doi.org/10.22159/ajpcr.2017.v10i2.15587.
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Objective: The purpose of present study was to formulate the gastro retentive floating tablets of tramadol hydrochloride for enhancement of the gastric residence time.Methods: The floating tablets were prepared by direct compression method and evaluated for hardness, thickness, and friability of the tablets. The in vitro drug release studies were performed for different formulations and to optimize the best formulae based on the dissolution profiles.Results: Fourier transform infrared spectroscopy and differential scanning calorimetry studies revealed that there was no interaction between tramodol hydrocholride and excipients. The formulated tablets were evaluated for properties like weight variation, hardness, thickness, friability, drug content, density and floating properties, matrix integrity and complied with USP requirements. The tablets of optimized formula had floating lag time of 120, 72 and 96 seconds and the tablets remained in the floating condition for more than 12 h. The results of drug excipients compatibility studies suggest that there was no significant change in the physical appearance of these blends, when stored at 40 °C/75% RH for a period of 4 weeks. Among various trial formulations developed with different concentration of polymer F3 (HPMC K4 M with 120mg of polymer), F5 (HPMC K15 M with 100 mg polymer), F11 (PEO WSR 303 with 100mg polymer), were chosen as the optimized formulations based on the release profile.Conclusion: Tramodol HCl floating tablets were successfully made using various polymers for the enhancement of the gastric residence time. From the present study it was concluded that hydroxy propyl methyl cellulose K 4 M can be used as effective polymer for the formulation of floating effervescent tablets of highly soluble drug indicating successful development of sustained release floating drug delivery system.Key words: Tramodol HCl, floating tablets, PEO 303 WSR, PEO N60, HPMC K 4 M, HPMC K15 M and HPMC K 100 M.
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Mohammad Gufran, Mohammad Faizan, Sailesh Kumar Ghatuary, Reena Shende, Prabhat Kumar Jain, and Geeta Parkhe. "Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 574–78. http://dx.doi.org/10.22270/jddt.v9i4-s.3401.
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Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline.
 Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.
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Azad, A. K., K. Jahan, TS Sathi, R. Sultana4, SA Abbas, and ABMH UddinUddin. "IMPROVEMENT OF DISSOLUTION PROPERTIES OF ALBENDAZOLE FROM DIFFERENT METHODS OF SOLID DISPERSION." Journal of Drug Delivery and Therapeutics 8, no. 5 (2018): 475–80. http://dx.doi.org/10.22270/jddt.v8i5.1942.
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Poor aqueous solubility of drugs results in poor absorption and bioavailability. The objective of Solid dispersion technology is to increase the dissolution properties of highly lipophilic drugs, by using different hydrophilic carriers thereby improving their bioavailability. This technology is useful for enhancing the dissolution, absorption and therapeutic efficacy of drugs in dosage forms. Albendazole is a broad-spectrum antihelminthic agent used for the treatment of a variety of parasitic worm infestations. It is practically insoluble in water but slightly soluble in solvents like chloroform, methanol, ethyl acetate, and acetonitrile. The aim of our study was to improve the dissolution profile of Albendazole using HPMC K 100 LV, Kollidon VA64 and Mannitol as carriers by solid dispersion techniques. From the prepared solid dispersion, formulation code CSF5 showed better result where carrier was HMPC K 100 LV at 1:10 ratio in solvent evaporation method. Among the carrier used here to conduct our study, HPMC K 100 LV showed better result for both kneading and solvent evaporation methods. And among the method employed here, solvent evaporation method showed better solubility of drug at 60 min also at 1:10 ratio which was 78.86%.
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Gaware, Ravi U., Gayatri R. Waykar, Madhuri K. Yewale, Rutuja B. Mhaske, and Poonam S. Mhaske. "Formulation and In-vitro evaluation of sustained release matrix tablet of Metformin hydrochloride." Journal of Drug Delivery and Therapeutics 9, no. 3 (2019): 95–98. http://dx.doi.org/10.22270/jddt.v9i3.2606.
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The low bioavailability and short half-life of Metformin hydrochloride (MH) make the development of sustained-release forms desirable. Present work involves preparation and optimization of sustained release matrix tablet of MH by direct compression method using HPMC K 100 and ethyl cellulose as a matrix forming polymer. Avicel was added as a direct compaction vehicle to improve the compaction behavior of Metformin which otherwise exhibits poor compaction behavior which again is further increased by its relatively high dose. Hydrophilic matrix of HPMC alone resulted in initial burst of Metformin release, however when combined with ethyl cellulose drug release was slowed down and thereafter it became optimal at particular concentration of polymers.
 Keywords: Metformin, HPMC, Ethyl cellulose, sustained release, matrix, tablet.
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Avinash, B. Darekar, N. Jadhav Sonali, and B. Saudaga Ravindra. "Design Development and Evaluation of Bilayer Tablet Using Eprosartan Mesylate for the Treatment of Hypertension." International Journal of Current Pharmaceutical Review and Research 8, no. 4 (2017): 328–37. https://doi.org/10.5281/zenodo.12674990.
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The aim of present study is to formulate Eprosartan Mesylate sustained release (SR) and immediate release (IR) bilayertablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the releasepattern. The sustained release layer of Eprosartan Mesylate was prepared by using different grades of HPMC like, HPMCK-100, HPMC along with other excipients by direct compression technique. The immediate release layer of EprosartanMesylate was prepared by Cross carmellose sodium and Sodium starch glycolate by direct compression technique. Thepowders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. Theboth immediate release and sustained release layers of Eprosartan Mesylate were characterized by FT-IR and in vitrodissolution studies. The drug release study of Eprosartan Mesylate was evaluated using USP-II paddle type dissolutionapparatus. The release rate of Eprosartan Mesylate in immediate release layer was studied for 1hr in 0.1 N HCL media andthat of Eprosartan Mesylate in sustained release layer was studied for 12 hr in pH 6.8 phosphate buffer media. From thenine batches S9 batch showed good release behaviour 98.82% of drug is released over 12 hours. Eprosartan Mesylate is apoorly water soluble (BCS class II) antihypertensive drug. Due to the poor water solubility of this drug, its bioavailabilityis dissolution rate-limited.
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D. Shivhare, Umesh, Vikrant P. Dorlikar, Kishore P. Bhusari, Vijay B. Mathur, and Bhiku N. Mirani. "Effect of Polymeric Compositions on Pharmacotechnical Properties of Carvedilol Transdermal Film." International Journal of Pharmaceutical Sciences and Nanotechnology 2, no. 1 (2009): 457–64. http://dx.doi.org/10.37285/ijpsn.2009.2.1.10.
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Transdermal films of carvedilol were prepared by using Eudragit RL100 (ERL100) either alone or in combination with Eudragit RS100 (ERS100), hydroxypropyl methylcellulose K 15 LV (HPMC), and ethyl cellulose (EC). The drug release was extended over a period of 24 h from all formulations. The formulation A5 showed 98.33 cumulative % drug releases in 24 h and followed zero order kinetics. The drug transport mechanism was observed to be Fickian. The cumulative % drug diffused through artificial permeation membrane (cellophane A 393) from same formulation was 100.52 % over a 12 h. The mechanism of dug release was governed by Peppas model and the drug diffusion rate followed zero order kinetics. The formulation A5 comprising of polymers ERL 100, ERS 100, EC and HPMC in 7:1:1:1 ratio fulfills the requirement of good TDDS.
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Prusty, Amaresh, Chinmaya Keshari Sahoo, Sanjit Kumar Senapati, Priyanka Singh, and Gyanranjan Behera. "Formulation and Characterization of Methyldopa Floating Tablets Using Polymeric Excipients: A Study on Gastroretentive Drug Delivery System." Jordan Journal of Pharmaceutical Sciences 18, no. 2 (2025): 423–36. https://doi.org/10.35516/jjps.v18i2.2718.
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This research aims to develop a novel gastro retentive drug delivery system (GRDDS) that can prolong the drug release of methyldopa. In the present research tablets are prepared by direct compression method using carbapol 934 and HPMC K100M polymer, by the use effervescent (for Formulations F1, F2, F3, and F4) and non-effervescent (F5) technology. One of the medications used to treat hypertension is methyldopa, a sympatholytic drug that acts centrally having short half-life of 2 h. Sedation, nausea, and vomiting are some of the drug's side effects that occur as a result of its frequency of its administration (250 mg two to three times day). Therefore, it would be far more effective to prepare GRDDS of methyldopa to release drug in the gastric environment for an extended duration. F3 is the most effective formulation batch because the combination of polymers HPMC K 100M and carbopol 934 in methyldopa effervescent tablets significantly prolongs the drug release in 0.1N HCl for more than 12 hours with a floating lag time of 60 seconds. The drug release mechanism reveals a new approach to treat hypertension with methyldopa floating tablets by utilising a mixture of HPMC K 100 M and carbopol 934 polymers.
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Suja, C., and Sismy C. "Formulation and Evaluation of Sustained Release Dosage Forms of Norfloxacin." International Journal of Pharmaceutical Sciences and Nanotechnology 11, no. 6 (2018): 4331–37. http://dx.doi.org/10.37285/ijpsn.2018.11.6.6.
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The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.
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Pradeep Kumar, M., Goparaju Suryanarayana Murthy, Annamdasu Lakshmi Poojitha, P. Sindhuri, A. Sreekanth, and Yerikala Ramesh. "Formulation and Evaluation of Colchicine Sustained release tablet by using factorial designs." Journal of Drug Delivery and Therapeutics 11, no. 5-S (2021): 100–107. http://dx.doi.org/10.22270/jddt.v11i5-s.5028.
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The study on the effect of polymer concentration on in vitro drug release profile revealed that there is a change in vitro drug release parameters (t50, t80, and MDT) with a change in polymer concentration. Fraction of HPMC K4M, HPMC K 100 M, and Ethyl Cellulose were required to be 15, 10, and 7 mg respectively for designing optimized batch F7. The release rate of Colchicine decreased proportionally with an increase in the concentration of ethyl Cellulose and HPMC K100 M. Also the high amount of HPMC K4M leads to the less initial release and sustain effect. A theoretical drug release profile was generated using pharmacokinetic parameters of Colchicine. The value of t50 and t80 of theoretical drug release profile was found to be 242 min and 529 min respectively. The similarity factor f2 was applied between the in vitro drug release profile of optimizing batches and theoretical profile, which indicate a decent similarity between all in vitro drug release profiles (f2 = 68.28 for F7). All the batches except F1shows the value of f2 value within a range. Batch F7 showed the highest f2 (f2 = 68.28) among all the batches and this similarity was also reflected in t50 (≈ 256 min) and t80 (≈ 554 min) values. A 23 full factorial design was applied to systemically optimize in vitro drug release profile. The HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) were selected as independent variables. The time required for 50% drug released (t50), the time required for 80% drug release (t80), similarity factor f2, and mean dissolution time (MDT) were selected as dependent variables. The results of full factorial design indicate that the HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) have a significant effect on in vitro drug release profile. To find out the release mechanism the in vitro release data were fitted in the Korsmeyer-Peppas equation. All Batches except F1 and F3 show Anomalous diffusion-controlled release (combined mechanism of diffusion and case II transport).
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Gunda, Raghavendra K., Naga Suresh K. Jujjuru, Vijayalakshmi A., Prathap M., and Koteswararao G. S. N. "STATISTICAL OPTIMIZATION AND ASSESSMENT OF DIVALPROEX SODIUM EXTENDED RELEASE TABLET." INDIAN DRUGS 60, no. 08 (2023): 31–37. http://dx.doi.org/10.53879/id.60.08.13485.
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The purpose of the current experimental research was to optimize the quantities of macromolecules such as Eudragit L/100-55 and HPMC-K-100M for the development of extended release tablets of divalproex sodium, an anti-convulsant or epileptic agent used in the effective management of bipolar disorders, mania, seizures, convulsions, tremors/epilepsy. Divalproex sodium ER tablets were formulated with the help of Eudragit L/100-55 and HPMC-K-100M in variable compositions and variable amounts as per 32 factorial design technique. Tablets were prepared by direct compression technique. Quantities of polymers required for exhibiting extended release of active agent from the tablet were chosen as independent variables, in similar manner time required for drug release was chosen as dependent variable (t10%, t50%, t75%, t90%). Nine formulations were created in accordance with the plan, formulated, and tested for quality control criteria. It is obvious from the data that all formulations exceed the compendial restrictions. Kinetic parameters were established, and the data from the dissolution investigation suited kinetic models very well. For the responses, polynomial equations were created and validated. The optimum formulation of SOD5, which contains 31.25 mg of Eudragit L/100-55 & 31.25 mg of HPMCK-100M, exhibits resemblance to the commercial product of f2=85.91 and f1=2.25 (DIVALEX). SOD5 is made in a zero-order fashion, and the mechanism of drug release was found to be non - Fickian in nature (n = 0.645)
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Kumar, S. Mahesh, M. J. N. Chandrasekar, R. Gopinath, R. Srinivasan, M. J. Nanjan, and B. Suresh. "In Vitro and In Vivo Studies on HPMC-K-100 M Matrices Containing Naproxen Sodium." Drug Delivery 14, no. 3 (2007): 163–69. http://dx.doi.org/10.1080/10717540601098682.
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Socorrina, Colaco Ramesh. N. Ramakrishna Shabaraya. "FORMULAITON AND PHARMACOKINETIC EVALUATION OF NAPROXEN SODIUM MODIFIED RELEASE TABLET." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 05 (2018): 3960–67. https://doi.org/10.5281/zenodo.1249923.
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The objective of the study was to develop naproxen sodium SR tablets were prepared by direct compression method using hydroxy propyl methyl cellulose (HPMC K 100). To know the effect of polymer concentration invitro study performed it has been observed that as the polymer concentration increases, the drug release rate decreases, and bioavailability study carried out in healthy human subject by administering the developed sustained release and marketed immediate release tablet. The developed naproxen sodium showed confirmed longer time to reach peak concentration than marketed immediate release table, controlled and constant drug delivery system, maintains better plasma concentration than conventional tablet by which it overcome the shortcoming of conservative treatment. The rate and extent of absorption of naproxen sodium SR tablets were higher than the marketed immediate release tablet shows more competent and controlled drug release which would sustain plasma concentration level throughout and produce desired effect. Further evidenced with lower elimination rate and higher half life. Keywords: Naproxen sodium SR tablets, Marketed immediate release tablet, HPMC, LCMS-MS, Bioavailability study
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Islam, Asraful, Shimul Halder, and Sitesh Chandra Bachar. "Formulation and in vitro Evaluation of Betahistine Dihydrochloride Twice Daily Controlled Release Matrix Tablet." Dhaka University Journal of Pharmaceutical Sciences 10, no. 2 (2012): 93–100. http://dx.doi.org/10.3329/dujps.v10i2.11786.
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In order to reduce dosing frequency, a sustained release dosage form of betahistine dihydrochloride was developed as a twice daily controlled release tablet formulation that could be used to decrease vertigo resulted in Meniere's disease for a prolonged time. Six formulations were developed by using Methocel K4M CR, Methocel K15M CR and Methocel K 100 LVCR as single and combinations in different percentage. The tablets were prepared by wet granulation method. Physical properties of betahistine dihydrochloride granules and betahistine dihydrochloride matrix tablets were evaluated. The tablets were characterized for Betahistine Dihydrochloride release in both gastric simulated fluid (0.1 N HCl, pH 1.3) and simulated intestinal fluid (buffer solution pH 6.8). The data were subjected to different models in order to evaluate their release kinetics and mechanisms. The results of the in vitro dissolution study indicate that most of the formulations showed above 80% of drug release in 12 hours but formulations (F-2 and F-4) met the official specification of release profile. Dissolution data were fitted to zero order equation, Higuchi square root law, Korsmeyer-Peppas model and Hixson-Crowell cube root law as these plots showed the highest value of linearity to evaluate kinetic data. The release of betahistine dihydrochloride was prolonged for 12 hours indicating the usefulness of the formulations for twice daily dosage forms, leading to improve efficacy, controlling the release and better patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v10i2.11786 Dhaka Univ. J. Pharm. Sci. 10(2): 93-100, 2011 (December)
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G., Jagadish 1. *. Dr. Anil Kumar Middha 2. "FORMULATION AND EVALUATION OF FLOATING AND MUCOADHESIVE TABLET OF ORAL HYPOGLYCEMIC DRUG OF NATEGLINIDE." Journal of Pharma Research 7, no. 6 (2018): 109–12. https://doi.org/10.5281/zenodo.1291615.
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<strong><em>ABSTRACT</em></strong> <strong><em>I</em></strong><em>n the present research work gastro retentive mucoadhesive floating formulation of Nateglinide by using various hydrophilic polymers. Nateglinide is a drug for the treatment of type 2 diabetes. Initially analytical method development was done for the drug molecule (1-4). Absorption maxima was determined based on that calibration curve was developed by using different concentrations. Gas generating agent accrual and bioadhesive polymer carbopol concentration was optimized. Twelve formulations were developed by using different concentrations of polymers of various polymers. The formulation blend was subjected to various preformualation studies (5-8), flow properties and all the formulations were found to be good indicating that the powder blend has good flow properties. The prepared tablets were evaluated, by invitro dissolution test results it was found that formulation F12 prepared by using HPMC K15 M and HPMC k 100 M has shown the maximum drug release hence it was considered as the optimized formulation. The optimized formulation dissolution data was subjected to release kinetics (9-10), from the release kinetics data it was evident that the formulation followed zero order kinetics of drug release.</em> <strong><em>KEYWORDS:</em></strong><em> Nateglinide, Preformualation, Hydrophilic Polymers.</em>
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Karkare, Swati, Nilima Thosar, Milind Wagh, and Nikita Wagh. "Formulation and Evaluation of Haemocoagulase Gel for Dental Pulp- an In-vitro study." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 14, no. 03 (2024): 1248–56. http://dx.doi.org/10.25258/ijddt.14.3.01.
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This study aims to develop a novel hemostatic gel of hemocoagulase, a snake venom-derived serine protease enzyme, by incorporating it into the matrix of bioadhesive polymers to prevent damage due to hemorrhage. Haemocoagulase was combined with polymers Carbopol 940 and HPMC K 100, and these formulations were evaluated for physical properties, efficacy, safety and stability. Batches F3 and F6 were selected for further studies on animal models, which were found to be safe without any skin irritation effect and effective as hemostats with blood clotting times of 1.24 ± 0.007 min and 1.36 ± 0.014 min, respectively, in a rat liver incision model. From this study, it can be suggested that the combination of hemocoagulase with bioadhesive polymer can provide a novel hemostatic tool for controlling bleeding.
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Kumar, Mukesh, Deeksha Singh, and Vatan Chaudhary. "Formulation and Characterization of Sustained Release Matrix Tablet of Pantoprazole." EAS Journal of Pharmacy and Pharmacology 4, no. 4 (2022): 64–69. http://dx.doi.org/10.36349/easjpp.2022.v04i04.001.
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Pantoprazole is a proton pump inhibitor prodrug used in the treatment of gastric, duodenal ulcers and gastro esophageal reflux disease (GERD), Zollinger- Ellison syndrome. This is the most popular drug used in cure and maintenance therapy of peptic ulcer along with antibiotics. It suppresses the acid production by inhibiting the H+ K+ ATPase. Pantoprazole must be absorbed in the gastrointestinal tract and because it is unstable under acidic conditions, enteric delivery systems are required. The purpose of this study was to prepare matrix tablet using eudragit Rs 100, eudragit S100, and HPMC. On the basis of above result the formulation showed satisfactory result as it has the maximum release i.e. F5 66.50%in 10 hrs. Result of our study suggest that the matrix tablet containing pantoprazole may be suitable for the anti ulcer drug.
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Sharma, Saurabh, Yogesh Matta, Sandeep Singh, Kajol Rustage, Ashwani Kumar, and Neha Arora. "Formulation and Evaluation of Floating Microspheres of 1,1-Dimethylbiguanide." Journal of Drug Delivery and Therapeutics 9, no. 4-A (2019): 742–47. http://dx.doi.org/10.22270/jddt.v9i4-a.3594.
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1,1-Dimethylbiguanide is a hypoglycemic agent used in the treatment of non-insulin dependent Diabetes mellitus. It is a BCS Class –III drug having poor permeability. Plasma half life ranges from 1.5-3 hrs & oral bioavailability is 50-60%. Hence require frequent oral administration for adequate treatment of Diabetes in order to extend the gastric retention time oral sustained dosage form was developed in the form of microspheres using polymers (sodium CMC, HPMC K 100 M). The results presented that drug dissolution rate and drug entrapment increases while decreasing the polymer amount. All the formulations are evaluated for dissolution, entrapment efficiency, percentage buoyancy and 1,1-Dimethylbiguanide Microspheres of formulations, F-4 was found to be optimized formulation based on in-vitro release pattern and percentage buoyancy entrapment efficiency. Keywords: 1,1-Dimethylbiguanide, half-life formulations, efficiency.
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Ramesh, Yerikala, Abhilash Kaki Rohan, Balasaradhi Koorapati, and P. Sudarsanam. "Formulation and evaluation of almotriptan controlled release pellets." Journal of Drug Delivery and Therapeutics 9, no. 1-s (2019): 312–18. http://dx.doi.org/10.22270/jddt.v9i1-s.2355.
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Abstract: The aim of the present study was to formulate and evaluate Almotriptan pellets. Almotriptan controlled release pellets were prepared by Solution layering technique by using croscarmellose and povidone in former case and three different polymers HPMC K 100, Ethyl cellulose and Eudragit RS 100 as rate controlling polymer in three different ratios like 1:1, 1:1.5 and 1:2 to achieve desired release in later case. Evaluation was performed according to the Pharmacopoeia standards including Drug excipients compatibility, Percentage yield, Particle size distribution, Drug content analysis and in-vitro release study. The best results were found to be using Almotriptan and Eudragit RS 100 in 1:2 ratios. A broad variety of drug release pattern could be achieved by variation of polymers ratios which was optimized to match the target release profile. In comparison of in-vitro release studies for different controlled release formulations, F9 releases 98.54% of drug at the end of 12th hour and was considered as best formulation. Stability study has shown no significant change in the drug content analysis and in-vitro dissolution study of best formulation even after 6 months.
 Keywords: Almotriptan, Controlled release, Dissolution profile, in-vitro drug release, Stability studies.
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Kendre, P. N., and P. D. Chaudhari. "DESIGN AND OPTIMIZATION OF ORAL BIOADHESIVE NANOCURCUMIN DELIVERY USING NOVEL HYDROPHILIC CARRIER FOR CANCER TREATMENT: AN ALTERNATIVE TO PARENTERAL CHEMOTHERAPY." INDIAN DRUGS 53, no. 08 (2016): 24–36. http://dx.doi.org/10.53879/id.53.08.10522.
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Present study involves the design and optimization of oral bioadhesive delivery system of curcumin. Solid dispersion of curcumin was developed using novel hydrophilic carrier, Gelucire® 50/13, by melt granulation technique. Based on HPMC K 100 LV(X1) and carbopol 934P (X2), bio-adhesive tablets containing curcumin solid dispersion was developed by direct compression, using central composite designs for two factors at three levels. Tablet formulation was optimized for t50%, Rel24h and bioadhesive strength. The drug release mechanism was found to be by fickian diffusion, approaching zero-order kinetics. Average plasma uptake of curcumin was found to be 0.289μg/mL as compared to plain curcumin tablet formulation. The results were found highly significant (p<0.05). The swelling matrices behavior over the time period studied showed that the gelling layer thickness increases continuously. From this study, it may be concluded that the oral controlled bioadhesive curcumin delivery may be an alternative to parenteral chemotherapy.
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Shinde, Smruti1 Shinde Soham2 Shinde Vaishnavi3 Shirfule Pragati4 Shrungare Aishwarya5 Chintale Ashwini*. "A Review On Multipurpose Therapeutic Use Of Herbal Gel." International Journal in Pharmaceutical Sciences 1, no. 12 (2023): 569–78. https://doi.org/10.5281/zenodo.10408739.
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In this review the study of traditional plants which are using to prepare herbal gels for multipurpose. Herbal medicines is still the mainstay of about 75-80% of the world’s population, mainly in developing countries, for primary health care because of better cultural acceptability, better compatibility with human body and lesser side effects. Herbal medicines consist of plant or its part to treat injuries, disease or illnesses and are used to prevent and treat diseases and ailments or to promote health and healing. Herbal medicines are the oldest form of healthcare known to mankind. From that the Herbal Gel are used topically for treating many disorders. By the extraction of plant herb formulate the herbal gel with adding some components such as Carbopol 934, HPMC K 100 Mand Xanthan gum showed good homogeneity, no skin irritation, good stability and anti-inflammatory activity. The extract shows best and promising activity. Now a day’s topical agents are widely used to treat skin conditions.
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Chauhan, Anushree, Ganesh Prasad Mishra, and Surbhi Gupta. "Design, Optimize and Evaluate Dapagliflozin Sustained Release Microspheres using Box-Behnken Design." International Journal of Drug Delivery Technology 15, no. 02 (2025): 01–07. https://doi.org/10.25258/ijddt.15.2.13.
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This study aimed on optimizing dapagliflozin microspheres for sustained release to improve efficacy over the marketed product. Microspheres were formulated by a Solvent Evaporation method involving sodium alginate, ethyl cellulose and HPMC K 100. The process was optimized through Box- Behnken statistical experimental model, adjusting polymer concentration, surfactant amount and rotational speed. Seventeen formulations were formulated and the optimized formulation (F2) was investigated for its micromeritic characteristics, SEM, in-vitro release, kinetic modeling, and stability. FT-IR study showed no negative correlation among the drug and polymers. F2 exhibited maximum yield (81.78%), entrapment efficiency (82.21%) with optimum particle size (278.69 μm). Increased concentration of polymer improved yield and efficiency of drug entrapment while stirring rate decreased particle size. SEM analysis revealed rough, porous and spherical microspheres, and the release was sustained, with 98.02% of the drug released over 20 hours. The optimized microspheres showed prolonged drug release under gastrointestinal conditions, offering increased efficacy and potentially enhancing patient adherence by lowering dosing compared to the marketed product.
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Payal, Mohaniya* Neelam Patel Rajat Pawar Deepti Modi. "Development and Evaluation of Sustained Release Matrix Tablet of Naproxen Using Natural Polymer." International Journal of Pharmaceutical Sciences 3, no. 4 (2025): 2938–51. https://doi.org/10.5281/zenodo.15273781.
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The present study aims to develop sustained-release matrix tablets of Naproxen using Moringa oleifera gum, a natural polymer, for its release-retarding properties, and with the synthetic polymer HPMC K-100. Compatibility study between the drug and the selected polymers was confirmed through FTIR spectroscopy. Matrix tablets were prepared using the wet granulation method. The granules were assessed for bulk density, tapped density, compressibility index, Hausner’s ratio, and angle of repose, all of which were found within acceptable limits. The compressed tablets were evaluated for physical parameters including thickness, hardness, friability, weight variation, drug content, in vitro drug release, and stability. All formulations complied with Pharmacopeial standards. In vitro dissolution studies conducted over a 12-hour period for nine formulations (F1–F9) demonstrated that formulations F5 and F3 exhibited optimal sustained-release profiles, releasing 98.69% and 97.8% of the drug, respectively. Stability studies of formulation F3 indicated no significant changes, confirming its stability over the test period.
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Gaur, A., and H. P. Shah. "Formulation, Development and Evaluation of floating tablet of Metformin Hydrochloride using optimization of gas generating agent." Formulation, Development and Evaluation of floating tablet of Metformin Hydrochloride using optimization of gas generating agent 1, no. 3 (2011): 26–31. https://doi.org/10.5281/zenodo.12699386.
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The present study deals with drug release enhancement of MetforminHydrochloride using floating technology by optimization of gas generating agent to improvethe buoyancy time. Metformin hydrochloride is a oral antihyperglycemic agent of biguanideclass used in treatment of type 2 Diabetes. It is hydrophilic drug which absorbed slowly andnot completely form the gastrointestinal tract. The absolute bioavailability is reported to be50-60%. This technology uses direct compression method to prepare floating tablet ofMetformin Hydrochloride with release retardant polymer HPMC K-100, PVP K-30, Carbopol934p and different concentration of gas forming agents sodium bicarbonate and citric acid.The floating behavior and in vitro dissolution studies ware carried out. From the result finalformulation release was found to be approximately 96% in 24 hr, while the floating lag timewas observed to be 3 min and the tablet remained floatable throughout studies. Form theresult of the study we conclude that incorporation of gas generating agent produced initialburst-effect due to production and release of CO2 form polymeric matrix. Increasedconcentration of sodium bicarbonate results in increased bursting effect. Optimumconcentration of sodium bicarbonate was found to be 8-10% to produce low floating lag time.Thus, with using of optimum concentration of gas generating agent the floating tablet ofMetformin Hydrochloride was successfully developed.
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Thulluru, Ashok, Manthena Mohan Varma, Chitrali Mallikarjuna Setty, Pavan Kumar Chintamaneni, and Sriharshavardhan Samayamanthula. "Effect of Sodium alginate in Combination With HPMC K 100 M in Extending the Release of Metoprolol Succinate from its Gastro-Retentive Floating Tablets." Indian Journal of Pharmaceutical Education and Research 49, no. 4 (2015): 293–303. http://dx.doi.org/10.5530/ijper.49.4.7.
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Das, Manoj Kr, Bhanu P. Sahu, and Jahan Nur Rahman Hazarika. "DEVELOPMENT OF BILAYER TABLETS FOR IMMEDIATE AND CONTROLLED RELEASE OF ALLICIN." International Journal of Current Pharmaceutical Research 9, no. 4 (2017): 153. http://dx.doi.org/10.22159/ijcpr.2017v9i4.20982.
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Objective: The purpose of this study was to develop and evaluate bilayer tablet for the immediate and controlled release of Allicin (Garlic Extract) for effective treatment of Hypertension.Methods: The immediate release layer was prepared by using super disintegrants-sodium starch glycolate and binder used xantham gum and the sustained release layer was prepared by using hydrophilic polymer like HPMC K 100 and PVP. Before preparation of the tablets, all the pre-formulation parameters were checked and the tablet of Allicin were prepared by direct compression method and was evaluated for physical characteristics like hardness, weight variation, drug content and friability. In vitro release of drug was performed USP type II dissolution test apparatus using phosphate buffer (pH 7.4) as dissolution media and dissolution was continued for 8 hrs for the sustained release layer.Results: It was found that all the formulations were within the limit of the standard. The drug release of the tablet was in the range of 66%-83% in 8 h.Conclusion: It was concluded that the F4 formulation showed the optimum result as a bilayer tablet for the effective treatment of hypertension.
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Shiv, Sagar Mahapatra*1 Akanksha Patel2 Manmath Purohit3. "Design Development And Evaluation Of Floating Drug Delivery System For Lornoxicam NSAID Drug." International Journal in Pharmaceutical Sciences 2, no. 4 (2024): 231–51. https://doi.org/10.5281/zenodo.10927489.
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Lornoxicam is one of the drugs used for the management of arthritic pain. The site of absorption of Lornoxicam is in the GIT and it has a short half life of 3-4 h. Therefore, the present investigation was concerned with the development of the floating matrix tablets, which after oral administration are designed to prolong the gastric residence time and thus, improve the bioavailability of the drug as well as its half life. Lornoxicam showed maximum absorption at wavelength at 374 nm in 0.1 N HCl. Drug-Polymer compatibility studies by FTIR gave conformation about their purity and showed no interaction between drug and selected polymers. Various formulations were developed by using release rate controlling gel forming polymers like HPMC (K-4 M, K-15 M & K-100 M) in a single by direct compression method with the incorporation of NaHCO3 as a gas generating agent. All the formulation had floating lag time below 55 seconds and constantly floated on dissolution medium for more than 24 hours. Swelling studies indicated significant water uptake and contributed in drug release. From among all the developed formulations, as formulation F-3 prolonged the drug release for longer period of time and it had less floating lag time as compared to other formulations. So, it was selected as the best formulation. It was concluded that the drug release followed Zero order kinetics, as the correlation coefficient (R2 value) was higher for Zero order release, so the drug release followed controlled release mechanism. The best formulation was found to be stable during the stability studies for two months. Thus, the best formulation satisfied physicochemical parameters, floating properties, swelling index and in vitro drug release profile requirements for a floating drug delivery system.
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Dr.Shaikh, Siraj N* Mo. Irfan Mo.Hasnain Dr.G. J. Khan Shoaib Ahmad. "FORMULATION, OPTIMIZATION AND EVALUATION COLON TARGATED DRUG DELIVERY SYSTEM FOR ORNIADAZOLE." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 04 (2018): 3168–76. https://doi.org/10.5281/zenodo.1238402.
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The colon is a site where both local and systemic delivery of drugs can take place. The present investigation concerns with formulation and evaluation of Colon Targeted dip coated tablets of Ornidazole by using HPMCK4 M, Xanthan gum polymers .Initially core tablets were prepared and then coated by using Eudragit S100 as a enteric coating polymer with the help of Isopropyl alcohol, acetone (1:1) by deep coating. Optimization of colon targeted tablet of Ornidazole was carried out by using design expert software considering combination of HPMC K 4 M & Xanthan gum as independent variable & Time for 25% Drug release (hrs), Drug Release at 12 hrs as a dependent variable. All the formulations FB1 to FB9 were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The tablets were passed all the tests. Among all the formulations FB5 formulation was found to be optimized as it was retarded the drug release up to 12 hours and showed maximum of 91.57% drug release. The results of the present study have demonstrated that developed colon targeted coated tablet were promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of ornidazole for the treatment of disease of colon region. Key Words: Colon targeted, Ornidazole, Optimization, Eudragit S 100, Coating.
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Kumar, Suraj, and Bishnu Upreti. "Formulation and Evaluation of Gastroretentive Floating Microspheres of Amiloride Hydrochloride." Asian Pacific Journal of Health Sciences 11, no. 3 (2024): 14–24. http://dx.doi.org/10.21276/apjhs.2024.11.3.04.
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Background: Amiloride, a potassium-sparing diuretic, is widely prescribed for the management of hypertension, congestive heart failure, and various renal disorders. However, its low oral bioavailability due to extensive first-pass metabolism and short half-life necessitates frequent dosing, leading to patient inconvenience and compromised therapeutic outcomes. To address these limitations, the development of novel drug delivery systems capable of enhanced gastrointestinal retention of amiloride has garnered significant attention. Among these, gastroretentive microspheres represent a promising approach, offering prolonged drug release and improved absorption. Objectives: The present work by formulation and evaluation of gastroretentive floating microsphere (FM) plays a highly significant role as a particulate drug delivery method. Particle sizes for microspheres range from 0.1 to 200 μm, and they can be administered orally, parenterally, nasally, ophthalmologically, transdermal, colonically, etc. Site-specific targeting and enhanced release kinetics are just two of the issues that have been solved through recent advances in microspheres, including those that are mucoadhesive, hollow, floating, micro-balloons, and magnetic. Microspheres will play a key role in novel drug delivery in the future by fusing different new methods, particularly sick cell sorting, genetic materials, safe, targeted, and effective drug delivery. Discussion: Hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone, and ethylcellulose were used in varying concentrations to give the FMs of amiloride HCl release-controlling properties by increasing their bioavailability. Lactose was used as a diluent and sodium bicarbonate served as an effervescent agent. Using a solvent evaporation method approach, the gastroretentive FM of amiloride HCl was created. The generated microsphere indicated good floating strength and remained buoyant in the sustained released medium for 24 h. For systemic delivery of amiloride, a potassium-sparing diuretic and antihypertensive medication, through the oral route, a gastroretentive FMs drug delivery system was developed. The different ratios of ethylcellulose and HPMC K-100, sodium lauryl sulfate, sodium bicarbonate, and ethanol are used in formulation. The weight, thickness, percentage of moisture absorbed and lost, surface pH, folding resistance, content homogeneity, in vitro residence time, in vitro release, and ex vivo penetration of the microspheres were all assessed. Conclusion: The formulation and evaluation of gastroretentive FMs represent a significant advancement in particulate drug delivery systems. These microspheres, with particle sizes ranging from 0.1 to 200 μm, offer versatility in administration.
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Gorjanović, Stanislava, Darko Micić, Ferenc Pastor, et al. "Evaluation of Apple Pomace Flour Obtained Industrially by Dehydration as a Source of Biomolecules with Antioxidant, Antidiabetic and Antiobesity Effects." Antioxidants 9, no. 5 (2020): 413. http://dx.doi.org/10.3390/antiox9050413.
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Apple pomace flour (APF) obtained at industrial scale level by the application of innovative technological process (dehydration (5 h, T ≤ 55 °C), grinding (300 µm)) was evaluated as a source of bioactive compounds with antioxidative, antiobesity and antidiabetic effects. Proximate composition, individual (HPLC–DAD–MS/MS) and total phenols (TPC) as well as flavonoids content (TFC), antioxidant (AO) activity (DPPH, ABTS, HPMC), water and oil holding capacity (WHC and OHC) of APFs obtained from apple pomace from mixed and individual apple cultivars grown conventionally and organically were compared. The effect of APF supplementation on the glycaemic status and glucose tolerance (oral glucose tolerance test (OGTT)) of C57BL/6J mice exposed to high-fat and sucrose diet was examined. High K content (4.2–6.4 g/kg), dietary fibres (35–45 g/100 g), TPC (4.6–8.1 mg GAE/g), TFC (18.6–34.6 mg QE/g), high water and oil holding capacity (4.7–6.4 and 1.3–1.6 g/g) were observed in the APFs. Content of major phenols (phlorizin, chlorogenic acid, quercetin), TPC and TFC correlated highly with prominent AO activity. APF supplementation lowered the increase of body weight gain and blood glucose, and improved glucose tolerance significantly. Health-promoting biomolecules, AO activity, functional properties and prevention of diet-driven glucose metabolism disorders pave the way to APF exploitation in human nutrition.
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Bansal, Mukesh, Dilip Kumar Gupta, Monika Sachdeva, and ,. Kamini. "Formulation and Characterization of Expandable Tablet of Diacerein using Swellable Polymers." Journal of Drug Delivery and Therapeutics 12, no. 5 (2022): 156–69. http://dx.doi.org/10.22270/jddt.v12i5.5612.
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Some of the drugs have poor absorption because of a narrow absorption window in the gastrointestinal tract (GIT). To improve the absorption of such drugs in the GIT, gastro-retentive drug delivery techniques play an important role. Diacerein is an antirheumatic drug used for joint pain and arthritis. The expandable gastro-retentive tablets were prepared to attain an extended therapeutic action of Diacerein. Expandable tablets were formulated to prolong gastric retention, enhance the bioavailability of the drug candidate and attain a desirable size greater than the diametric size of the pyloric sphincter (i.e., 13 mm in diameter) of the tablet after administration by expandable technique. The expandable tablet was formulated using swellable polymers and polyelectrolytes, i.e., HPMCK 100, PEO, chitosan, and carbopol. The proposed expandable tablets were evaluated by preliminary evaluation parameters, micromeritic investigations, all physicochemical evaluations including swelling index, weight variation, drug content, in-vitro release studies and their release kinetics. Method: The wet granulation method is used for the preparation of expandable tablets of Diacerein. Result: The release of Diacerein from all formulations was studied in phosphate buffer pH 1.2 at 37±5°C. The net results conclude that the formulation having HPMC K 100, PEO with the addition of carbopol (formulation C1) showed the maximum swelling index as compared to others. And it was found that formulation C1 is the most superior and reliable formulation in terms of all physicochemical parameters and in-vitro drug release studies. The best formulation obtained from in-vitro drug release studies was shown.
 Keywords: Gastro retentive, expandable system, noval drug delivery system, controlled drug delivery system, gastric transit time, swellable polymers, GIT.
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Subhajit, Roy* Mayukh Jana Amlan Bishal Anwesha Adak. "Formulation and Development of Metformin Sustained Release Tablets by Hydrophilic Polymer." International Journal in Pharmaceutical Sciences 1, no. 9 (2023): 129–39. https://doi.org/10.5281/zenodo.8330636.
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Metformin HCL, the only biguanide still in use today, reduces peripheral insulin resistance and hepatic glucose production in people with Type 2 diabetes. It has a short plasma half-life and a low absolute bioavailability. The primary goal of this study was to create an oral sustained release metformin tablet employing the direct compression technique and rate-controlling ingredients like hydrophilic hydroxypropyl methylcellulose and Xanthan gum polymer. Thickness, weight fluctuation, hardness, consistency of drug content, and in vitro drug release were all assessed for all batches. The term "mean dissolution time," which describes the rate at which a medication is released from a dosage form, demonstrates a polymer's effectiveness in delaying drug release. When coupled with xanthan gum, the hydrophilic matrix of HPMC was able to successfully control metformin release for 12 hours. As a result, it is now possible to create sustained-release matrix tablets. According to data that fits the Korsmeyer equation, both erosion and diffusion could be exploited as drug release mechanisms.
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Arefin, Paroma, Md Shehan Habib, Mohammad Mostafa, et al. "Evaluation of the Influence of Stirring Speed on the Release Kinetics of Fexofenadine HCl Polymeric Microspheres." Biosciences Biotechnology Research Asia 18, no. 4 (2021): 733–41. http://dx.doi.org/10.13005/bbra/2955.
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Microspheres, a potential drug delivery approach, has opened a new era for attaining versatile release patterns needed. By optimizing the formulation variables, they can be prepared to obtain targeted release, immediate release, sustained release patterns. The release of the active drug material depends upon a number of formulation parameters such as polymers, stirring speed (rpm), methodology, surfactants, etc. Fexofenadine hydrochloride (HCl) is a second generation antihistamine. Our present research has explored the effects of using different rpm (600- 1000 rpm) in preparing fexofenadine hydrochloride (HCl) microspheres by emulsion solvent evaporation method. The formulation is aimed to provide sustained release for the required long period with a high margin of safety. We used a blended mixture of Hydroxy Propyl Methyl Cellulose (HPMC) K 100 MCR and Eudragit RL100 polymers to have sustained-release microspheres. The impact of different rpm on Yield, drug encapsulation efficiency, flow properties, and dissolution pattern were appraised. We observed the release of the drug for 10 hours in phosphate buffer (pH 6.8) and evaluated the drug release spectrophotometrically. Our study finds that the release of fexofenadine HCl from the microspheres was significantly increased with drug loading. We found the dosage forms to follow Higuchi release kinetics and Hixson-Crowell release kinetics the most, indicating successful achievement of sustained-release pattern in the dosage form. The change in drug release rate was statistically significant for variation in the stirring rate. We found that 600 rpm was the most optimized stirring rate for preparing microspheres in the emulsion solvent evaporation method.
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Prasad, Garrepally. "Progress and Characterization of Pramipexole Extended-Release Tablets." Journal of Clinical and Medical Case Reports and Reviews 1, no. 1 (2021): 1–4. http://dx.doi.org/10.59468/2837-469x/004.
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Pramipexole dihydrochloride monohydrate is an antiparkinson’s agent which is known as dopamine D2 receptor agonist. It is structurally different from the ergot-derived drugs, e.g. bromocriptine or pergolide. Pramipexole is designated chemically as (S)-2-Amino-4, 5, 6, and 7- tetrahydro-6-(propylamino) benzothiazole and has the molecularformula C10H17N3S. It comes under class I of Biopharmaceutical Classification System. The purpose of this study was to develop and evaluate pramipexole dihydrochloride monohydrate extended release tablets by wet granulation method using different proportions of polymers and binder. Pre-formulation studies were done initially and the results were found to be within the limits. All the mentioned batches were prepared and granules were evaluated for pre-compression parameters such as loss on drying, bulk density, tapped density and compressibility index. Tablets were evaluated for weight variation,thickness, hardness, friability; disintegration time and assay were found to be within the limits. In vitro dissolutions were performed with 0.05M 6.8 PH phosphate buffer and effectof various polymerswere explored. Final selection of formulation was based on dissolution profile,from dissolution studies formulation 9 showed 80% drug release within 20 hours, so it will be compared with innovator. Similarity and difference factors which revealed that formulation (F 9) containing HPMC K 200, Eudragit L100 and binderare most successful as it exhibited in vitro drug release that matched with innovator product.In vitro drug release profilereveals that with increased concentration of Eudragit L 100. Accelerated stability studies were performed for the optimized batch which indicatedthat there were no changesin drug contentand in vitro dissolution.
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Rayakwar, Neetesh, and Yuvraj Singh Dangi. "Development and characterization of controlled release bilayered tablets of Citicoline sodium." Journal of Drug Delivery and Therapeutics 9, no. 2-s (2019): 125–31. http://dx.doi.org/10.22270/jddt.v9i2-s.2471.
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Objectives: The aim of present investigation was formulation development and evaluation of bi-layer tablets of citicoline sodium. Materials and Methods: An aqueous granulation process was adopted to formulate citicoline sodium (CTS) bilayer tablets. Wet granulation method has been utilized for the formulation of bilayer CTS tablet. Citicoline sodium, microcrystalline cellulose (pH 101 & 102), HPMC K4, K15, K-100, PVP K-30, Magnesium stearate, cross-carmellose sodium, sodium starch glycolate and red oxide were used for preparation. Pre-formulation studies of citicoline sodium and drug excipient compatibility study was carried to optimize the formulation variables. Two layers, immediate release (IR layer) and sustained release (SR) has been developed and evaluated for the various parameters e.g. micromeritic properties, percentage yield, particle size, hardness, thickness, weight variation, percent friability and percent assay, In-vitro dissolution and In-vitro release studies. Result and Discussion: Pre-formulation study of citicoline sodium denotes that evaluated parameters confirm the suitability and compliance of drug with polymers. Drug excipient compatibility study through the DSC confirmed that polymer, excipient and drug were compatible with each other and no incompatibility issue found during the preparation of formulation. FT-IR study is also executed to confirm the drug-excipient incompatibility. In all physical mixtures of drug and polymer, there was neither masking of single characteristic peak nor existence of additional peak in drug spectra; this has proven that drug and polymers are compatible with each other. Hardness 10-11 kg/cm2, thickness 7.3-7.4 mm, percent weight variation 1.2%, friability 0.1-0.3%, assay was 99-101% denotes the successful development of CTS tablets. Conclusion: These all parameters denote that the formulation has optimized, evaluated and were in the standard range. Hence, this optimized bilayer tablet formulation could be a potential formulation to promote sustained release, promote delivery of drugs from a single dosage form to improve patient compliance and give better disease management. Keywords: Citicoline sodium, bi-layer tablet, DSC, immediate release, sustain release.
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Langhorne, Samuel. "Theoritical Uses of Pramipexole dihydrochloride in Parkinson's Resistance Depression." Psychology and Mental Health Care 1, no. 2 (2017): 01–03. http://dx.doi.org/10.31579/2637-8892/045.
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Pramipexole dihydrochloride monohydrate is an antiparkinson’s agent which is known as dopamine D2 receptor agonist. It is structurally different from the ergot-derived drugs, e.g. bromocriptine or pergolide. Pramipexole is designated chemically as (S)-2-Amino-4, 5, 6, and 7-tetrahydro-6-(propylamino) benzothiazole and has the molecular formula C10H17N3S. It comes under class I of Biopharmaceutical Classification System. The purpose of this study was to develop and evaluate pramipexole dihydrochloride monohydrate extended release tablets by wet granulation method using different proportions of polymers and binder. Pre-formulation studies were done initially and the results were found to be within the limits. All the mentioned batches were prepared and granules were evaluated for pre-compression parameters such as loss on drying, bulk density, tapped density and compressibility index. Tablets were evaluated for weight variation, thickness, hardness, friability; disintegration time and assay were found to be within the limits. In vitro dissolutions were performed with 0.05M 6.8 PH phosphate buffer and effect of various polymers were explored. Final selection of formulation was based on dissolution profile, from dissolution studies formulation 9 showed 80% drug release within 20 hours, so it will be compared with innovator. Similarity and difference factors which revealed that formulation (F 9) containing HPMC K 200, Eudragit L100 and binder are most successful as it exhibited in vitro drug release that matched with innovator product. In vitro drug release profile reveals that with increased concentration of Eudragit L 100. Accelerated stability studies were performed for the optimized batch which indicated that there were no changes in drug content and in vitro dissolution.
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Chaturvedi, Prateek Kumar, Rajesh Gour, Janki Prasad Rai, and Akhlesh Kumar Singhai. "Development and Evaluation of Losartan Potassium Floating Matrix Tablet." Journal of Drug Delivery and Therapeutics 12, no. 3-S (2022): 106–14. http://dx.doi.org/10.22270/jddt.v12i3-s.5388.
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The present study was aimed towards the development of controlled release formulations of Losartan Potassium based on designed to enhance the bioavailability by prolonging its duration in the stomach via the floating dosage forms with controlled release. This study was intended to evaluate the influence of formulation variables like levels of polymer, amount of mannitol concentrations, and coating solution ratios of semi permeable membrane on the drug release from the developed formulations. Thus, there is a strong clinical need and market potential for a dosage form that will deliver Losartan Potassium in a controlled manner to a patient needing this therapy, thereby resulting in a better patient compliance. This study was designed to enhance the bioavailability of drug by prolonging its duration in the stomach via the floating dosage forms with controlled release. Floating matrix tablets of Losartan Potassium were prepared by the direct compression method, using locust bean gum and HPMC K 15M as polymers and Sodium bicarbonate as floating agent. The effect of the nature of polymers was studied by preparing various formulations of tablets. In all these formulations, a constant amount of drug (100 mg) was maintained. The blend was initially characterized for pre-compression and post- compression parameters. Pre-compression characterization was done for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio. The results of pre-compression characterization were indicated good to excellent flow characteristics. Post-compression characterization includes thickness, hardness, friability, weight variation, drug content, buoyancy lag time, floating time and in-vitro drug release. All the results were satisfactory as per the guideline of pharmacopoeia. The in vitro drug release studies found that formulations LPFT4 showed best sustained release profile in 24 hrs. Among the nine formulations (LPFT1 to LPFT9) prepared formulations LPFT4 was found to be the best formulations in terms of sustained drug release. Drug release kinetics was performed by using various kinetic models such as Zero order, First order, Korsmeyer- Peppas and Higuchi’s equation and followed supercase II transport diffusion kinetic models.
 Keywords: Oral drug delivery system, Gastroretentive technology, losartan potassium, floating tablet, matrix tablet
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Dr., M. Sunitha Reddy* Goparaju Ramya S. Muhammad Fazal Ul Haq. ""FORMULATION AND EVALUATION OF CONTROLLED RELEASE TABLET DOSAGE FORM OF NAPROXEN SODIUM USING BILAYER TECHNOLOGY"." November 30, 2018. https://doi.org/10.5281/zenodo.2530470.
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The goal of present study is to formulate and evaluate controlled release dosage form of Naproxen sodium using bilayer tablet technology, by wet granulation process. During this wet granulation process various parameters were studied like granulation , dried granules LOD, compression parameters and formula was optimized. In this wet granulation process various controlled release polymers were used like HPMC K4M, HPMC K15, HPMC K 100. Among the used polymers HPMC K4M Showed the high retarding the drug release rate, due to it contain high viscosity in nature. The drug and excipient computability studies and Preformulation studies were performed. In vitro dissolution test was performed by using USP type II (Paddle) apparatus, 1000 ml of phosphate buffer pH7.5 and the paddle was rotated at 50 rpm at temperature (37ºC ± 0.5ºC) similar as that of reference listed drug. The finished tablets were subjected to evaluation parameters and study on pH of different media were studied on controlled release tablets. Three months Stability studies indicate that it was similar as that of innovator product.
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Swathy, G. Panicker* K.Nithyapriya Anoop John SumeeshNath Nimsha Krishnan Vaijayanthi CM Pankaj H. Toshar Barish M. "Formulation And Evaluation Of Once Daily Ciprofloxacin Hcl Extended Release Matrix Tablet." February 28, 2013. https://doi.org/10.5281/zenodo.2348996.
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Ciprofloxacin HCl has invitro activity against a wide range of gram – negative and gram – positive organisms. The bactericidal action of Ciprofloxacin HCl results from inhibit the enzyme bacterial DNA gyrase (topoisomerase II ).The main objective of this research work was to prepare Ciprofloxacin HCl matrix tablet using HPMC as the polymer and invitro drug release study. In the present study wet granulation method is used for preparing the matrix tablet. Different grades of HPMC were used for the formulation such as, HPMCK 100 LVEP, HPMC K 4M, HPMC E10MCR, HPMC K15M, HPMCK100M. During preparation, all powders were mixed and are then passed through 60# sieve and then granulated using PVP 30 in Isopropyl alcohol and are dried for 2 hours and again passed through 16# sieve. The dried granules were then mixed in poly bag using magnesium stearate and talc. Granules were then punched using rotary tablet machine .The extended release matrix tablet were subjected to in vitro release using USP 2 apparatus. Formulation F14 shows 99.36 % drug release in 24th hour. Stability studies were performed for optimized batch. The optimized formulation F14 showed better stability when stored at 40◦c under 75% RH for one month. From similarly factor F2 of F 14 trial batch shows that dissolution profile matches with the marketed product Cifran. Thus it is concluded that HPMC matrix tablet of Ciprofloxacin can be prepared by Wet granulation method and invitro release data is satisfactory.
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Pradip, Das*1 R. P. Ezhil muthu2 Diptanu Biswas3. "Formulation and Evaluation of L-arginine Sustained Release Tablets." INDO AMERICAN JOURNAL OF PHARMACEUTICAL RESEARCH 01, no. 04 (2011). https://doi.org/10.5281/zenodo.2270149.
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L-Arginine is an amino acid that has numerous functions in the body. In the body L-Arginine is used to make nitric oxide which reduces blood vessels Stiffness, increases blood flow and improves blood vessel function. L-Arginine also used for erectile dysfunction by enhancing the action of Nitric Oxide, which relaxes muscle surrounding blood vessels supplying to the penis. As a result blood vessels in the penis dilate, increasing blood flow which helps to maintain an erection. Due to its less biological half life i.e., ≥ 1hours in India L-Arginine was available in 5-8 gms of granules and 1050 mg capsule and intake of dose is twice daily whose dosage quantity is much more. This can be overcome by formulating Sustained Release tablet of L-Arginine 525 mg twice daily. The tablet can be developed with the combination of 30% HPMC- K 100 and HPMC -K 15 M Polymer which can retard the drug release up to 12 hours.
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Panpaliya, Dinesh V., Atish Y. Sahare, Priyanka Lanje, and Pooja Dhoke. "Formulation Development and Evaluation of Sustained Release Microsphere of Levetiracetam." International Journal of Pharmaceutical Sciences Review and Research 71, no. 2 (2021). http://dx.doi.org/10.47583/ijpsrr.2021.v71i02.026.
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The aim of the present work was to develop and evaluate of oral microsphere of Levetiracetam to reduce the frequency of dosing by achieving 12 hours sustained drug release. The microsphere formed will also mask the bitter taste of the drug and thus increase the compatibility of the drug with the patients. Levetiracetam is a second-generation anti-epileptic agent useful in the treatment of partial onset and monoclinic seizures. It has a short half life of 7 hours and its recommended dose is 500 mg twice a daily. Microspheres are suitable drug delivery system for such drug candidate. For these reasons it is must to formulate a suitable dosage form by which it will be easier to administer the dose and also to get a sustained drug release hence microsphere was prepared using solvent evaporation method. Preformulation studies were carried out to rule out any drug polymer interaction by FTIR technique. In this study formulation was done solvent evaporation method using different percentage of HPMC– K 100, HPMC- K 15 and coated with Eudragit S100. Drug, polymer and physical mixture were evaluated for in compatibility study by Fourier transforms infrared spectroscopy. All the batches of microsphere (F1 to F5) were subjected for in vitro dissolution. Microsphere was evaluated for surface morphology, micromeritics properties, entrapment efficiency and in vitro drug release. The entrapment efficiency of microsphere ranged from 71.16%-73.66%. The size of the prepared microsphere ranges between 42.8 µm to 55.64 µm which was found to increase with increase in RPM at same polymer ratio. Micromeritics studies showed good flow properties. Among the microsphere batches, F5 was observed as an optimized batch as its formulation with polymer i.e. Eudragit-S 100 and HPMC-K 100 was found to be release in sustained manner. The F-5 batch shows is 79.45% drug release at the end of 7 hrs and its stability study indicate that these microspheres were stable at selected temperature and humidity
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Kiran, R. Shireesh, B. Chandra Shekar, and B. Nagendra Babu. "Formulation and Pharmacokinetic Evaluation of Ritonavir Floating Tablets in the Management of AIDS." International Journal of Pharmaceutical Sciences and Drug Research 10, no. 6 (2018). http://dx.doi.org/10.25004/ijpsdr.2018.1006010.
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In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.
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Kiran, R. Shireesh, B. Chandra Shekar, and B. Nagendra Babu. "FORMULATION AND PHARMACOKINETIC EVALUATION OF RITONAVIR FLOATING TABLETS IN THE MANAGEMENT OF AIDS." International Journal of Pharmaceutical Sciences and Drug Research, January 1, 2018, 492–96. http://dx.doi.org/10.25004/ijpsdr.2018.100610.
Full textAbstract:
In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16µg/mL, 8.00±1.23 h and 173 ± 26.34µg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.
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"Formulation and Evaluation of Sustained Release Matrix Tablet of Itopride." American Journal of PharmTech Research 11, no. 5 (2021). http://dx.doi.org/10.46624/ajptr.2021.v11.i5.008.
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The objective of this research work was to carry out design and evaluation of sustained release matrix tablets of Itopride by use of natural and synthetic polymers. Matrix tablets were prepared by wet granulation technique by using natural polymers like Carbopol 934, Tamarind poly saccharide, Locust bean gum, Ethyl cellulose, HPMC K 100 as matrix forming agent and excipients such as Lactose, Starch 1500, Magnesium stearate, MCC and talc were used. The dissolution medium consisted of 900 ml of 0.1 N HCl for first 2 hours and then 7.4 phosphate buffer for remaining 10 hours. The release of Itopride from matrix containing lactose, micro crystalline cellulose and starch 1500 as diluents. The drug release rate was found in order of lactose> micro crystalline cellulose>starch 1500. The formulation was optimized on the basis of acceptable tablet properties and in-vitro drug release. The release data were fit into different kinetic models (zero-order, first- order, Higuchi’s equation and Korsmeyer-Peppas equation). Optimized formulation was tested for their compatibility with Itopride by FT-IR studies, which revealed that there is no chemical interaction occurred with polymer and other excipients. The drug release profile of the best formulation was well controlled and uniform throughout the dissolution studies. Keywords: Matrix tablets, Itopride, Carbopol 934, HPMC K 100, Ethyl cellulose.