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Devi Thamizhanban, Gampa Tulja Rani, and Kathiresan krishnasamy. "Development of bio-relevant dissolution method for prognosis of In-vivo performance of Dipyridamole from modified release capsules." International Journal of Research in Pharmaceutical Sciences 11, no. 2 (May 7, 2020): 2340–49. http://dx.doi.org/10.26452/ijrps.v11i2.2211.
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In-vitro biorelevant dissolution test method was developed for Dipyridamole in modified release multi-particulate dosage form, to simulate the product drug release after oral administration to human. The Dipyridamole concentration in blood plasma achieved after oral administration under pre-prandial (fasting) condition were used for deriving the target dissolution profile deconvoluting the plasma concentration using numerical deconvolution technique. The fraction of drug absorbed was considered as the target dissolution profile. The drug product was tested by using the dissolution method recommended by office of generic drugs, and the dissolution results observed are not comparable with the target dissolution profile. Dissolution method was developed using reciprocating cylinder, Bio-Dis (apparatus -3 as per USP), by simulating the pre-prandial conditions. A full factorial design of experiment was carried out to achieve the target dissolution profile. Media volume and dips per minute (DPM) are considered as main factors, in design of experiment. The dissolution results achieved with media volume 250ml and 10DPM were found to be comparable with target dissolution profile and observed with the F2 value (similarity factor) of 92%. The developed dissolution method demonstrates a very good in-vitro/in-vivo correlation under pre-prandial condition, and shall be used as a predictive in-vitro tool for evaluation Dipyridamole extended release capsules.
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Janeva, Emilija, Liljana Anastasova, Irena Slaveska Spirevska, Tatjana Rusevska, Tanja Bakovska Stoimenova, Teuta Ibrahimi, and Rumenka Petkovska. "A comparative in vitro dissolution study of generic moxifloxacin immediate-release film coated tablets and referent pharmaceutical product." Macedonian Pharmaceutical Bulletin 64, no. 02 (2019): 27–34. http://dx.doi.org/10.33320/maced.pharm.bull.2018.64.02.003.
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Dissolution testing of generic immediate release solid dosage forms represents a valuable tool to obtain dissolution profiles and to establish the similarity/dissimilarity between tested dosage forms. In this study, the in vitro dissolution profiles of generic immediate-release moxifloxacin (MOX) film coated tablets and a referent pharmaceutical product were compared and evaluated. The dissolution behavior of the generic product was investigated in three different dissolution media (pH=1.2, 4.5 and 6.8). The amount of dissolved MOX was determined using validated UV spectrophotometric method. For comparison of the dissolution behavior, the similarity factor, f2, was used. The dissolution profile of the generic product showed a release of >85 % MOX in the time frame of 30 min, in all the tested dissolution media. The similarity factor, f2, calculated from the comparison of the dissolution profiles of the generic and the referent pharmaceutical product in pH=1.2 dissolution medium was 50, 58, thus the products were established as similar. Based on the results of our study, the dissolution similarity between the generic MOX immediate-release film coated tablet and the referent product could be successfully used as a part of the approach to ensure their in vivo bioequivalence. Keywords: moxifloxacin, immediate-release solid dosage forms, dissolution, in vitro similarity
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Dandam, Ponjul, and Jennifer D. Audu-Peter. "Assessment of the pharmaceutical equivalence and in vitro dissolution studies of amlodipine tablets marketed in Northern Nigeria." Journal of Pharmacy & Bioresources 17, no. 2 (April 9, 2021): 200–207. http://dx.doi.org/10.4314/jpb.v17i2.14.
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The extensive supply of poor quality and/or counterfeit drug products in many developing countries has made it vital to frequently carry out suitable tests to assess bioequivalence (BE) in a cost-effective manner. This study was intended to assess the pharmaceutical equivalence and dissolution profile of amlodipine 5mg tablets marketed in Jos and Kaduna metropolis. Ten brands of Amlodipine 5mg tablets were obtained from different community pharmacies and evaluated for different quality control parameters such as percent drug content, friability, hardness, thickness, weight uniformity, disintegration time, and dissolution. The results showed that brands F and I failed the test for percent drug content while the rest of the brands passed it. In addition, all the brands passed the disintegrationand friability test while Brands C, F and I did not pass the hardness test. The dissolution profiles of all the brands were similar to the innovator brand at pH 6.8, whereas at pH 1.2, only four brands (B, E, H and I) had similar dissolution profile to the innovator. This study serves to justify for the assessment of in vitro parameters of commercially available amlodipine generics which may aid the prescribers’ decision making.
Keywords: Amlodipine; Jos; Tablet properties, Dissolution profile
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Medina, Jose Raul, Mariel Cortes, and Erik Romo. "COMPARISON OF THE USP APPARATUS 2 AND 4 FOR TESTING THE IN VITRO RELEASE PERFORMANCE OF IBUPROFEN GENERIC SUSPENSIONS." International Journal of Applied Pharmaceutics 9, no. 4 (July 13, 2017): 90. http://dx.doi.org/10.22159/ijap.2017v9i4.19926.
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Objective: The aim of this study was the comparison of the in vitro release performance of ibuprofen generic suspensions and reference, based on the hydrodynamic environment generated by the flow-through cell method (USP Apparatus 4). Results were compared with those obtained by the use of the USP Apparatus 2.Methods: The Advil® suspension (2 g/100 ml) and two generic formulations with the same dose were tested. Dissolution studies were carried out using a USP Apparatus 4 Sotax CE6 with 22.6 mm cells, laminar flow at 16 ml/min, and pH 7.2 phosphate buffer at 37.0±0.5 °C as dissolution medium. Ibuprofen was quantified spectrophotometrically at 222 nm. The in vitro release of the three drug products were studied using the USP Apparatus 2. The dissolution profiles of generic products were compared with the reference by model-independent, model-dependent, and analysis of variance (ANOVA)-based comparisons.Results: The dissolution profile of the generic product A was similar to the dissolution profile of reference, only with the use of the USP Apparatus 4. The f2 similarity factor was>50 and no significant differences were found with dissolution efficiency data (*P>0.05). Similar results were found with the comparison of t50% and t63.2% values. Similar dissolution profiles between generic product A and reference were also found with ANOVA-based comparisons.Conclusion: The flow-through cell method was adequate for study the in vitro release of ibuprofen suspensions. It is necessary to evaluate the in vivoperformance of the drug products used in order to estimate the predictability of the proposed methodology.
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Begum, Rehana, Md Zakir Sultan, Jakir Ahmed Chowdhury, and Md Shah Amran. "In vitro Pharmaceutical Equivalence Study of Three Brands of Atenolol Tablets Available in Bangladesh." Dhaka University Journal of Pharmaceutical Sciences 18, no. 1 (May 16, 2019): 43–48. http://dx.doi.org/10.3329/dujps.v18i1.41426.
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The aim of the present work was to assess the pharmaceutical equivalence of three brands of atenolol (50 mg) tablets available in Bangladesh using in vitro dissolution study. The dissolution study was carried out using the paddle apparatus according to the guidelines of United States Pharmacopoeia (USP). The dissolution profiles of three locally manufactured atenolol tablets were determined and compared with the dissolution profile of atenolol tablet from innovator’s company. All samples attained more than 85% dissolution within 10 minutes. Mean dissolution values were employed to estimate difference factor (f1) and similarity factor (f2). Difference factor (f1) and similarity factor (f2) were used to assess in vitro bio-equivalency among the three brands. Other general quality assessment parameters such as hardness, friability and disintegration time were also determined. All brands complied with the official specifications for hardness, friability and disintegration time. The study indicated that all brands can be prescribed interchangeably.
Dhaka Univ. J. Pharm. Sci. 18(1): 43-48, 2019 (June)
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Duque, Marcelo Dutra, Daniela Amaral Silva, Michele Georges Issa, Valentina Porta, Raimar Löbenberg, and Humberto Gomes Ferraz. "In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation." Pharmaceutics 11, no. 5 (May 5, 2019): 215. http://dx.doi.org/10.3390/pharmaceutics11050215.
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A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution. This study aimed to simulate plasma concentrations of fluconazole capsules with different dissolution profiles and run population simulation to evaluate their bioequivalence. The dissolution profiles of two batches of the reference product Zoltec® 150 mg capsules, A1 and A2, and two batches of other products (B1 and B2; C1 and C2), as well as plasma concentration–time data of the reference product from the literature, were used for the simulations. Although products C1 and C2 had drug dissolutions < 85% in 30 min at 0.1 M HCl, simulation results demonstrated that these products would show the same in vivo performance as products A1, A2, B1, and B2. Population simulation results of the ln-transformed 90% confidence interval for the ratio of Cmax and AUC0–t values for all products were within the 80–125% interval, showing to be bioequivalent. Thus, even though the in vitro dissolution behavior of products C1 and C2 was not equivalent to a rapid dissolution profile, the computer simulations proved to be an important tool to show the possibility of bioequivalence for these products.
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Patrício, José P. H., Cristina Santos, and Rui Cerdeira. "In Vitro Dissolution Profile of Two Commercially Available Iron Preparations." Drugs in R&D 12, no. 1 (March 2012): 35–40. http://dx.doi.org/10.2165/11631560-000000000-00000.
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Kazandjievska, Elena, Iva Antova, Slavica Mitrevska, Aleksandar Dimkovski, Elena Dimov, Maja Hadzieva Gigovska, Packa Antovska, Sonja Ugarkovic, Jasmina Tonic Ribarska, and Suzana Trajkovic-Jolevska. "Non-compendial vs compendial analytical tests - a powerful tool for predicting in vitro similarity of highly viscous oral suspension." Macedonian Pharmaceutical Bulletin 64, no. 02 (2019): 61–72. http://dx.doi.org/10.33320/maced.pharm.bull.2018.64.02.007.
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In vitro dissolution profiles are increasingly used to evaluate drug release characteristics of pharmaceutical products. The dissolution methods is expected to be an appropriate tool for checking consistency of the pharmaceutical attributes by discriminating similarities and dissimilarities between different drug formulations. Expansion in development of novel “special” dosage forms, due to the manner in which these dosage forms release the active pharmaceutical ingredient, usually requires applying non-compendial dissolution strategy that differs from the traditional compendial recommendations. For demonstrating sameness in the dissolution profile, in vitro drug release comparison between test and reference product of highly viscous oral suspension by applying non-compendial peak vessel against conventional hemispheric vessel was demonstrated in this study. All reference batches exhibited high variability in dissolution data when using hemispheric vessel due to forming mound compact mass at the bottom of the vessel. Different strategies for samples manipulation, before and during dissolution period, were performed in order to eliminate additional variabilities. Modifications of conventional USP 2 apparatus such as using peak vessel provided with more reproducible and reliable result for distinguishing in vitro similarities between different formulations of oral suspensions. Misinterpretation of dissolution data can lead to negative impact on product development. Taking time to observe and evaluate what is happening to the product in the vessel during dissolution is of curtail consideration for proper selection of the dissolution strategy. Keywords: oral suspensions; in-vitro release; hydrodynamic variability; USP apparatus 2/ Paddle apparatus; peak vessel
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T N K, Suriyaprakash, S. Lakshmana Prabu, Arumugarajan A, and Sumathi A. "Formulation and Evaluation of Oral Controlled Release Clarithromycin Matrix Tablets using Hydrophilic Polymer." International Journal of Pharmaceutical Sciences and Nanotechnology 6, no. 4 (December 31, 2013): 2255–59. http://dx.doi.org/10.37285/ijpsn.2013.6.4.8.
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The objective of the present study was to develop clarithromycin tablets from polymeric hydrophilic matrices using methocel and characterization for its physic-chemical properties and in vitro release studies to optimize its release profile with the standard marketed product. Matrix tablets were prepared by wet granulation method using PVP and ethyl cellulose as binding agents. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and in vitro release studies. The drug delivery was analyzed using the paddle method in phosphate buffer pH 6.0 (dissolution medium I) and phosphate buffer pH 6.8 containing 0.5% sodium lauryl sulfate (dissolution medium II) and compared with USP dissolution limits. The dissolution release profile of formulation F9 was comparable with the market formulation and the difference factor and similarity factor f1 and f2 was found to be 2.44 and 83.18 in dissolution medium I; 1.44 and 89.71 in dissolution medium II. Stability studies were carried out as per ICH guidelines and tested for its physicochemical properties and in vitro studies. The study shows that the matrix method can be employed for preparing clarithromycin sustained release formulation using combination of hydrophilic polymers like Methocels and sodium carboxy methyl cellulose.
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Hailu, Gebremedhin Solomon, Girma Belachew Gutema, Hailemichael Zeru Hishe, Yimer Said Ali, and Adissu Alemayehu Asfaw. "Comparative In vitro Bioequivalence Evaluation of Different Brands of Amoxicillin Capsules Marketed in Tigray, Ethiopia." International Journal of Pharmaceutical Sciences and Nanotechnology 6, no. 1 (May 31, 2013): 1966–71. http://dx.doi.org/10.37285/ijpsn.2013.6.1.7.
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The availability of multisource generic brands of amoxicillin in the market today places health professionals and patients in a difficult situation about the choice of a suitable product among numerous generic brands. The purpose of this study was to estimate the bioequivalence of amoxicillin capsules marketed in Ethiopia using in vitro tests in order to determine their interchangeability. The in vitro dissolution study was carried out on the six brands of amoxicillin capsules according to USP guidelines. To compare the dissolution profiles, a difference factor (f1), similarity factor (f2), dissolution efficiency (DE) and statistical methods were employed. Results have shown significant differences in the dissolution profiles of the brands based on the statistical analysis (p<0.0001). Pair-wise comparisons using Dunnett’s test indicated that the innovator brand has a significantly faster dissolution than the generic brands, except brand D. According to f1, f2 and DE calculations, only brand D was found to have similar dissolution profile with the innovator. Based on the in vitro studies, only brand D may be considered bioequivalent and interchangeable, while the other brands may not be considered bioequivalent and interchangeable with the innovator brand. This research highlights among other things the need for constant monitoring and surveillance on the marketed drugs by regulatory bodies to ascertain bioequivalence and quality medicines, especially for drugs like amoxicillin for which there exists evidence of non-bioequivalence from different firms, resulting in efficacy issues.
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Shah, Vinod P., Norlin W. Tymes, Lawrence A. Yamamoto, and Jerome P. Skelly. "In vitro dissolution profile of transdermal nitroglycerin patches using paddle method." International Journal of Pharmaceutics 32, no. 2-3 (October 1986): 243–50. http://dx.doi.org/10.1016/0378-5173(86)90185-7.
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Stolk, L. M. L., R. Rietbroek, E. H. Wiltink, and J. J. Tukker. "Dissolution profiles of mesalazine formulationsin vitro." Pharmaceutisch Weekblad Scientific Edition 12, no. 5 (October 1990): 200–204. http://dx.doi.org/10.1007/bf01980047.
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Chowdhury, Mohammed Motaher Hossain, Abedah Nawreen, and Md Sohel Rana. "Formulation Development and In vitro Evaluation of Combination Product of Glyburide and Metformin Hydrochloride Tablet." Bangladesh Pharmaceutical Journal 16, no. 2 (February 20, 2015): 195–203. http://dx.doi.org/10.3329/bpj.v16i2.22304.
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This study was attempted to formulate a combination product of Glyburide and Metformin Hydrochloride Tablets USP 2.5mg/500mg and to evaluate their physico-chemical properties. Wet granulation method was adopted for preparation of tablet using different excipients namely Microcrystalline cellulose, Povidone K-30, Copovidone, Croscarmellose sodium and Sodium stearyl fumerate in six different formulations (F1-F-6). The granules for tabletting were evaluated for angle of repose, bulk density, tapped density, compressibility index and drug content etc. The tablets were subjected to thickness, hardness, friability, disintegration and in vitro release studies. The results of physical parameters of tablets showed that there were capping, hardness and friability problems in formulation F-1, F-2 and F-3. Granules of formula F-4, F-5 and F-6 showed satisfactory flow properties, compressibility index and the physical parameters of tablets from these three formulations gave optimum result in comparison to innovator's brand. Disintegration time of these three formulations (7-8 min) was found similar with innovator's brand (6.30-7.30 min). Assay of formula F-6 of glyburide (97.97%) and Metformin Hydrochloride (100.2%) met the USP specification (90%-110%). It was also found that dissolution profile of Glyburide depends on particle size of Glyburide powder. When micronized and non micronized grade of Glyburide was used in a ratio of 3:1 (F-6) it gave similar dissolution profile as innovator's brand where the similarity factor (f2) was calculated as 59. On the other hand, dissolution profile of Metformin hydrochloride was found similar in all the three formulations (F-4, F-5, F-6) with reference to innovator having all f2 values above 50. Formulation F-6 possessed good stability in accelerated condition for 6 months study. By comparing the dissolution profiles with the innovator's drug glucovance® tablet, it was revealed that the formulation F-6 exhibit similar drug release profile for both Glyburide and Metformin Hydrochloride. DOI: http://dx.doi.org/10.3329/bpj.v16i2.22304 Bangladesh Pharmaceutical Journal 16(2): 195-203, 2013
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Lee, Dong-Seok, Dong Wook Kang, Go-Wun Choi, Han-Gon Choi, and Hea-Young Cho. "Development of Level A In Vitro–Vivo Correlation for Electrosprayed Microspheres Containing Leuprolide: Physicochemical, Pharmacokinetic, and Pharmacodynamic Evaluation." Pharmaceutics 12, no. 1 (January 2, 2020): 36. http://dx.doi.org/10.3390/pharmaceutics12010036.
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This study optimized the preparation of electrosprayed microspheres containing leuprolide and developed an in vitro–in vivo correlation (IVIVC) model that enables mutual prediction between in vitro and in vivo dissolution. The pharmacokinetic (PK) and pharmacodynamic (PD) study of leuprolide was carried out in normal rats after subcutaneous administration of electrosprayed microspheres. The parameters of the IVIVC model were estimated by fitting the PK profile of Lucrin depot® to the release compartment of the IVIVC model, thus the in vivo dissolution was predicted from the in vitro dissolution. From this correlation, the PK profile of leuprolide was predicted from the results of in vivo dissolution. The IVIVC model was validated by estimating percent prediction error (%PE) values. Among prepared microspheres, an optimal formulation was selected using the IVIVC model. The maximum plasma concentration and the area under the plasma concentration–time curve from zero to infinity from the predicted PK profile were 4.01 ng/mL and 52.52 h·ng/mL, respectively, and from the observed PK profile were 4.14 ng/mL and 56.95 h·ng/mL, respectively. The percent prediction error values of all parameters did not exceed 15%, thus the IVIVC model satisfies the validation criteria of the Food and Drug Administration (FDA) guidance. The PK/PD evaluation suggests that the efficacy of OL5 is similar to Lucrin depot®, but the formulation was improved by reducing the initial burst release.
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Costa, Mayre Aparecida Borges da, Ana Lucia Vazquez Villa, Rita de Cássia da Silva Ascenção Barros, Eduardo Ricci-Júnior, and Elisabete Pereira dos Santos. "Development, characterization and evaluation of the dissolution profile of sulfasalazine suspensions." Brazilian Journal of Pharmaceutical Sciences 51, no. 2 (June 2015): 449–59. http://dx.doi.org/10.1590/s1984-82502015000200022.
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<p>This paper reports the development, characterization and <italic>in vitro</italic>dissolution behavior of sulfasalazine suspensions for treatment of chronic intestinal inflammatory diseases. Three formulations were developed, from powdered sulfasalazine obtained from different suppliers. The sulfasalazine was characterized regarding concentration, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), particle size distribution, polydispersion and solubility. The suspensions were developed and characterized regarding pH, viscosity, density, particle size, sedimentation volume, concentration and dissolution. The pH values were slightly acidic. The method of preparing the suspensions reduced the particle sizes and made the size distribution more homogeneous. The dissolution studies showed that the sulfasalazine suspensions had low solubility in acidic media, but dissolve quickly, reaching levels of 85%, in neutral media or media containing 0.5% of surfactants such as polysorbate 80. Besides this, the sulfasalazine suspensions were classified as having immediate dissolution because they reached dissolution levels near 100% in 20 minutes.</p>
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Brahmaiah, B., K. Sasikanth, Sreekanth Nama, P. Suresh, and Patan Adam Khan. "Formulation and Dissolution Study of Valsartan Immediate Release Tablets." Indian Journal of Pharmaceutical and Biological Research 1, no. 02 (June 30, 2013): 01–08. http://dx.doi.org/10.30750/ijpbr.1.2.1.
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In the present study, design of oral immediate release tablets of Valsartan by direct compression technique was carried out. The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV’S) in different ratios. The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate. To determine the best fit dissolution profile for the dosage forms. Valsartan tablets were formulated by using microcrystalline cellulose (diluents), potato starch, acacia (binder) and magnesium stearate (lubricant). The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. The In-vitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.
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Uzunović, Alija, Edina Vranić, and Šeherzada Hadžidedić. "Impairment of the in vitro Release of Carbamazepine from Tablets." Bosnian Journal of Basic Medical Sciences 10, no. 3 (August 20, 2010): 234–38. http://dx.doi.org/10.17305/bjbms.2010.2693.
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Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine. As model tablets for this investigation, two formulations (named “A” and “B” formulations) of carbamazepine tablets labeled to contain 200 mg were evaluated. The aim of this study was to establish possible differences in dissolution profile of these two formulations purchased from the local market.The increased crystallinity together with enlarged particle size, enhanced aggregation and decreased wettability of the drug, resulted in insufficient dissolution rate for formulation “B’.’ From the dissolution point of view, this formulation was inferior to the formulation “A, due to the solubilization effect.
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Ilić, Marija, Ivan Kovačević, and Jelena Parojčić. "Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect." Acta Pharmaceutica 65, no. 4 (December 1, 2015): 427–41. http://dx.doi.org/10.1515/acph-2015-0039.
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Abstract With the increased reliance on in vitro dissolution testing as an indicator of in vivo drug behavior and the trend towards the in silico modeling of dosage form performance, the need for bioperformance dissolution methodology development has been enhanced. Determination of the in vivo drug delivery profile is essential for the bioperformance dissolution test development and in vitro/in vivo correlation modeling, as well as the understanding of absorption mechanisms. The aim of this study was to compare different methods in terms of their usefulness and applicability in deciphering in vivo delivery of nifedipine administered in modified release dosage forms. A detailed survey of publications on nifedipine pharmacokinetics was done and used to identify the magnitude of food effect. In vitro dissolution testing was performed under various experimental conditions. Obtained results indicate the potential for using the developed in silico model coupled with discriminative in vitro dissolution data for identification of the in vivo drug product behavior
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Fries, Aline Taís, Natália Olegário, Sarah Chagas Campanharo, Vitor Paulo Pereira, and Martin Steppe. "EVALUATION OF THE PRESENCE OF POLYMORPHIC FORMS AND INFLUENCE ON THE DISSOLUTION PROFILE OF TENOXICAM IN ACTIVE PHARMACEUTICAL INGREDIENT AND FORMULATIONS." Drug Analytical Research 2, no. 2 (December 16, 2018): 27–36. http://dx.doi.org/10.22456/2527-2616.90005.
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Polymorphism is a relatively common phenomenon among pharmaceutical compounds, and one of the main aspects to be considered in the production and development of medications. The investigation of polymorphism associated with oxicams, a group belonging to the class of non-steroidal anti-inflammatory drugs (NSAIDs) has increased in recent years and, in the case of tenoxicam, the existence of four polymorphic forms is reported in the literature. The objective of this study was to characterize the presence of different polymorphic forms of tenoxicam in active pharmaceutical ingredient and oral pharmaceutical formulations, as well as to evaluate the influence on in vitro dissolution. The characterization of the three samples of pharmaceutical ingredient of tenoxicam from different suppliers by X-Ray Diffraction (XRD), Infrared (IR) and dissolution profile indicated the presence of a form III crystalline structure, without presenting significant differences between the in vitro dissolution profiles analyzed, and a Dissolution Efficiency (DE%) of 60.30%, 60.70% and 72.34%, respectively. When the four pharmaceutical specialties of tenoxicam were submitted to XRD analysis, they also presented form III crystalline structures. Despite this, the formulations presented different dissolution profiles and a DE% of 75.23%, 83.69%, 78.19% and 90.63%, respectively, without compromising their quality. However, often polymorphism affects physico-chemical properties of drugs, showing the importance of studying this phenomenon, by correlating the presence of crystalline structures to alterations in the quality of active ingredients and pharmaceutical products.
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Nanaki, Stavroula G., Evi Christodoulou, Nikolaos D. Bikiaris, Afroditi Kapourani, Konstantinos N. Kontogiannopoulos, Souzan Vergkizi-Nikolakaki, and Panagiotis Barmpalexis. "Leflunomide Sustained Skin Delivery Based on Sulfobetaine-Modified Chitosan Nanoparticles Embedded in Biodegradable Polyesters Films." Polymers 13, no. 6 (March 21, 2021): 960. http://dx.doi.org/10.3390/polym13060960.
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The aim of the present study was to prepare a leflunomide (LFD) sustained release transdermal delivery system for the treatment of psoriasis. In this context, LFD-loaded nanoparticles (NPs) based on either neat chitosan (CS) or CS modified with [2-(methacryloyloxy)ethyl]dimethyl-(3-sulfopropyl)ammonium hydroxide (SDAEM, a sulfobetaine zwitterionic compound) were initially prepared via ionotropic gelation and characterized in terms of in vitro dissolution, physicochemical, and antibacterial properties. Results showed that the use of the SDAEM-modified CS resulted in the formation of LFD-loaded NPs with improved wetting and solubilization properties, better in vitro dissolution profile characteristics (i.e., higher dissolution rate and extent), and improved (enhanced) antibacterial properties. The resultant LFD-loaded NPs were then embedded in suitable thin-film skin patches, prepared via spin-coating, utilizing two different biodegradable polyesters, namely methoxy polyethylene glycol-b-poly(L-lactide) (mPEG-b-PLA, at a ratio of 25/75 mPEG to PLA) and poly(lactic-co-glycolic acid) (PLGA at a ratio of 75/25 DL-lactide/glycolide copolymer). Results showed the formation of polymeric thin-films with no agglomeration (or trapped air) and uniform structure in all cases, while the LFD-loaded NPs were successfully embedded in the polymeric matrix. Analysis of the obtained in vitro dissolution profiles revealed a sustained release profile of the drug for up to approximately twelve days, while between the two proposed systems, the use of CS-SDAEM NPs (independently of the polyester type) was the most promising formulation approach.
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Olayemi, Olubunmi J., and Sophie Nock-Anyebe. "Evaluation of Novel co-processed excipient for fast disintegration of aspirin tablet formulations." Journal of Pharmacy & Bioresources 18, no. 1 (May 28, 2021): 1–11. http://dx.doi.org/10.4314/jpb.v18i1.1.
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Co-processing is a technique that ensures sub-particulate interaction of individual excipients leading to overall functionality of the resulting excipient. The aim of this study is to co-process Cyperus esculentus starch with mannitol by fusion and evaluate its effect on tablet disintegration and in vitro dissolution. Co-processed excipients were prepared from Cyperus esculentus starch and mannitol by fusion in ratios of 1:1, 1:2 and 2:1 (CM1, CM2, and CM3 respectively) and evaluated for flow and swelling properties. The excipients were incorporated into Aspirin tablet formulations at 5 %w/w by direct compression (FM1, FM2, FM3 respectively). Similar tablets were prepared using sodium starch glycolate (FSG) and the formulations were assessed for hardness, friability, wetting time, disintegrationtime and in vitro dissolution profile. All the prepared excipients possessed excellent flow with Carr’s index between 17.31 and 20.78 and Hausner ratio between 1.21 and 1.26. CM3 had the highest swelling profile (1.491) while CM2 had the lowest (1.321). Formulation FM1 had the highest tensile strength (14.12 N/cm2 ) but slower wetting time (34.33 sec) compared to FM3 with tensile strength of 11.32 N/cm2 and wetting time of 9.00 sec. Disintegration time of CM3 (4.26 min) was comparable to that of FSG (4.01 min); their dissolution profile was also found to be similar. Coprocessing Cyperus esculentus starch and mannitol by fusion (2:1) influenced tablet disintegration and in vitro dissolution and has potential to be used in manufacture of fast dissolving tablet formulations.
Keywords: Co-processing; Cyperus esculentus starch; Mannitol; Disintegration; Dissolution
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Md, Shadab, Bradon Kit, Sumeet Jagdish, Dexter David, Manisha Pandey, and Lipika Chatterjee. "Development and In Vitro Evaluation of a Zerumbone Loaded Nanosuspension Drug Delivery System." Crystals 8, no. 7 (July 12, 2018): 286. http://dx.doi.org/10.3390/cryst8070286.
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Zerumbone extracted from the volatile oil of rhizomes available from the Zinigiber zerumbet has promising pharmacological activity. However, it has poor aqueous solubility and dissolution characteristics. To improve this, a nanosuspension formulation of zerumbone was developed. Nanosuspensions were formulated using high-pressure homogenization (HPH) with sodium dodecyl sulphate (SDS) and hydroxypropylmethylcellulose (HPMC) as stabilizers; the formulation was optimized and freeze dried. The optimized nanosuspension product was evaluated using an optical light microscope, photon correlation spectroscopy (PCS), polydispersity index, zeta potential, SEM, differential scanning calorimetry (DSC) and FT-IR. The physical stability of the nanosuspensions was evaluated for 30 days at 4 °C, 25 °C, and 37 °C. To validate the theoretical benefit of the increased surface area, we determined an in vitro saturation solubility and dissolution profile. The mean particle size, polydispersity index and zeta potential of the zerumbone nanosuspensions stabilized by SDS versus HPMC were found to be 211 ± 27 nm vs. 398 ± 3.5 nm, 0.39 ± 0.06 vs. 0.55 ± 0.004, and −30.86 ± 2.3 mV vs. −3.37 ± 0.002 mV, respectively. The in vitro saturation solubility and dissolution revealed improved solubility for the zerumbone nanosuspension. These results suggested that the nanosuspensionlization improves the saturation solubility and dissolution profile of zerumbone, which may facilitate its use as a therapeutic agent in the future.
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Pop, Anca, Simona Crișan, Maria Bârcă, Anne-Marie Ciobanu, Valentin Varlas, Coriolan Pop, Mariana-Ana Pali, et al. "Evaluation of Dissolution Profiles of a Newly Developed Solid Oral Immediate-Release Formula Containing Alpha-Lipoic Acid." Processes 9, no. 1 (January 19, 2021): 176. http://dx.doi.org/10.3390/pr9010176.
Full textAbstract:
Alpha-lipoic acid (ALA, thioctic acid), a naturally-occurring essential dithiol compound, has become a common ingredient in many pharmaceutical and food supplement products (FSP), used in oxidative stress-dependent pathologies; oral bioavailability of ALA is limited by pharmacokinetic particularities that reduce its therapeutic efficacy-reduced solubility, lack of gastric stability and hepatic degradation, doubled by formulation hinders. The objectives were to develop a solid oral 600 mg ALA FSP to obtain an optimal pharmaceutical profile compared to a reference listed drug (RLD) with a similarity factor f2 50. A comparative dissolution study was performed; an HPLC method was used for ALA quantification. After planning combinatory simulations (formulation stage), two prototype formulas (#1 and #2) were manufactured and further optimized by adjusting ALA physical characteristics and the excipients quantities (#3 and #4) in order to achieve the Quality Target Product Profile. A misshapen of ALA’s in vitro release was observed for #3 Formula (f2 = 31.6); the optimal profile was obtained for Formula #4 (f2 = 58.5). A simple quantitative formula is not enough to assure good ALA bioavailability; the formulation needs multiple compounding modulations under physicochemical compatibility algorithms, with multiple dissolution profiles testing back-ups. It is essential to ensure a formulation with an in vitro dissolution comparable with the RLD, allowing the compound to reach its target level to assure the optimum claimed antioxidant activity of ALA at the cellular level, even for food supplement formulations.
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de Meira, Rafaela Zielinski Cavalheiro, Aline Biggi Maciel, Fabio Seigi Murakami, Paulo Renato de Oliveira, and Larissa Sakis Bernardi. "In Vitro Dissolution Profile of Dapagliflozin: Development, Method Validation, and Analysis of Commercial Tablets." International Journal of Analytical Chemistry 2017 (2017): 1–6. http://dx.doi.org/10.1155/2017/2951529.
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Dapagliflozin was the first of its class (inhibitors of sodium-glucose cotransporter) to be approved in Europe, USA, and Brazil. As the drug was recently approved, there is the need for research on analytical methods, including dissolution studies for the quality evaluation and assurance of tablets. The dissolution methodology was developed with apparatus II (paddle) in 900 mL of medium (simulated gastric fluid, pH 1.2), temperature set at 37±0.5°C, and stirring speed of 50 rpm. For the quantification, a spectrophotometric (λ=224 nm) method was developed and validated. In validation studies, the method proved to be specific and linear in the range from 0.5 to 15 μg·mL−1 (r2=0.998). The precision showed results with RSD values lower than 2%. The recovery of 80.72, 98.47, and 119.41% proved the accuracy of the method. Through a systematic approach by applying Factorial 23, the robustness of the method was confirmed (p>0.05). The studies of commercial tablets containing 5 or 10 mg demonstrated that they could be considered similar through f1, f2, and dissolution efficiency analyses. Also, the developed method can be used for the quality evaluation of dapagliflozin tablets and can be considered as a scientific basis for future official pharmacopoeial methods.
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Hernawan, Hernawan, Septi Nurhayati, Khoirun Nisa, A. W. Indrianingsih, Cici Darsih, and Muhammad Kismurtono. "FORMULATION AND IN VITRO STUDY OF PROPRANOLOL HYDROCHLORIDE CONTROLLED RELEASE FROM CARBOXYMETHYL CHITOSAN-BASED MATRIX TABLETS." Indonesian Journal of Chemistry 13, no. 3 (December 18, 2013): 242–47. http://dx.doi.org/10.22146/ijc.21283.
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Formulation and in vitro study of propranolol hydrochloride controlled release from carboxymethyl chitosan-based matrix tablets have been conducted. Formulations with various concentrations of carboxymethyl chitosan 2% (F1), 4% (F2), 6% (F3) were done by wet granulation method. Compatibility test was conducted by XRD and FTIR spectroscopy to determine interaction between propranolol hydrochloride and polymer excipients. Dissolution profiles was obtained through in vitro tests release using simulated gastric fluid (without enzymes, pH 1.2) for the first 2 h and followed by simulated intestinal fluid (phosphate buffer solution without enzyme, pH 7.2) for 2 h remaining. The dissolution profile of each formulation was fitted with five kinetics modeling of drug release (zero order, first order, Higuchi, Peppas-Korsmeyer, and Hixson-Crowell). The compatibility test results showed that formulation caused physical interactions between propranolol hydrochloride and polymer excipient but doesn't make crystallinity nature of propranolol hydrochloride disturbed even after formulation. Dissolution profiles of each formulation showed that controlled release of propranolol hydrochloride from the tablet followed Peppas-Korsmeyer model. It is concluded that carboxymethyl chitosan in appropriate proportions is suitable for formulating propranolol hydrochloride controlled release tablets which exhibit Peppas-Korsmeyer release kinetics.
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Sarwar, Golam, Abhijit Das, Md Golam Kibria, Palash Karmakar, and Mohammad Mafruhi Sattar. "In vitro Quality Analysis of Different Brands of Alprazolam Tablet Available in Bangladesh." Bangladesh Pharmaceutical Journal 16, no. 2 (February 20, 2015): 185–88. http://dx.doi.org/10.3329/bpj.v16i2.22302.
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Alprazolam is a benzodiazepine anxiolytic commonly prescribed as a sleeping aid and for the treatment of anxiety disorders. The current study was undertaken with the aim of analyzing quality of commercially available brands of alprazolam tablets available in Bangladesh. To assess the quality, locally available 0.25 mg alprazolam tablet of seven different manufacturers were selected and certain physico-chemical parameters like weight variation, hardness, friability, disintegration time and dissolution profile etc. were evaluated using in-vitro analytical methods. All the tablet brands met the requirements of British Pharmacopoeia as they showed acceptable weight variation and friability (below 1%). Brands were slightly different in hardness, disintegration time and dissolution profile from each other. The hardness of all the brands was found to be in the range of 1.50±0.18 to 4.21±0.11 kg-ft. In water medium the disintegration time of all brands were found to be 0.57±0.45 to 2.22±0.23 min. Five out of seven brands showed better dissolution profile as they released more than 90% drug in 30 min. The study revealed that most of the marketed alprazolam tablets met the BP standards for physico-chemical properties which are the indicators of drug quality. It can be concluded that drug products should always comply standard quality parameters that are the prerequisites for getting satisfactory clinical effects. DOI: http://dx.doi.org/10.3329/bpj.v16i2.22302 Bangladesh Pharmaceutical Journal 16(2): 185-188, 2013
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Howlader, Md Sariful Islam, Jayanta Kishor Chakrabarty, Khandokar Sadique Faisal, Uttom Kumar, Md Raihan Sarkar, and Mohammad Firuz Khan. "Enhancing dissolution profile of diazepam using hydrophilic polymers by solid dispersion technique." International Current Pharmaceutical Journal 1, no. 12 (November 1, 2012): 423–30. http://dx.doi.org/10.3329/icpj.v1i12.12453.
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The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug by a solid dispersion technique, in order to investigate the effect of these polymers on release mechanism from solid dispersions. Diazepam was used as a model drug to evaluate its release characteristics from different matrices. Solid dispersions were prepared by using polyethylene glycol 6000 (PEG-6000), HPMC, HPC and Poloxamer in different drug-to-carrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solid dispersions were prepared by solvent method. The pure drug and solid dispersions were characterized by in vitro dissolution study. Distilled water was used as dissolution media, 1000 ml of distilled water was used as dissolution medium in each dissolution basket at a temperature of 37°C and a paddle speed of 100 rpm. The very slow dissolution rate was observed for pure Diazepam and the dispersion of the drug in the polymers considerably enhanced the dissolution rate. This can be attributed to improved wettability and dispersibility, as well as decrease of the crystalline and increase of the amorphous fraction of the drug. SEM (Scanning Electron microscope) studies shows that the solid dispersion having a uniform dispersion. Solid dispersions prepared with PEG-6000, Poloxamer showed the highest improvement in wettability and dissolution rate of Diazepam. Solid dispersion containing polymer prepared with solvent method showed significant improvement in the release profile as compared to pure drug, Diazepam.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12453 International Current Pharmaceutical Journal 2012, 1(12): 423-430
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Rahman, Md Ziaur, Sayed Koushik Ahamed, Sujan Banik, and Mohammad Salim Hossain. "Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet." Bangladesh Pharmaceutical Journal 16, no. 2 (February 20, 2015): 177–83. http://dx.doi.org/10.3329/bpj.v16i2.22301.
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The present study was undertaken to develop sustained release (SR) matrix tablets of Losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method along with Kollidon SR and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013
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Verma, Ravinder, and Deepak Kaushik. "Development, Optimization, Characterization and Impact of In vitro Lipolysis on Drug Release of Telmisartan Loaded SMEDDS." Drug Delivery Letters 9, no. 4 (October 31, 2019): 330–40. http://dx.doi.org/10.2174/2210303109666190614120556.
Full textAbstract:
Objective: The objective of the current research is systematic optimization and development of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability profile of Telmisartan utilizing D-optimal mixture design. Methods: Solubility studies in a variety of lipidic ingredients and optimization of formulations were carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing the interaction performance of desired responses (such as % cumulative drug release and globule size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative drug release and globule size performance for determining the dissolution rate and oral bioavailability of drug. Results: The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant (Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant goodness of fit between drug release. Stability studies indicated stability of the optimized SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release. Conclusion: Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully shows the potential usage of SMEDDS for delivery of BCS-II class drugs.
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Pawar, Harshal Ashok, and Pooja Rasiklal Joshi. "Development and Validation of a Discriminating In Vitro Dissolution Method for Oral Formulations Containing Satranidazole." International Journal of Spectroscopy 2014 (April 24, 2014): 1–7. http://dx.doi.org/10.1155/2014/624635.
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The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Satranidazole (BCS Class II drug) is a new nitroimidazole derivative with potent antiamoebic action. There is no official dissolution medium available in the literature. In the present study, parameters such as saturation solubility in different pH medium, dissolution behavior of formulations, influence of sink conditions, stability, and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium. Results of solubility data revealed that solubility of Satranidazole decreases with an increase in pH. Satranidazole showed better sink condition in 0.1 N HCl as compared to other media. The drug and marketed formulations were stable in the dissolution media used. An agitation speed of 75 rpm showed a more discriminating drug release profile than 50 rpm. Using optimized dissolution parameters (paddle at 75 rpm, 900 mL 0.1 N HCl) greater than 80% of the label amount is released over 60 minutes. UV-spectroscopic method used was validated for the specificity, linearity, precision, robustness, and solution stability. The method was successfully applied to granular formulations and also to marketed tablets containing 300 mg Satranidazole.
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Kaur, Manpreet, Amit Mittal, Monica Gulati, Deepika Sharma, and Rajesh Kumar. "Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients." Recent Patents on Drug Delivery & Formulation 14, no. 1 (October 13, 2020): 48–62. http://dx.doi.org/10.2174/1872211314666191224121044.
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Background: Febuxostat is a novel, orally-administered, powerful, non-purine, xanthine oxidase inhibitor used for treating gout and ceaseless tophaceous gout. The drug exhibits low bioavailability (about 49%) which is ascribed to its dissolution rate-limited absorption. Objective: The current work is aimed to provide a novel strategy to improve the dissolution profile and thus, the bioavailability of Febuxostat. Methods: Formulation of Fast Dissolving Tablets (FDT) is anticipated to provide immediate release of the drug, which in turn, will improve its dissolution profile to provide the initial surge in plasma concentration required in an acute gout attack. Incorporation of co-processed excipients in a tablet is known to improve the compressibility and disintegration characteristics of the tablets, which, in turn, result in enhanced in vitro drug release and improved bioavailability. A combination of crospovidone (it rapidly wicks saliva into the tablet to create the volume development and hydrostatic weight important to give quick disintegration) and microcrystalline cellulose (a highly compressible ingredient with good wicking and absorbing capacity) was, therefore, used as co-processed excipients. Results: The tablets were prepared by direct compression technique with the application of a 32 randomized full factorial design. The prepared tablets were able to release more than 80% of the drug within 10 minutes of the start of dissolution testing and were able to show a better drug release profile in comparison to available marketed formulation. Conclusion: So, it can be concluded that the developed fast release formulation was found to exhibit convincing in vitro results and may prove a boon in the treatment of acute gout attack after establishing in vivo potential.
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Peleshok, K. Y. "QUALITY CONTROL MEASUREMENT AND IN VITRO BIOEQUIVALENCE OF VALSARTAN AND ATENOLOL TABLETS MARKETED IN UKRAINE." International Journal of Medicine and Medical Research 6, no. 2 (May 18, 2021): 52–58. http://dx.doi.org/10.11603/ijmmr.2413-6077.2020.2.12013.
Full textAbstract:
Background. The urgent issue of hypertension is determined by its high population incidence, significant burden of the disease, risk of disability and impact on life expectancy. Rational combinations of drugs of different pharmacological groups in case of ineffectiveness of monotherapy to achieve the clinical effect of pharmacotherapy are clearly recommended in the world and national recommendations for diagnosis and treatment of hypertension. Therefore, innovative pharmaceutical development of a combination of antihypertensive drugs and creation of domestic drugs with antihypertensive action is an urgent task of contemporary pharmacy.
Objective. The aim of this study was to perform the quality control measurements and evaluation of dissolution tests for different brands of valsartan and atenolol tablets available in Ukraine.
Methods. The concentrations of valsartan and atenolol in samples (drug content and dissolution study) were determined by the proposed HPLC method.
Results. The results of the tests conducted for evaluation of the tablets were found to be in acceptable limits for all the selected brands. The correlation coefficient (R2) was 0.9991 and the regression equation was y=61.39x+0.3117. It has been established that the equivalence of dissolution profiles for all recommended dissolution media is observed (рН 1.2, 4.5, and 6.8) for the studied drugs. In all three dissolution media, the release rates of valsartan and atenolol of all dosage forms are more than 85% in 15 min. The dissolution profile of all the selected brands was within the standard limits and was acceptable.
Conclusions. Analytical method development is an integral part of the quality control measurements and evaluation of dissolution tests. Our previously developed HPLC method is essential for quality control of a large number of samples in short time intervals. Therefore, the method developed by our group is suitable for a routine quality control analysis of any pharmaceutical preparation containing two tested drugs with the suggested chromatographic method advantages for checking quality during dissolution studies of their dosage forms.
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Pudjiastuti, Pratiwi, Siti Wafiroh, Esti Hendradi, Handoko Darmokoesoemo, Muji Harsini, M. Al Rizqi Dharma Fauzi, Lutfun Nahar, and Satyajit D. Sarker. "Disintegration, In vitro Dissolution, and Drug Release Kinetics Profiles of k-Carrageenan-based Nutraceutical Hard-shell Capsules Containing Salicylamide." Open Chemistry 18, no. 1 (April 7, 2020): 226–31. http://dx.doi.org/10.1515/chem-2020-0028.
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AbstractThe release of drugs from solid drug delivery materials has been studied intently in recent years. Quantitative analyses achieved from in vitro dissolution becomes easier if a zero-order mathematical model is used. Non-gelatin nutraceutical hard-shell capsules of zero size (approximately 0.7-0.8 cm) were produced from carrageenan-based natural polymers, namely carrageenan-alginate (CA) and carrageenan-starch (CS). Disintegration, dissolution and zero-order drug release kinetics of hard-shell capsules containing 100 mg of salicylamide were studied. The disintegration time of CA and CS were observed to be less than 30 min for both CA and CS. In vitro dissolution profile showed that the percentage dissolution of CA capsules was better at pH 4.5, while that of CS was poor at pH 1.2, 4.5 and 6.8. Determination of drug release kinetics profiles of carrageenan-based hardshell capsules utilized the Noyes-Whitney and Peppas-Sahlin modification rules for zero-order. The drug release from carrageenan-based capsules followed zero-order kinetics, especially at pH 6.8, and was compared to the Higuchi model. Salicylamide in CA hard-shell capsules at a pH 6.8 had a release rate constant (kH) of 2.91 %(ppm/ ppm) min-1/2, while the release rate constant of CS was 0.36 %(ppm/ppm) min-1.
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Hossain, ASM Monjur Al, Konika Rani Dutta, and Md Lokman Hossain. "In Vitro Evaluation of Different Approaches and Dissolution Enhancement Technique of Poorly Water-Soluble Drug Ibuprofen." Dhaka University Journal of Science 64, no. 2 (July 31, 2016): 169–75. http://dx.doi.org/10.3329/dujs.v64i2.54497.
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Ibuprofen Solid Dispersion (SD) was prepared by simple Physical Mixing (PM) and Kneading Method (KM). In these two cases, four polymers named poloxamer 407, sodium carboxy methyl cellulose, croscarmellose sodium and pregelatinized starch were used to enhance the dissolution profile of Ibuprofen. In both methods, the ratio of drug and carrier were 1:1, 1:2, 1:3 of which the ratio of 1:3 in KM gave comparatively better result than PM method. In vitro dissolution study was performed in distilled water in 50 rpm and at 37 ± 0.5°C. In case of pure Ibuprofen, dissolution rate was only 26% after 60 minutes (mins) of dissolution. While in KM, Ibuprofen pregelatinized starch formulation at 1:3 ratio showed better dissolution rate. After 60 mins, dissolution rate of Ibuprofen was 72%. The SD formulations of Ibuprofen-pregelatinized starch and Ibuprofen-Na-CMC of physical mixing and kneading techniques (1:3 ratio) were characterized by Fourier Transform Infrared Spectroscopy (FTIR).
Dhaka Univ. J. Sci. 64(2): 169-175, 2016 (July)
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Patel, Madhubhai M., and Rahulkumar J. Patel. "Linagliptin loaded Solid-SMEEDS for enhanced solubility and dissolution: Formulation development and optimization by D-optimal design." Journal of Drug Delivery and Therapeutics 9, no. 2 (March 15, 2019): 47–56. http://dx.doi.org/10.22270/jddt.v9i2.2465.
Full textAbstract:
The aim of the present investigation was to formulate and evaluate solid self-micro emulsifying drug-delivery systems (S-SMEDDS) to improve solubility and dissolution profile of Linagliptin. Solubility of Linagliptin in different oils, surfactants and co-surfactants was assessed and optimizations of pseudo-ternary plots were also carried out for preparation of liquid SMEDDS. D-optimal design mixture was used in the optimization of Linagliptin loaded liquid SMEEDS. The optimized SMEEDS were characterized for globule size, zeta potential, dilution stability, transmittance, pH and in-vitro release profile. The morphology of the Linagliptin SMEEDS was observed by Transmission Electron Microscopy (TEM). Among the different silicates, Nusillin US2 was used as the solid carrier/absorbent to formulate S-SMEEDS of Linagliptin. Improved in-vitro dissolution profile of optimized formulation was observed, resulting in multifold improvement in the absorption profile of Linagliptin as compared with pure drug. In a nutshell, this optimized S-SMEDD formulation holds great promise for enhancement of its physiochemical and biological attributes.
Keywords: Linagliptin, Solid Self-micro Emulsifying Drug Delivery Systems, D-optimal design, Zeta-potential, Transmission Electron Microscopy
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Jagdale, Swati Changdeo, Vinayak Narhari Jadhav, Aniruddha Rajaram Chabukswar, and Bhanudas Shankar Kuchekar. "Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes." Brazilian Journal of Pharmaceutical Sciences 48, no. 1 (March 2012): 131–45. http://dx.doi.org/10.1590/s1984-82502012000100015.
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The main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. Binary complex was prepared by different methods and was further characterized using XRD, DSC and FT-IR. A saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. The optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants Doshion P544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. Tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. Tablets showed an enhanced dissolution rate compared to pure nifedipine.
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Hazemba, Kubota Mwaka, Jivan Jyoti, Sheetu Wadhwa, Sananda Som, Souvik Mohanta, Ankit Kumar Yadav, Bimlesh Kumar, et al. "INFLUENCE OF FORMULATION PARAMETERS ON DISSOLUTION RATE ENHANCEMENT OF ACYCLOVIR USING LIQUISOLID FORMULATION." Asian Journal of Pharmaceutical and Clinical Research 11, no. 14 (July 27, 2018): 36. http://dx.doi.org/10.22159/ajpcr.2018.v11s2.28537.
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Objective: The objective of this research work is to explore the use of liquisolid technique in enhancement of acyclovir dissolution rate. This current study was planned to assess the impact of different formulation variables, such as non-volatile liquid type and concentrations of acyclovir on its dissolution rates profile. Method: Acyclovir liquisolid tablets were prepared with Tween 60 (liquid vehicle), Microcrystalline cellulose PH 102 (acted as a carrier to turn liquid medication into free-flowing powder) and Syloid XDP (coating material). In vitro, drug dissolution rate of liquisolid formulations of acyclovir was performed and compared with pure acyclovir drug using USP dissolution apparatus (Type II) for 60 min at a paddle speed of 50 rpm and filled with 900 mL of distilled water. Results: The dissolution study showed that 94.1% of the drug was released in 60 min of ratio 10 while only 66% of the pure drug acyclovir was released in 60 min. Hence, present work concluded that the acyclovir dissolution rate profile has been improved with the formation of liquisolid formulations. Conclusion: From the present study, it may be ratified that the drug dissolution rate of acyclovir has been improved with the utilization of liquisolid formulations approach.
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Kar, Ayan Kumar, and Banhishikha Kar. "In-Vitro Comparative Dissolution Study of Commercially Available Paracetamol Tablet." Journal of Drug Delivery and Therapeutics 10, no. 1 (January 15, 2020): 18–23. http://dx.doi.org/10.22270/jddt.v10i1.3817.
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Quality is the most important issue in the pharmaceutical field due to the presence of a drug which is considered as safe and therapeutically active agent. In-vitro evaluation ensures their quality, bioavailability as well as optimum therapeutic activity. Paracetamol (acetaminophen) which are the active metabolites of phenacetin is commonly used for the relief of headaches and pains, and is a major ingredient in numerous cold and flu remedies. Paracetamols are available in different brands in Indian market. The main objective of the present study was to conduct the comparative in-vitro dissolution studies of various brands collected from the local market to determine whether all the formulations used were equivalent or significantly different. The calibration curve was constructed covering the concentration range of 1 to 10 mcg/ml at 268 nm by UV spectrophotometer (UV 2203 Double beam spectrophotometer, Shimadzu). Five different brands of Paracetamol of 500 mg conventional tablets from different manufacturers were selected in the study and dissolution testing in Phosphate buffer at pH 7.4 was conducted from each brands for 90 mins by using dissolution testing apparatus USP type-II. The dissolution rate was subjected to various mathematical models like zero order, first order, Higuchi and Hixson-Crowell equations to elucidate the kinetic behavior of drug release from the test samples. Different release kinetics model of all the selected brands was assuring the quality standard of manufacturing.
Keywords: Paracetamol, Marketed Tablet, In-Vitro dissolution study, Release profile.
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Kabir, Abul Kalam Lutful, Shimul Halder, Madhabi Lata Shuma, and Abu Shara Shamsur Rouf. "Formulation Development and in vitro Evaluation of Drug Release Kinetics from Sustained Release Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose." Dhaka University Journal of Pharmaceutical Sciences 11, no. 1 (November 4, 2012): 37–43. http://dx.doi.org/10.3329/dujps.v11i1.12485.
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The objective of the present study was to develop a once-daily sustained release matrix tablet of Aceclofenac using hydroxypropyl methyl cellulose (Methocel K 100M CR) as release controlling factor and to evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct compression method. The powder blends were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus in phosphate buffer (pH 7.4). The powder blends showed satisfactory flow properties, compressibility index and drug content etc. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-3 (40% Methocel K100M CR of total weight of tablet) could extend the drug release up to 24 hours and the total release pattern was very close to the theoretical release profile. By comparing the dissolution profiles with the originator brand of Arrestin SR, the formulation F-3 exhibited drug release profile like originator brand. From this study, a decrease in release kinetics of the drug was observed by increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion mechanism in all cases. The drug release from the formulation (F-3) was satisfactory after 3 months storage in 400C and 75% RH. Besides, this study explored both of the optimum concentration and effect of polymer(s) on Aceclofenac release pattern from the tablet matrix for 24 hour period. The matrix tablet of Aceclofenac using HPMC with molecular weight of K100M controlled the drug release effectively for 24 hours; hence the formulation can be considered as a once daily sustained release tablet of Aceclofenac in order to improve patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12485 Dhaka Univ. J. Pharm. Sci. 11(1): 37-43, 2012 (June)
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Ivana Mitrevska, Hristijan Mickoski, Katerina Brezovska, and Aneta Dimitrovska. "Evaluation of in vitro dissolution similarity of bisoprolol film-coated tablets based on Weibull modelling using MATLABTM simulation software." World Journal of Advanced Research and Reviews 10, no. 1 (April 30, 2021): 056–73. http://dx.doi.org/10.30574/wjarr.2021.10.1.0143.
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The aim of this study was to compare the in vitro dissolution behaviour of reference (R) and generic-test (T) medicinal products with non-linear effects model. Mathematical function Weibull, was employed as basis for the non-linear effects model, coupled with MATLABTM simulation software to describe the release profile of the active substance. Medicinal products selected for the presented study include immediate-release tablets Concor 10 mg and Bisoprolol 10 mg, which belongs to BCS class 1 of biopharmaceutics classification system. The result from the study indicated that Weibull distribution function coupled with computer-based program is more useful for comparison of the dissolution profiles. This combined approach provides robust and informative results, with accurate estimation on the in vitro performance for the medicinal products and it’s the most suitable tool for prediction of in vivo behaviour of the medicinal product. In summary, we have employed Simulink graphical programming to design our system in a simulation environment.
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Sehgal, Nikita, Vishal Gupta N, Gowda Dv, and Sivadasu P. "FABRICATION AND EVALUATION OF SOLID DISPERSION CONTAINING GLIBENCLAMIDE." Asian Journal of Pharmaceutical and Clinical Research 11, no. 8 (August 7, 2018): 158. http://dx.doi.org/10.22159/ajpcr.2018.v11i8.26236.
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Objective: The aim of the present study was to increase the dissolution rate of glibenclamide (GLIB) by molecular dispersion of drug in the polymeric matrix of Pluronic F-127.Methods: GLIB-loaded solid dispersions were formulated by fusion method. The formulated solid dispersions were characterized for scanning electron microscopy (SEM), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and evaluated for percentage yield, drug content, solubility, and in vitro dissolution profile, and stability studies were conducted as per International Conference on Harmonisation guidelines Q1A in stability chamber, both at intermediate and accelerated conditions.Results: Both XRD and DSC studies suggested that crystalline GLIB was converted to amorphous form after loading into carrier. SEM studies revealed that the prepared solid dispersions were in the form of irregular particles with the absence of crystalline material. Due to this conversion of crystalline to amorphous state, formulated solid dispersions had shown improved dissolution rate profile of GLIB and stability studies suggested that formulated solid dispersions showed no significant changes in appearance and also in drug content.Conclusion: Thus, from the obtained results, it can be concluded that dissolution profile of GLIB can be improved by formulating as solid dispersion.
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Chella, Naveen, Nataraj Narra, and Tadikonda Rama Rao. "Preparation and Characterization of Liquisolid Compacts for Improved Dissolution of Telmisartan." Journal of Drug Delivery 2014 (October 12, 2014): 1–10. http://dx.doi.org/10.1155/2014/692793.
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The objective of the present work was to obtain pH independent and improved dissolution profile for a poorly soluble drug, telmisartan using liquisolid compacts. Liquisolid compacts were prepared using Transcutol HP as vehicle, Avicel PH102 as carrier, and Aerosil 200 as a coating material. The formulations were evaluated for drug excipient interactions, change in crystallinity of drug, flow properties, and general quality control tests of tablets using Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), angle of repose, and various pharmacopoeial tests. In vitro dissolution studies were performed at three pH conditions (1.2, 4.5 and 7.4). Stability studies were performed at 40°C and 75% RH for three months. The formulation was found to comply with Indian pharmacopoeial limits for tablets. FTIR studies confirmed no interaction between drug and excipients. XRD and DSC studies indicate change/reduction in crystallinity of drug. Dissolution media were selected based on the solubility studies. The optimized formulation showed pH independent release profile with significant improvement P<0.005 in dissolution compared to plain drug and conventional marketed formulation. No significant difference was seen in the tablet properties, and drug release profile after storage for 3 months.
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Menegola, Júlia, Martin Steppe, and Elfrides E. S. Schapoval. "Dissolution test for citalopram in tablets and comparison of in vitro dissolution profiles." European Journal of Pharmaceutics and Biopharmaceutics 67, no. 2 (September 2007): 524–30. http://dx.doi.org/10.1016/j.ejpb.2007.02.009.
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Galata, Farkas, Könyves, Mészáros, Szabó, Csontos, Pálos, Marosi, Nagy, and Nagy. "Fast, Spectroscopy-Based Prediction of In Vitro Dissolution Profile of Extended Release Tablets Using Artificial Neural Networks." Pharmaceutics 11, no. 8 (August 9, 2019): 400. http://dx.doi.org/10.3390/pharmaceutics11080400.
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The pharmaceutical industry has never seen such a vast development in process analytical methods as in the last decade. The application of near-infrared (NIR) and Raman spectroscopy in monitoring production lines has also become widespread. This work aims to utilize the large amount of information collected by these methods by building an artificial neural network (ANN) model that can predict the dissolution profile of the scanned tablets. An extended release formulation containing drotaverine (DR) as a model drug was developed and tablets were produced with 37 different settings, with the variables being the DR content, the hydroxypropyl methylcellulose (HPMC) content and compression force. NIR and Raman spectra of the tablets were recorded in both the transmission and reflection method. The spectra were used to build a partial least squares prediction model for the DR and HPMC content. The ANN model used these predicted values, along with the measured compression force, as input data. It was found that models based on both NIR and Raman spectra were capable of predicting the dissolution profile of the test tablets within the acceptance limit of the f2 difference factor. The performance of these ANN models was compared to PLS models using the same data as input, and the prediction of the ANN models was found to be more accurate. The proposed method accomplishes the prediction of the dissolution profile of extended release tablets using either NIR or Raman spectra.
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Kandel, Ramesh, Tushar Saha, Zia Uddin Masum, and Jakir Ahmed Chowdhury. "Formulation and In vitro Release Behavior of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Containing Poorly Soluble Fenofibrate." Bangladesh Pharmaceutical Journal 23, no. 1 (February 3, 2020): 10–16. http://dx.doi.org/10.3329/bpj.v23i1.45314.
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Fenofibrate, a water insoluble drug was used to prepare matrix tablet with four different viscosity grades of Hydroxypropyl Methylcellulose (HPMC) which were Methocel K4M CR, Methocel K15M CR, Methocel K100M CR and Methocel K100LV CR. The concentration of those excipients was 5, 10, 20, and 40% (w/w), respectively. The content of drug in a fixed quantity of powder in every formulation was ranged between 96.47 to 104.78 %. The dissolution study was done by using USP dissolution apparatus II. The kinetics of release was analyzed by using zero-order, first order, Korsmeyer-Peppas, Higuchi and Hixon-crowell equations to explain the drug release mechanism from the matrix tablets. In-vitro dissolution profile of matrix tablets were dependent upon the HPMC concentration and dissolution was rapid for tablets containing lower polymer proportion i.e. 5,10, and 20% Percentage (w/w) HPMC than those containing 40% (w/w) HPMC.
Bangladesh Pharmaceutical Journal 23(1): 10-16, 2020
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Vujovic, Maja, Milan Jokanovic, and Goran Nikolic. "In vitro dissolution profile study of mucolytic drug ambroxol hydrochloride from solid oral dosage form by UHPLC-MS/MS." Chemical Industry 71, no. 1 (2017): 75–83. http://dx.doi.org/10.2298/hemind160315020v.
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In this paper a simplified dissolution test was performed for the release of ambroxol from tablets according to the European Pharmacopoeia. In vitro, three different dissolution media; 0.1 M HCl pH 1.2, acetate buffer (ABS) pH 4.5 and phosphate buffer (PBS) pH 6.8 were used for the simulation of the gastrointestinal conditions at temperature of 37.0?0.5?C. The drug release was evaluated by a new ultra - high performance liquid chromatography (UHPLC) - tandem mass spectrometry (MS/MS) method. The method was validated to meet requirements as per ICH guidelines which include linearity, specificity, precision, accuracy and robustness. The corresponding dissolution profiles showed more than 80% drug release within 30 minutes without significant differences. Further, the developed and validated UHPLC-MS/MS method could find a useful application in the process of production, quality control and bioavailability/bioequivalence studies of new pharmaceutical formulations of drugs in order to achieve a safe therapeutic efficacy.
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Mumtaz, Hina, Muhammad Asim Farooq, Zainab Batool, Anam Ahsan, and Ashikujaman Syed. "Significance of In-Vitro and In-Vivo Correlation in Drug Delivery System." Research in Pharmacy and Health Sciences 4, no. 4 (December 15, 2018): 523–31. http://dx.doi.org/10.32463/rphs.2018.v04i04.23.
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The main purpose of development pharmaceutical dosage form is to find out the in vivo and in vitro behavior of dosage form. This challenge is overcome by implementation of in-vivo and in-vitro correlation. Application of this technique is economical and time saving in dosage form development. It shortens the period of development dosage form as well as improves product quality. IVIVC reduce the experimental study on human because IVIVC involves the in vivo relevant media utilization in vitro specifications. The key goal of IVIVC is to serve as alternate for in vivo bioavailability studies and serve as justification for bio waivers. IVIVC follows the specifications and relevant quality control parameters that lead to improvement in pharmaceutical dosage form development in short period of time. Recently in-vivo in-vitro correlation (IVIVC) has found application to predict the pharmacokinetic behaviour of pharmaceutical preparations. It has emerged as a reliable tool to find the mode of absorption of several dosage forms. It is used to correlate the in-vitro dissolution with in vivo pharmacokinetic profile. IVIVC made use to predict the bioavailability of the drug of particular dosage form. IVIVC is satisfactory for the therapeutic release profile specifications of the formulation. IVIVC model has capability to predict plasma drug concentration from in vitro dissolution media.
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Verma, Rajan, Shrikant Hodge, Chandrashekhar Gargote, Prakash Modi, Naresh Upreti, Lokesh Yadav, and Raviraj Pillai. "Assessment of physical and dissolution characteristics of various itraconazole capsule formulations: a comparative analysis." International Journal of Research in Dermatology 5, no. 4 (October 21, 2019): 765. http://dx.doi.org/10.18203/issn.2455-4529.intjresdermatol20194665.
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<p class="abstract"><strong>Background:</strong> This <em>in vitro</em> study compared physical parameters and the dissolution profile of innovator itraconazole capsule formulation, i-Tyza, and 5 other generic capsule formulations available in the Indian market.</p><p class="abstract"><strong>Methods:</strong> The number of pellets and size distribution were determined using naked eye examination and sieving method, respectively. Dissolution profile of formulations was done at 15, 30, 45, and 60 minutes, using a United States Pharmacopeia type II Paddle apparatus in simulated gastric fluid (SGF, pH 1.2) without enzymes, acetate buffer (pH 4.5) with 0.5% sodium lauryl sulfate (SLS), and phosphate buffer (pH 6.8) with 0.5% SLS.<strong></strong></p><p class="abstract"><strong>Results:</strong> All formulations had capsule size 0. Capsule fill weight (~335 to ~510 mg) and total pellet number (127 to 810) varied across formulation, with the innovator brand having the highest number of pellets. Innovator product and i-Tyza had similar fill weight (~460 mg). Pellet size distribution of the innovator product, brand 2, brand 3, and i-Tyza was relatively narrow. In SGF, except brand 1 (84% dissolved) and brand 5 (80% dissolved), all the formulations had near-complete (>85% drug dissolved) or complete dissolution (>90% drug dissolved) at 60 minutes. In acetate buffer, pH 4.5 with 0.5% SLS and phosphate buffer, pH 6.8 with 0.5% SLS, only the innovator product and i-Tyza demonstrated near-complete to complete dissolution at 60 minutes (96% and 90% dissolved).</p><p class="abstract"><strong>Conclusions:</strong> Across all the itraconazole generic formulations evaluated, i-Tyza had comparable physical characteristics and dissolution profile to the innovator product. The <em>in vitro</em> dissolution profile of i-Tyza may indicate adequate <em>in vivo</em> performance.</p>
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Sharafi, Mastaneh, Tyler White, Kelli Fowler, Kevin Ewell, Noe Galvan, and Nima Alamdari. "In Vitro Dissolution Evidence for Sustained and Prolonged Release of Vitamin C in a Phosphatidyl Choline-Enriched Lipid Encapsulation." Current Developments in Nutrition 5, Supplement_2 (June 2021): 1328. http://dx.doi.org/10.1093/cdn/nzab059_029.
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Abstract Objectives In vitro dissolution tests are valuable first-step tools in the development of bioavailable delivery systems, making it possible to assess the performance of novel technologies in releasing active ingredients through the amount dissolved in a dissolution medium. The objective of this study was to evaluate whether phosphatidyl choline-enriched lipid encapsulation releases the majority of vitamin C as ascorbic acid past the stomach in a standard in vitro dissolution procedure and to assess the release profile. Methods A novel phosphatidyl choline-enriched lipid encapsulation that is solid at room temperature was tested for dissolution in a standard dissolution apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. One serving (included 1000 mg ascorbic acid) was placed into vessels containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.8) for an additional 360 minutes. Aliquots were tested for ascorbic acid concentration at 8 time points by titration. The data was compared with 1000 mg of regular ascorbic acid in a capsule format. Results The phosphatidyl choline-enriched lipid encapsulation released 36% of the vitamin C at 2 hours in the acid phase and released 56% at 3 hours, 67% at 4 hours, 85% at 6 hours and 98% at 8 hours in the intestinal phase. Regular vitamin C filled capsules released 100% of the vitamin C at 30 minutes. Conclusions The dissolution results indicated that phosphatidyl choline-enriched lipid encapsulation can pass the stomach and release the majority of vitamin C in the small intestine. The encapsulation demonstrated a sustained and prolonged release of vitamin C over an 8 hour period. The release profile observed in this in vitro study suggests phosphatidyl choline-enriched lipid encapsulation may improve nutrient absorption and bioavailability which requires further testing including human clinical trials. Funding Sources This study was supported by Lonza (Greenwood, SC) and Ritual (Natals Inc, Los Angeles, CA).
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Mehta, L. Sonali, D. V. Gowda, N. Vishal Gupta, and Manohar M. "FORMULATION AND DEVELOPMENT OF LENALIDOMIDE LOADED DELAYED RELEASE MINI TABLETS IN CAPSULES." International Journal of Applied Pharmaceutics 10, no. 5 (September 8, 2018): 239. http://dx.doi.org/10.22159/ijap.2018v10i5.26658.
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Objective: Formulation and development of delayed release mini tablets in the capsule of drug lenalidomidein terms of dissolution and stability was the objective of the present work.Methods: Tablets of less than or equal to 3 millimetres diameter are Mini-tablets, which were filled into a capsule. Direct compression method using multi-tip punch was used for compression and coated with eudragit L100 as a seal coating material and with eudragit L30D55 as an enteric coating material was done. Different formulations were prepared and subjected for evaluation like weight variation, hardness, friability, disintegration, and dissolution studies. The optimized formulation was compared to marketed product based on drug released profile and also subjected for stability studies.Results: The results revealed that the in vitro drug release of prepared formulations, F1, F2, F3, and F4 was subjected for acid resistance test for 2 h in 0.1N HCl and has a comparable dissolution profile in phosphate buffer of 6.8 pH. FormulationF4 was subjected for stability studies and no significant difference was observed in 3 mo 40 °C/75% RH accelerated stability condition.Conclusion: The dissolution profile of formulation F4 was found better than that of market product. Based on evaluation results, the study concluded that F4formulationwas considered as an optimized formulation.