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1
Schlich, Michele, Francesco Lai, Anna Maria Fadda, Chiara Sinico, and Elena Pini. "Drug-Excipients Compatibility Studies in Proniosomal Formulation: A Case Study with Resveratrol." Journal of Nanoscience and Nanotechnology 21, no. 5 (2021): 2917–21. http://dx.doi.org/10.1166/jnn.2021.19056.
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Proniosomal drug delivery system is one of the advancements in nanotechnology. Similarly to traditional dosage forms, chemical and physical compatibility of proniosomes components with the active ingredient(s) is a key step in the preformulation process of such systems. In this work, the compatibility of resveratrol with selected excipients in the development of proniosomal formulation was investigated by thermal and spectroscopic techniques. To evaluate the drug-excipient compatibility, different techniques such as differential scanning calorimetric study, attenuated total reflectance Fourier transform infrared spectroscopy study and powder X-ray diffraction were adopted. The results showed that the excipients used in the formulation were compatible with resveratrol.
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Tita, Ioana Cristina, Lavinia Lupa, Bogdan Tita, Roxana Liana Stan, and Laura Vicas. "Compatibility Studies of Valsartan with Different Pharmaceutical Excipients." Revista de Chimie 70, no. 7 (2019): 2590–600. http://dx.doi.org/10.37358/rc.19.7.7386.
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Compatibility studies between active drugs and excipients are substantial in the pharmaceutical technology. Thermal analysis has been extensively used to obtain information about drug-excipient interactions and to perform pre-formulation studies of pharmaceutical dosage forms. The objective of the present study was to evaluate the compatibility of the valsartan (VALS) with pharmaceutical excipients of common use including diluents, binders, disintegrants, lubricants and solubilising agents. Thermogravimetry (TG), derivative thermogravimetry (DTG), but especially differential scanning calorimetry (DSC) were used for a first screening to find small variations in peak temperature and/or their associated enthalpy for six drug/excipient mixtures (starch, cross caramelose sodique, microcrystalline cellulose 102, povidone K30, lactose monohydrate and magnesium stearate), which indicate some degree of interaction. Additional methods using Fourier transformed infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRPD) confirmed the incompatibility of VALS with starch, povidone K30, lactose monohydrate and magnesium stearate. Those excipients should be avoided in the development of solid dosage forms.
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Gao, Rui, Yi Jin, Qing-Yi Yang, Bai-Wang Sun, and Jun Lin. "Study of stability and drug-excipient compatibility of estradiol and pharmaceutical excipients." Journal of Thermal Analysis and Calorimetry 120, no. 1 (2014): 839–45. http://dx.doi.org/10.1007/s10973-014-4234-0.
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de Carvalho, Murilo Ferreira, Luane Ferreira Garcia, Isaac Yves Lopes de Macedo, et al. "Electroanalysis Applied to Compatibility and Stability Assays of Drugs: Carvedilol Study Case." Pharmaceuticals 13, no. 4 (2020): 70. http://dx.doi.org/10.3390/ph13040070.
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Carvedilol (CRV) is a non-selective blocker of α and β adrenergic receptors, which has been extensively used for the treatment of hypertension and congestive heart failure. Owing to its poor biopharmaceutical properties, CRV has been incorporated into different types of drug delivery systems and this necessitates the importance of investigating their compatibility and stability. In this sense, we have investigated the applicability of several electroanalytical tools to assess CRV compatibility with lipid excipients. Voltammetric and electrochemical impedance spectroscopy techniques were used to evaluate the redox behavior of CRV and lipid excipients. Results showed that Plurol® isostearic, liquid excipient, and stearic acid presented the greatest anode peak potential variation, and these were considered suitable excipients for CRV formulation. CRV showed the highest stability at room temperature and at 50 °C when mixed with stearic acid (7% w/w). The results also provided evidence that electrochemical methods might be feasible to complement standard stability/compatibility studies related to redox reactions.
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Pani, Nihar, Lila Nath, and Sujata Acharya. "Compatibility studies of nateglinide with excipients in immediate release tablets." Acta Pharmaceutica 61, no. 2 (2011): 237–47. http://dx.doi.org/10.2478/v10007-011-0016-4.
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Compatibility studies of nateglinide with excipients in immediate release tabletsExperiments were done to assess the compatibility of nateglinide with selected excipients in the development of immediate release tablets of nateglinide by thermal and isothermal stress testing (IST) techniques. To evaluate the drug-excipient compatibility, different techniques such as differential scanning calorimetric (DSC) study, infra-red (IR) spectrophotometric study and isothermal stress testing were adopted. The results of DSC study showed that magnesium stearate exhibited some interaction with nateglinide. However, the results of IR, and IST studies showed that all the excipients used in the formula were compatible with nateglinide. Optimized formulations developed using the compatible excipients were found to be stable over 3 months of accelerated stability studies (40 ± 2°C and 75 ± 5% RH). Overall, compatibility of excipients with nateglinide was successfully evaluated using a combination of thermal and IST methods and the formulations developed using the compatible excipients were found to be stable.
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Gurav, Sachin B., and Neela M. Bhatia. "Assessment of Structural Compatibility of Saxagliptin in Physical Mixtures with some excipient by Using HPLC." Current Pharmaceutical Analysis 16, no. 8 (2020): 1074–82. http://dx.doi.org/10.2174/1573412915666190617153004.
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Introduction: Saxagliptin hydrochloride is an oral hypoglycemic agent used for the treatment of type 2 diabetes mellitus. Saxagliptin is unstable because it undergoes an intra-molecular cyclisation reaction to form a cyclicamidine in both solution and solid states. In pharmaceutical development of saxagliptin it is important to select the excipients which are compatible and help to minimize the formation of cyclicamidine. In excipient compatibility study for saxagliptin it is essential to identify the formation of cyclicamidine and other related substances. Materials and Methods: In the current work, the method for quantification of saxagliptin, cyclicamidine and its related substances by high performance liquid chromatographic was developed and validated. This method was used as screening technique for assessing the compatibility of saxagliptin with some pharmaceutical excipients. These were evaluated by analyzing the pure saxagliptin and saxagliptin- excipient in physical mixture, which were stored under different conditions at 40°C/75% Relative Humidity (RH) for one month. The method was successfully validated as per ICH guidelines. Results and Conclusion: The results of compatibility study demonstrate the suitability of saxagliptin with Methocel, Polyethylene Glycol (PEG), Opadry Red, Opadry pink, Opadry white, and Opadry Pink.
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Chaves, Luíse L., Larissa A. Rolim, Maria L. C. M. Gonçalves, et al. "Study of stability and drug-excipient compatibility of diethylcarbamazine citrate." Journal of Thermal Analysis and Calorimetry 111, no. 3 (2012): 2179–86. http://dx.doi.org/10.1007/s10973-012-2775-7.
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Balestrieri, Fabrizio, Andrea D. Magrì, Antonio L. Magrì, Domenico Marini, and Amalia Sacchini. "Application of differential scanning calorimetry to the study of drug-excipient compatibility." Thermochimica Acta 285, no. 2 (1996): 337–45. http://dx.doi.org/10.1016/0040-6031(96)02904-8.
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Lavor, Edilene Pereira, Marco Vinícius M. Navarro, Fátima D. Freire, et al. "Application of thermal analysis to the study of antituberculosis drugs–excipient compatibility." Journal of Thermal Analysis and Calorimetry 115, no. 3 (2013): 2303–9. http://dx.doi.org/10.1007/s10973-013-3050-2.
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Sharma, Shyam Bihari, Suman Jain, and K. Ganesan. "Preformulation Studies of Pralidoxime Chloride for Formulation Development of Microspheres." Journal of Drug Delivery and Therapeutics 9, no. 4-s (2019): 338–42. http://dx.doi.org/10.22270/jddt.v9i4-s.3336.
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Microspheres are one of the novel drug delivery system which possess several applications and are made up of assorted polymers. Microspheres can be defined as solid, approximately spherical particles ranging in size from 1 to 1000 μm range in diameter having a core of drug and entirely outer layers of polymers as coating material. They are made up of polymeric, waxy or other protective materials i.e. biodegradable synthetic polymer and modified natural products such as starches, gums, proteins, fats and waxes. Preformulation is a group of studies that focus on the physicochemical properties of a new drug candidate that could affect the drug performance and the development of a dosage form. This couldprovide important information for formulation design or support the need for molecular modification. Every drug has intrinsic chemical and physical properties which has been consider before development of pharmaceutical formulation. This property provides the framework for drugs combination with pharmaceutical ingredients in the fabrication of dosage form. Objective of preformulation study is to develop the elegant, stable, effective and safe dosage form by establishing kinetic rate profile, compatibility with the other ingredients and establish Physico-chemical parameter of new drug substances. The purpose of the present study was to systematically investigate some of the important physicochemical properties of pralidoxime chloride for preparation of microspheres. The physicochemical properties such as solubility, pKa, dissolution, melting point, assay development, excipient compatibility etc. of pralidoxime chloride was carried out. Before selection of excipients, the Preformulation study of drug pralidoxime is completed for successful formulation of microspheres. The result of Preformulation studies shows good flow properties, excipient compatibility, solubility efficiency and melting point. From this study we concluded that pralidoximewith HPMC and EC can be used to formulate pralidoxime microspheres for modified release.
 Keywords: Microspheres, Preformulation, Pralidoxime chloride, Physico-chemical parameter.
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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 (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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Pires, Felipe Q., Tamara Angelo, Joyce K. R. Silva, et al. "Use of mixture design in drug-excipient compatibility determinations: Thymol nanoparticles case study." Journal of Pharmaceutical and Biomedical Analysis 137 (April 2017): 196–203. http://dx.doi.org/10.1016/j.jpba.2017.01.037.
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Vlachou, Marilena, Natassa Pippa, Angeliki Siamidi, and Aimilia Kyrili. "Thermal analysis studies on the compatibility of furosemide with solid state and liquid crystalline excipients." Chemical Industry 74, no. 1 (2020): 15–23. http://dx.doi.org/10.2298/hemind190910002v.
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In the context of the present study, the thermal behavior of furosemide and the solid state excipients, sodium alginate, poly(ethylene oxide), poly(vinylpyrrolidone), lactose mono-hydrate and magnesium stearate, using Differential Scanning Calorimetry (DSC), was probed. It was found that the thermal behavior of these solid-state pharmaceutical excipients and furosemide correlates nicely with the literature relevant data. Regarding the furosemide-excipients mixtures, the DSC scans appear as a compilation of the thermal curves of each excipient. This suggests that the formulations containing these mixtures, may retain their stability over time. This information, which arises from the cooperativity of materials, their thermal stability and behavioris very helpful for the research and development of safe and effective pharmaceutical formulations. DSC experiments were also carried out with chimeric bilayers (called ?liposomes?), composed of hydrogenated soy phosphatidylcholine (HSPC) and poly(n-butylacrylate)-b-poly(acrylic acid) block copolymer with 70 % content of poly(acrylic acid (PnBA-b-PAA 30/70) with the addition of furosemide at the molar ratio of 9:0.1:1.0 in the system HSPC:PnBA-b-PAA 30/70:furosemide. Chimeric liposomal systems were characterized as ?fluid-like? by their DSC curves, which may be potentially translated as an easy way for release of furosemide from the advanced delivery system.
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Li, Yu, Xiangwen Kong, and Fan Hu. "Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets." Current Pharmaceutical Analysis 16, no. 7 (2020): 950–59. http://dx.doi.org/10.2174/1573412915666190328234326.
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Background: Clarithromycin is widely used for infections of helicobacter pylori. Clarithromycin belongs to polymorphic drug. Crystalline state changes of clarithromycin in sustained release tablets were found. Objective: The aim of this study was to find the influential factor of the crystal transition of clarithromycin in preparation process of sustained-release tablets and to investigate the possible interactions between the clarithromycin and pharmaceutical excipients. Methods and Results: The crystal transition of active pharmaceuticals ingredients from form II to form I in portion in clarithromycin sustained release tablets were confirmed by x-ray powder diffraction. The techniques including differential scanning calorimetry and infrared spectroscopy, x-ray powder diffraction were used for assessing the compatibility between clarithromycin and several excipients as magnesium stearate, lactose, sodium carboxymethyl cellulose, polyvinyl-pyrrolidone K-30 and microcrystalline cellulose. All of these methods showed compatibilities between clarithromycin and the selected excipients. Alcohol prescription simulation was also done, which showed incompatibility between clarithromycin and concentration alcohol. Conclusion: It was confirmed that the reason for the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.
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Sharma, Deepak, Gurmeet Singh, Dinesh Kumar, and Mankaran Singh. "Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate, Cetirizine Hydrochloride in Combined Pharmaceutical Dosage Form: A New Era in Novel Drug Delivery for Pediatrics and Geriatrics." Journal of Drug Delivery 2015 (February 25, 2015): 1–10. http://dx.doi.org/10.1155/2015/640529.
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The objective of the present study was to prepare the fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form for respiratory disorders such as bronchitis, asthma, and coughing for pediatrics and geriatrics. The tablets were prepared by direct compression technique. Superdisintegrant such as Sodium Starch Glycolate was optimized as 4% on the basis of least disintegration time. Different binders such as MCC and PVP K-30 were optimized along with optimized superdisintegrant concentration. 1% MCC was selected as optimum binder concentration on the basis of least disintegration time. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and drug content uniformity. Optimized formulation was further evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. Percent weight variation and content uniformity were within the acceptable limit. The friability was less than 1%. The wetting time and disintegration time were practically good for all formulations. FTIR studies and accelerated stability study showed that there was no interaction between the drug and excipients. It was concluded that, by employing commonly available pharmaceutical excipients such as superdisintegrants, hydrophilic and swellable excipients and proper filler, a fast disintegrating tablet of Salbutamol Sulphate, Cetirizine Hydrochloride in combined tablet dosage form, were formulated successfully with desired characteristics.
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., Pooja, Pankaj Kumar Sharma, and Viswanath Agrahari. "DESIGN AND EVALUATION OF SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS OF ALVERINE FOR ENHANCEMENT OF SOLUBILITY." International Research Journal of Pharmacy 12, no. 7 (2021): 25–31. http://dx.doi.org/10.7897/2230-8407.1207153.
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Background: The aim of this study is to develop a liquid self-nano emulsifying drug delivery system for alverine (liquid-SNEDDS).Excipients in the alverine SNEDDS include Ethyl oleate as the oil phase, Tween 80 as a surfactant, and PEG600, Propylene glycol as a cosurfactant.The prepared eleven formulations of alverine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies.The optimised alverine liquid SNEDDS formulation (D1) was studied for drug-excipient compatibility using infrared spectroscopy, as well as particle size, zeta potential, transmission electron microscopy, and stability. Alverine SNEDDS have a spherical shape with uniform particle distribution, according to their morphology. D1's optimised formulation's drug release percentage (96.6). The stability data revealed no discernible changes in drug content, emulsifying properties, drug release, or appearance. As a result, a potential SNEDDS formulation of alverine with improved solubility, dissolution rate, and bioavailability was developed.
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Budai-Szűcs, Mária, Gabriella Horvát, Barnabás Áron Szilágyi, et al. "Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations." Journal of Ophthalmology 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/2647264.
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Dry eye disease is a relatively common ocular problem, which causes eye discomfort and visual disorders leading to a decrease in the quality of life. The aim of this study was to find a possible excipient for eye drop formulations, which is able to stabilize the tear film. A cationic thiolated polyaspartamide polymer, poly[(N-mercaptoethylaspartamide)-co-(N-(N′,N′-dimethylaminoethyl)aspartamide)] (ThioPASP-DME), was used as a potential vehicle. Besides satisfying the basic requirements, the chemical structure of ThioPASP-DME is similar to those of ocular mucins as it is a protein-like polymer bearing a considerable number of thiol groups. The solution of the polymer is therefore able to mimic the physiological properties of the mucins and it can interact with the mucus layer via disulphide bond formation. The resultant mucoadhesion provides a prolonged residence time and ensures protective effect for the corneal/conjunctival epithelium. ThioPASP-DME also has an antioxidant effect due to the presence of the thiol groups. The applicability of ThioPASP-DME as a potential excipient in eye drops was determined by means of ocular compatibility tests and through examinations of the interactions with the mucosal surface. The results indicate that ThioPASP-DME can serve as a potential eye drop excipient for the therapy of dry eye disease.
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Kopelman, Susan H., and Larry L. Augsburger. "Excipient compatibility study of Hypericum perforatum extract (St. John's Wort) using similarity metrics to track phytochemical profile changes." International Journal of Pharmaceutics 237, no. 1-2 (2002): 35–46. http://dx.doi.org/10.1016/s0378-5173(02)00025-x.
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Sharma, Hemanta Kumar, and Lila Kanta Nath. "Study of the Effect of Dillenia indica Fruit Mucilage on the Properties of Metformin Hydrochloride Loaded Spray Dried Microspheres." International Scholarly Research Notices 2014 (November 20, 2014): 1–6. http://dx.doi.org/10.1155/2014/628382.
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Natural materials are preferred over synthetic counterparts because of their biodegradable and biocompatible nature. The present work was proposed to utilize mucilage from natural source for the development of controlled release formulation of metformin hydrochloride. Natural mucilaginous substance extracted from Dillenia indica L. (DI) fruit was used in fabricating controlled release microspheres. The microspheres were prepared by spray drying method under different formulation parameters. The prepared microspheres were studied for particle size, drug excipient compatibility, particle shape and surface morphologies, drug entrapment efficiency, mucoadhesivity, and in vitro drug release properties. The prepared microspheres exhibited mucoadhesive properties and demonstrated controlled release of metformin hydrochloride. The study reveals that the natural materials can be used for formulation of controlled release microspheres and would provide ample opportunities for further study.
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Toma, Claudia Crina, Teodora Alina Neag, and Bogdan Tita. "Thermal Characterization of Extracts Obtained from Different Parts of Nigella damascena (Ranunculaceae) by TG and DSC." Revista de Chimie 68, no. 5 (2017): 1007–9. http://dx.doi.org/10.37358/rc.17.5.5599.
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The increased search for herbal products has generated an increasing interest in improving the quality control of extracts by pharmaceutical industry since these are raw materials of great importance by their quality and versatility. Thermal analysis such as thermogravimetry (TG) is a technique of high sensitivity, reproductibility and rapid response to variations in mass, obtaining results related to the composition and thermal stability of the sample, being important to the characterization of raw plants. Thermogravimetric techniques and differential scaning calorimetry (DSC) used for the study of pre-formulation of drug-excipient compatibility have been gaining importance. These techniques are being used for the verification of possible interactions between drugs and excipients. Aiming at studying the behavior of a plant extract, using these thermoanalytical techniques, the plant species Nigella damascena semen and Nigella damascena herba was used. This plant has healing and anti-inflammatory properties. The methodology for obtaining the extract followed the European Pharmacopoeia methodology. The TG and DSC curves were obtained under nitrogen and air atmosphere (20 mL/min) at a heating rate of 10�C/min. The TG and DSC tests were analyzed within a temperature range from 25 to 1000�C.
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Jagdale, Swati C., and Payal V. Kothekar. "Development of Emulgel Delivery of Mupirocin for Treatment of Skin Infection." Recent Patents on Anti-Infective Drug Discovery 15, no. 2 (2020): 137–56. http://dx.doi.org/10.2174/1386207323999200819153404.
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Aim:: To design controlled release topical delivery of mupirocin for the treatment of skin infection. Background:: Mupirocin is an antibacterial drug. Mupirocin works to kill the bacteria, which include strains of Staphylococcus aureus and Streptococcus pyogenes. It is also used for the treatment of inflammation of a hair follicle. The half-life of mupirocin is only 20-40 min. It has very slight solubility in water. Patent literature had shown work on ointment, antibiotic composition, nasal and topical composition. Emulgel is a duel control release system for the topical delivery of hydrophobic drugs. Objective:: The objective was to formulate emulgel with controlled delivery of mupirocin using Sepineo P 600. Methods:: Soya oil, tween 80 and polyethylene glycol 400 (Oil:Surfactant:Cosurfactant) were used for emulsion formulation. Emulgel was optimized by 32 factorial design. Sepineo P 600 and hydroxy propyl methyl cellulose K4M were used as independent variables. Drug excipient compatibility analysis was carried out by FTIR, UV and DSC spectra. Emulgel was evaluated for its physical characterization, in vitro release, ex vivo release, antimicrobial and anti-inflammatory study. Results:: DSC, UV and FTIR analysis confirmed drug excipient compatibility. FE SEM showed a size range between 228-255 nm. Zeta potential was found to be -25.1 mV, which showed good stability of the emulsion. Design expert software showed F2 as an optimized batch. Release studies indicated that the controlled release of drugs forms Sepineo P 600 gel due to its higher gelling capacity. Batch F2 showed comparable results with marketed formulation against Staphylococcus aureus. For batch F2, 40 μg/ml was the minimal inhibitory concentration. Conclusion:: Antimicrobial and anti-inflammatory study proved successful development of stably controlled release mupirocin emulgel.
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N., Manjunath P., Satish C. S., Vasanti S., Preetham A. C., and Naidu Ras. "FORMULATION AND EVALUATION OF SIMVASTATIN GASTRORETENTIVE DRUG DELIVERY SYSTEM." International Journal of Applied Pharmaceutics 9, no. 3 (2017): 55. http://dx.doi.org/10.22159/ijap.2017v9i3.18763.
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Objective: The aim of this study was to formulate and evaluate gastro retentive drug delivery system (GRRDS) using an effervescent approach for simvastatin.Methods: Floating tablets were prepared using directly compressible polymers hydroxypropyl methylcellulose (HPMC) K100M, HPMC K4M and carboxymethylcellulose sodium (NaCMC). The prepared tablets were subjected to pre-formulation studies like Compressibility index, Hausner ratio and post compression parameters like buoyancy/floating test and In vitro dissolution study.Results: Drug-excipient compatibility studies performed with the help of FTIR instrument indicated that there were no interactions. The DSC thermogram of the formulations revealed that crystalline form of simvastatin existed in the formulation which was confirmed by X-ray powder diffraction. Dissolution studies indicated that there was a decrease in the drug release with an increase in the polymer viscosity. The tablets prepared with low-viscosity grade HPMC K4M exhibited short Buoyancy Lag Time and floated for a longer duration as compared with formulations containing high viscosity grade HPMC K100M. The ‘n’ value for dissolution studies for all the formulations was found to be in the range of 0.647 to 0.975 indicating non-Fickian or anomalous drug transport. Conclusion: The drug release rate and floating duration of tablets depended on the nature of the polymer and other added excipients. The release rate of the drug can be optimized by using different ratios of polymers and other excipients. The formulation F8 achieved the optimized batch and complied with all the properties of the tablets.
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Sharma, Hemanta Kumar, Sunita Lahkar, and Lila Kanta Nath. "Formulation and in vitro evaluation of metformin hydrochloride loaded microspheres prepared with polysaccharide extracted from natural sources." Acta Pharmaceutica 63, no. 2 (2013): 209–22. http://dx.doi.org/10.2478/acph-2013-0019.
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The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study
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Pakhale, Nilesh V., S. B. Gondkar, and R. B. Saudagar. "Formulation Development and Evalua Tion of Fluoxetine Effervescent Floating Tablet." Journal of Drug Delivery and Therapeutics 9, no. 4-A (2019): 358–66. http://dx.doi.org/10.22270/jddt.v9i4-a.3490.
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The objective of the present study was to formulate and evaluate Effervescent Floating Tablet of Fluoxetine for the treatment of antidepressant agent. Tablets were prepared by direct compression using directly compressible polymers such as HPMC K4M, and Carbopol 934 were evaluated for drug-excipient compatibility, density, buoyancy test, swelling study, drug content and In-Vitro release profile. Sodium bicarbonate and citric acid were used producing effervescent base for buoyancy of tablets. Analysis of drug release from tablet indicates drug release by zero order, first order rate kinetics. No significant change was observed in physical appearance, drug content, floatability or in-vitro dissolution pattern after storage at 450C/750C RH for three months.
 Keywords: Floating effervescent tablet, GIT, Fluoxetine , HPMC K4M, Carbopol 934.
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Enéas, Paula Cristina Rezende, Renata Barbosa de Oliveira, and Gerson Antônio Pianetti. "Oxcarbazepine: validation and application of an analytical method." Brazilian Journal of Pharmaceutical Sciences 46, no. 2 (2010): 265–72. http://dx.doi.org/10.1590/s1984-82502010000200013.
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Oxcarbazepine (OXC) is an important anticonvulsant and mood stabilizing drug. A pharmacopoeial monograph for OXC is not yet available and therefore the development and validation of a new analytical method for quantification of this drug is essential. In the present study, a UV spectrophotometric method for the determination of OXC was developed. The various parameters, such as linearity, precision, accuracy and specificity, were studied according to International Conference on Harmonization Guidelines. Batches of 150 mg OXC capsules were prepared and analyzed using the validated UV method. The formulations were also evaluated for parameters including drug-excipient compatibility, flowability, uniformity of weight, disintegration time, assay, uniformity of content and the amount of drug dissolved during the first hour.
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Vimalson, D. Christopher, S. Parimalakrishnan, N. S. Jeganathan, and S. Anbazhagan. "SOLID DISPERSION TECHNIQUE TO ENHANCE THE SOLUBILITY AND DISSOLUTION OF FEBUXOSTAT AN BCS CLASS II DRUG." International Journal of Applied Pharmaceutics 11, no. 1 (2019): 241. http://dx.doi.org/10.22159/ijap.2019v11i1.30539.
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Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method.
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Rahman, Yasir, Saima Amin, Showkat R. Mir, and Kanchan Kohli. "Pre-Formulation Study for Palatable Microbeads of Lycopene." Journal of Drug Delivery and Therapeutics 9, no. 4-A (2019): 320–27. http://dx.doi.org/10.22270/jddt.v9i4-a.3484.
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Lycopene is a widely used nutraceuticals for its antioxidant property but the molecule has poor aqueous solubility, high instability, and extremely low intestinal permeability leading to its poor bioavailability. In the present study, pre-formulation study was carried out to prepare sodium alginate microbeads with the intention to deliver an effective amount of lycopene for high absorption through oral route. A thorough physical characterization and spectral analysis were done to understand the characteristic of lycopene such as its melting point, UV spectrophotometric analysis, chromatography through reverse phase HPLC. Fourier transform infrared spectroscopy and differential scanning calorimetry were adopted to know the interaction of sodium alginate with lycopene. Box-Behnken design (version 9.0.2.0, Stat Ease Inc, USA) was used to analyse the effect of formulation variables such as sodium alginate (%), glutaraldehyde (%) and stirring speed on lycopene entrapment and its loading into microbeads. The adopted preformulation strategy revealed that lycopene was a crystalline powder with a sharp melting point at 155oC and the prominent functional groups were present in the sample. UV and HPLC analysis revealed precise quantitation and authenticity of lycopene. Excipient compatibility also revealed inertness of sodium alginate. Response surface morphology revealed significant effect of alginate, glutaraldehyde and stirring speed on formation of best composition. Therefore, it is concluded that lycopene can be formulated as microbeads for oral drug delivery.
 Keywords: lycopene, sodium alginate, permeation, absorption, microbeads
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D. V. R. N., Bhikshapathi, and Muralichand G. "Development, Solubility Enhancement and Characterization of Nimodipine Solid Dispersions." International Journal of Pharmaceutical Sciences and Nanotechnology 11, no. 5 (2018): 4231–39. http://dx.doi.org/10.37285/ijpsn.2018.11.5.2.
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The main aim of this study was to formulate and characterize nimodipine solid dispersions using various novel polymers. Solid dispersions were prepared by solvent evaporation method in order to improve the solubility and overall bioavailability of nimodipine. Solubility and dissolution studies indicate that Kolliwax RH 40 is the most suitable polymer. The solubility studies was corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96 ± 5.15% in about 90 minutes. In vitro release data from several formulations containing Nimodipine was determined kinetically using different mathematical models like Zero order, First order, Higuchi, and Korsmeyer–Peppas model. XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. These results confirm the viability of enhancing the solubility of nimodipine by formulating the drug as solid dispersions in Kolliwax.
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Salman, B. Syed, and Mohd Abdul Hannan Baig. "Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method." International Journal of Research in Pharmaceutical Sciences and Technology 1, no. 2 (2019): 73–78. http://dx.doi.org/10.33974/ijrpst.v1i2.148.
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Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.
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K, Raja Rajeswari, and V. Rama Mohan Gupta. "Solubility Enhancement of Ebastine by Self-Nanoemulsifying Delivery Strategy: Formulation, Optimization and Characterization." International Journal of Pharmaceutical Sciences and Nanotechnology 10, no. 4 (2017): 3779–87. http://dx.doi.org/10.37285/ijpsn.2017.10.4.5.
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The aim of the study was to develop and optimize Self-nanoemulsifying drug delivery systems (SNEDDS) for the improvement of solubility and dissolution of an anti-allergic drug, Ebastine, a BCS class II drug. Preliminary screening was carried out to select proper components combination of Oil (Oleic acid): Surfactant (Tween® 80): Co-solvent (Ethanol). Pseudo-ternary phase diagram experimental design was applied to formulate and optimize the SNEDDS containing 3:7 of (oil: Smix). Drug-Excipient compatibility studies were performed by FTIR and found no chemical interaction between the drug and excipients. The systems were assessed for evaluation parameters like optical clarity in three stages by exposing the SNEDDS to heating-cooling cycle at 4 to 45 oC, centrifugation at 5000rpm and freeze-thaw cycles at -21 oC to 21 oC. The droplets of optimized SNEDDS formulation were found to be spherical with a size range of 76-111nm and emulsification efficiency of 97.67 ± 0.3% and 91.1 ± 0.06% drug release at the end of 30 minutes with a significant increase in dissolution rate compared to the marketed drug suspension under the same conditions. The optimized SNEDDS formulation charged for the accelerated stability studies at 40 oC/75% RH for three months revealed to be stable with 95.31 ± 1.4% drug content and 90.12 ± 1.98% drug release. It was hence concluded that the solubility of poorly soluble drugs like Ebastine can be effectively enhanced using Self nano emulsifying approaches with the use of Oleic acid, Tween 80 and Ethanol as Oil, surfactant and co-solvent respectively. 
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Devara, Rajakumar, Mohammed Habibuddin, and Jithan Aukunuru. "ENHANCEMENT OF DISSOLUTION RATE OF POORLY SOLUBLE DRUG ITRACONAZOLE BY NANOSUSPENSION TECHNOLOGY: ITS PREPARATION AND EVALUATION STUDIES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 4 (2018): 414. http://dx.doi.org/10.22159/ajpcr.2018.v11i4.19933.
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Objective: The objective of this study was to prepare and evaluate itraconazole (ITZ) nanosuspensionsusing polymer Eudragit RL-100 and stabilizer Tween-80 by nanoprecipitation method.Materials and Methods: Itraconazole is a potent broad-spectrum Biopharmaceutical Classification System Class II triazole antifungal drug. Nanosuspensions were prepared using solvent displacement/nanoprecipitation method with the help of Eudragit RL-100 as rate-controlled polymer in different ratios and using Tween-80 as stabilizer. The nanosuspension preparation was optimized for particle size by investigating two factors that are solvent:anti-solvent ratio and surfactant concentration, at three levels. The prepared nanosuspensions were evaluated and characterized for particle size, drug excipient compatibility, percentage yield, drug entrapment efficiency, surface morphology, zeta potential, saturation solubility, solid state, and in vitro drug release studies.Results: The nanosuspensions of itraconazole were successfully prepared using solvent displacement/nanoprecipitation method. The two factors solvent: anti-solvent ratio and surfactant concentration influenced the particle size of the nanosuspensions prepared. The Fourier-transform infrared spectroscopy studies confirmed that drug and excipients are compatible, and the X-ray powdered diffraction and differential scanning calorimetry results indicated that the nanoprecipitation method led to the amorphization of itraconazole. Itraconazolenanosuspensions increased the saturation solubility to an extent of 4 times. Itraconazole nanosuspensions completely dissolved in the dissolution medium within 10 s and 72% drug release within 5 min, while the pure drug was dissolved only up to 20% in 15 min and nanosuspensions showed increased dissolution rate of 3 folds, the active drug.Conclusions: Stable itraconazole nanosuspensions were successfully prepared and these nanosuspensions demonstrated dramatic improvement in dissolution rate of the active drug.
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Bhusara, Hiral S., Ara T. Patel, and Mayuree D. Patel. "Development of gastroretentiv floating tablets of losartan potassium by sublimation method." International Journal of Pharmaceutical Chemistry and Analysis 8, no. 2 (2021): 66–74. http://dx.doi.org/10.18231/j.ijpca.2021.014.
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The purpose of present study was to formulate and Evaluate Sustained release floating tablet of losartan Potassium using Camphor and Polyethylene Oxide as Pore formation for floating and release retarding agent respectively to improve gastric residence time and patient compliance in management of hypertension. The tablet was prepared by direct compression by using HPMC K4 as dry binder. Camphor and PEO as floating and release retarding agent for sustained release floating tablet. Post compression was done to increase the hardness and floating time of tablet. Release modifier was used to speed up the release of drug from sustained release floating tablet. The effect of two independent variables like amount of Sublimating agent (camphor) and amount of Polyethylene oxide (PEO) on Q30min, Q360min, and Q720min was optimized using 32 factorial design and analyzed using the software design expert 10.0.3. The observed (actual values) responses were coincided well with the predicted values, given by the optimization technique. The floating tablet were characterized by FTIR for drug excipient compatibility.
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Brondi, Ariadne M., Jerusa S. Garcia, and Marcello G. Trevisan. "Development and Validation of a Chromatography Method Using Tandem UV/Charged Aerosol Detector for Simultaneous Determination of Amlodipine Besylate and Olmesartan Medoxomil: Application to Drug-Excipient Compatibility Study." Journal of Analytical Methods in Chemistry 2017 (2017): 1–8. http://dx.doi.org/10.1155/2017/4878316.
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A study was carried out to investigate compatibility of amlodipine besylate and olmesartan medoxomil with a variety of pharmaceutical excipients. Both drugs are antihypertensive agents that can be administered alone, in monotherapy, or in pharmaceutical association. The studies were performed using binary and ternary mixtures, and samples were stored for 3 and 6 months at 40°C under 75% relative humidity and dry conditions. For this study, a method based on high-performance liquid chromatography (HPLC) was developed and validated for the simultaneous determination of amlodipine besylate and olmesartan medoxomil in samples from pharmaceutical preformulation studies using diode array detector (DAD) and charged aerosol detector (CAD). The runtime per sample was 10 min with retention time of 7.926 min and 4.408 min for amlodipine and olmesartan, respectively. The validation was performed according to ICH guidelines. The calibration curve presents linear dynamic range from 12 to 250 μg mL−1 for amlodipine and from 25 to 500 μg mL−1 for olmesartan with coefficient of determination (R2 ≥ 0.9908) while repeatability and reproducibility (expressed as relative standard deviation) were lower than 1.0%. The excipients such as corn starch, croscarmellose sodium, magnesium stearate, polyvinyl alcohol, talc, polyvinylpyrrolidone, lactose monohydrate, and polyethylene glycol showed potential incompatibilities after accelerated stability testing.
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Al-dhahir, Rasha Khalid, and Myasar Al-kotaji. "FORMULATION OF ORALLY DISINTEGRATING TABLETS OF CINNARIZINE BY USING DIRECT COMPRESSION METHOD." International Journal of Applied Pharmaceutics 11, no. 1 (2019): 117. http://dx.doi.org/10.22159/ijap.2019v11i1.29599.
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Objective: The aim of this work was to formulate and evaluate orally disintegrating tablets of cinnarizine that were prepared by direct compression method using different types of diluents and super disintegrants. The rationale behind this work was to accelerate the disintegration of the tablet to provide rapid dissolution, quick action and enhanced bioavailability of the drug.Methods: The tablets were prepared by direct compression method using different types of diluents as mannitol, microcrystalline cellulose (MCC), and lactose. Different super disintegrants were used such as crospovidone (CP), sodium starch glycolate (SSG) and Kyron T-314; Kyron T-314 was used in different concentrations of 5%, 6%, 7%, and 8%. The prepared formulae (F1-F9c) were subjected to flowability studies and post-compression evaluation studies. The optimized formula was selected depending on the time of disintegration and dissolution; then it was subjected to drug-excipient compatibility study and stability study.Results: Flowability results were ranging from excellent, excellent to good, and good to fair according to the type of the diluent used. All of the prepared tablets showed acceptable hardness, friability, drug content, and disintegration. A rapid disintegration of 11.66±2.25 s with the highest percentage 2 min-drug release of 74.55±3.01% was obtained by using the diluent lactose and the super disintegrant Kyron T-314 (8%) in the formula F9c. The infrared spectroscopic studies of the formula F9c showed no drug-excipient interaction. In addition, the stability study indicated that the optimized formula is a stable formula.Conclusion: Formula F9c of a rapidly disintegrating tablet was easy to be manufactured, and the results showed that this formula had a rapid disintegration, high dissolution profile, no noticeable chemical incompatibility and it was stable upon storage.
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Sirisha, Yella, Gopala Krishna Murthy T E, and Avanapu Srinivasa Rao. "EFFECT OF FORMULATION FACTORS ON ORODISPERSIBLE TRIPTAN FORMULATIONS – NOVEL APPROACH IN TREATMENT OF MIGRAINE." Asian Journal of Pharmaceutical and Clinical Research 11, no. 3 (2018): 212. http://dx.doi.org/10.22159/ajpcr.2018.v11i3.23401.
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Objective: The present research work is an attempt to determine the effect of various diluents and superdisintegrants on drug release of eletriptan orodispersible tablets and designs an optimized formulation using 22 factorial design. Further, evaluate the tablets for various pre-compression and post-compression parameters.Methods: The drug excipient compatibility study was conducted by infrared spectroscopy, differential scanning colorimetry and X-ray diffraction studies were conducted to test the purity of the drug. The tablets were formulated by direct compression method using spray dried lactose, mannitol, microcrystalline cellulose, starch as diluents and crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants. The powder formulations were evaluated for pre-compression parameters such as bulk density, tapped density, Carr’s Index, Hausner’s ratio, and angle of repose. The tablets were evaluated for post-compression parameters such as the hardness, thickness, friability, weight variation, and disintegrating time in the oral cavity, in vitro drug release kinetics studies, and accelerated stability studies. The formulations were optimized by 22 factorial design.Results: The drug and excipients were compatible, and no interaction was found. The drug was pure, and all the pre-compression parameters were within Indian Pharmacopoeial Limits. Post-compression parameters were also within limits. The disintegration time was found to be 27 s for the formulation F29 containing Croscarmellose sodium (5%) and Mannitol as diluent, and in vitro drug release was found to be 99.67% in 30 min and follows first-order kinetics. This was also the optimized formulation by 22 factorial design with a p=0.013.Conclusion: The orodispersible tablets of eletriptan were successfully formulated, and the optimized formulation was determined that can be used in the treatment of migraine.
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Chaudhari, Pallavi M., and Madhavi A. Kuchekar. "DEVELOPMENT AND EVALUATION OF NANOEMULSION AS A CARRIER FOR TOPICAL DELIVERY SYSTEM BY BOX-BEHNKEN DESIGN." Asian Journal of Pharmaceutical and Clinical Research 11, no. 8 (2018): 286. http://dx.doi.org/10.22159/ajpcr.2018.v11i8.26359.
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Objective: The aim of this study was to develop a nanoemulsion for topical delivery. Methods: Topical nanoemulsion was prepared by homogenization method. Box-behnken design was utilized to study the effect of oil, surfactant and Co-surfactant, on droplet size, entrapment efficiency and drug release. Nabumetone a non-steroidal anti-inflammatory drug was incorporated in castor oil with Tween 80 and Polyethylene glycol 600 to form the nanoemulsion by homogenization method. The nanoemulsion was further subjected to different evaluation parameters and ex-vivo study. The crystalline nature of drug was confirmed by powder X-ray diffraction studies. Drug-excipient compatibility was confirmed by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), respectively. Results: The average globule size of nabumetone-containing nanoemulsion decreased with decrease in concentration of oil and surfactant. Nanoemulsion was evaluated by pH, rheology, globule size, zeta potential, scanning electron microscopy, DSC, FTIR spectroscopy, and stability. In vitro drug release shows maximum 84.35% permeation rate through cellophane membrane and ex-vivo drug release shows 86.32% permeation rate through goat skin. Conclusion: Thus, the nanoemulsion formulated showed good results regarding topical delivery.
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Ishan Dubey, Manmeet Singh Saluja, Ritu M Gilhotra, and Mahavir Chhajed. "Evaluation of Polyherbal Anticancer Tablets: A Review." Journal of Pharmaceutical Technology, Research and Management 6, no. 1 (2018): 67–79. http://dx.doi.org/10.15415/jptrm.2018.61006.
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Cancer is a malignant abnormal growth of cells, one of the most dreaded and complex diseases. It concerns with several tempo spatial changes in cell composition, which finally lead to neoplasia. Various types of cancers have been reported. Chemotherapy, radiation, and/or surgery may cure them. Herbal remedies are supposed to be harmless as they cause fewer complications and are less likely to habitual. Antioxidant compositions of therapeutic plants show the anticancer activity and therefore, use of different proportions of the active components to formulate various standardized preparation with single or multiple components for their synergistic effects play a crucial role in curing cancer. Evaluation parameters to assess the in vitro anticancer activity includes Caspase-3, Caspase-9, alamar blue, LDH assay, XTT assay, sulforhodamine-B assay, MTT assay, DNA fragmentation assay, neutral red uptake cytotoxic assay, tryphan blue assay. Evaluation of dried extract or granules includes bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose while the tablets evaluated by drug-excipient compatibility study by FT-IR, stability studies, hardness, thickness, weight variation, friability, disintegration time and dissolution test.
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Ciurba, Adriana, Paula Antonoaea, Nicoleta Todoran, et al. "Polymeric Films Containing Tenoxicam as Prospective Transdermal Drug Delivery Systems: Design and Characterization." Processes 9, no. 1 (2021): 136. http://dx.doi.org/10.3390/pr9010136.
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The administration of drugs via transdermal therapeutic systems has become an attractive form of therapeutic approach, considering its advantages and the high patient compliance achieved, making them a viable alternative, especially in the treatment of chronic diseases. The purpose of our study was the development of polymer-based films containing tenoxicam (TX) and the analysis of dissolution kinetics. Auxiliary substances represent an important part of pharmaceutical forms, so during the first stage, TX and excipient compatibility were verified. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analyses were performed on TX and on physical mixtures of TX-HPMCE5 and TX-HPMC15kcP. Three polymeric films of TX (TX1, TX2, and TX3) were prepared using a solvent evaporation technique. Release studies were done at 32 °C ± 1 °C with a Franz diffusion cell. The results of the DSC and FT-IR analyses demonstrated the compatibility of the active substance with the two matrix-forming polymers. The results obtained in the release studies of TX from the proposed polymeric films suggested a pH-dependent behavior in all three polymeric films. At pH 5.5, flux values were between 8.058 ± 0.125 μg × cm−2 × h−1 and 10.850 ± 0.380 μg × cm−2×h−1; and at pH 7.4, between 10.990 ± 0.2.490 μg×cm−2×h−1 and 53.140 ± 0.196 μg × cm−2 × h−1. The Korsmeyer–Peppas model described a non-Fickian transport mechanism. The n values varied between 0.63–0.7 at pH 5.5 and 0.73–0.86 at pH 7.4, which suggested a diffusion depending on the matrix hydration and polymer relaxation.
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Ciurba, Adriana, Paula Antonoaea, Nicoleta Todoran, et al. "Polymeric Films Containing Tenoxicam as Prospective Transdermal Drug Delivery Systems: Design and Characterization." Processes 9, no. 1 (2021): 136. http://dx.doi.org/10.3390/pr9010136.
Full textAbstract:
The administration of drugs via transdermal therapeutic systems has become an attractive form of therapeutic approach, considering its advantages and the high patient compliance achieved, making them a viable alternative, especially in the treatment of chronic diseases. The purpose of our study was the development of polymer-based films containing tenoxicam (TX) and the analysis of dissolution kinetics. Auxiliary substances represent an important part of pharmaceutical forms, so during the first stage, TX and excipient compatibility were verified. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analyses were performed on TX and on physical mixtures of TX-HPMCE5 and TX-HPMC15kcP. Three polymeric films of TX (TX1, TX2, and TX3) were prepared using a solvent evaporation technique. Release studies were done at 32 °C ± 1 °C with a Franz diffusion cell. The results of the DSC and FT-IR analyses demonstrated the compatibility of the active substance with the two matrix-forming polymers. The results obtained in the release studies of TX from the proposed polymeric films suggested a pH-dependent behavior in all three polymeric films. At pH 5.5, flux values were between 8.058 ± 0.125 μg·cm−2·h−1 and 10.850 ± 0.380 μg·cm−2·h−1; and at pH 7.4, between 10.990 ± 0.2.490 μg·cm−2·h−1 and 53.140 ± 0.196 μg·cm−2·h−1. The Korsmeyer–Peppas model described a non-Fickian transport mechanism. The n values varied between 0.63–0.7 at pH 5.5 and 0.73–0.86 at pH 7.4, which suggested a diffusion depending on the matrix hydration and polymer relaxation.
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Chourasia, Ayushi, and Shikha Agrawal. "DEVELOPMENT AND EVALUATION OF CIPROFLOXACIN HYDROCHLORIDE LOADED OCULAR INSERT BY USING “PLANTAGO OVATA” AS NATURAL POLYMER." International Journal of Current Pharmaceutical Research 10, no. 4 (2018): 79. http://dx.doi.org/10.22159/ijcpr.2018v10i4.28474.
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Objective: The present work focus in the direction of “Development and evaluation of Ciprofloxacin Hydrochloride loaded ocular insert by using “plantago ovata” as natural polymer”. The current work was carried out to evaluate the control release profile of ocular insert. Natural polymer in ocular insert was used for studying the long acting property. Natural polymer is also used to enhance the bioavailability of drug and reduce toxicity. It is also used to increase the duration of action of drug for prolongs action and gives better in vitro performance as compare than to the conventional ocular formulation.Methods: Solvent casting method was used in the formulation of Ciprofloxacin Hydrochloride loaded ocular inserts. Different ocular insert formulations of varying polymer concentration were prepared. Ocular insert formulation H-1 to H-3 was prepared by using different concentration of HPMC and formulation P-1 to P-4 was prepared by using different concentration of Plantago Ovata.Results: The ocular inserts formulation was within the acceptable limits. All the pre formulation parameters of polymers such as derived properties, compressibility index, Hausner’s ratio, viscosity, melting point, swelling ratio, loss on drying, PH of mucilage solution and pre formulation of active pharmaceutical ingredient such as estimation of drug by using UV spectroscopy, determination of melting point, solubility, partition coefficient and FTIR for compatibility study of drug and excipient were evaluation. FTIR analysis also confirmed no drug-excipient interaction.Conclusion: Prepared inserts in the present study were semitransparent. The mixing of the drug in to the polymer is uniform, due to this; the drug content of all formulation is good. Formulation P4 was selected because it showed better release profile, drug content and other physicochemical properties than other formulated batch when compare. All the prepared inserts showed in vitro drug release for the period of 4 h as compare to the marketed formulation. An in vitro drug release study revealed that ocular formulation gives a prolong action. The formulation was found to be long acting.
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Eraga, S. O., C. M. Okolo, B. U. Odionyenma, C. E. Mbadugha, and M. A. Iwuagwu. "A Comparative Evaluation of Fast Dissolving Tablets of Acetaminophen Using Super-disintegrant Blends and Sublimation Method." Journal of Phytomedicine and Therapeutics 19, no. 1 (2020): 375–86. http://dx.doi.org/10.4314/jopat.v19i1.3.
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Fast disintegrating tablets (FDTs) are gaining prominence as drug delivery systems and emerging as one of the popular and widely accepted dosage forms, especially for the peadiatric and geriatric patients. This study aims to evaluate and compare the tablet properties of fast disintegrating tablets of acetaminophen prepared by super-disintegrant blends and sublimation methods. Two groups of tablets comprising various batches were prepared by wet granulation. Granules batches of one group of tablets (A-G) were prepared with different concentrations of sodium starch glycolate and croscarmellose sodium while the other group of tablets (H-N) were incorporated with varying concentrations of menthol into the batches. The granules were subjected to analysis and compressed into tablets. The post-compression parameters of the tablets such as weight uniformity, crushing strength, friability, wetting and disintegration times, as well as dissolution studies were evaluated. Drug-excipient compatibility studies using Fourier transform infrared (FTIR) analysis was also carried out. Granules were fair to good in flow with Carr’s indices ≤ 20.14 and angles of repose ranging from 21.34 to 35.00°. Tablets crushing strength values were between 3.44 to 8.26 kp while their friability values were < 1.52%. They showed wetting and disintegration times that were ≥ 0.18 and ≥ 0.25 min. Dissolution studies showed that four batches of tablets (two from each method used in formulation) achieved 100% drug release within 30 min. FTIR analysis shows no interactions between acetaminophen and excipients used in formulation. Tablets from both methods were comparable in their tablet properties but the disintegrant blend tablets exhibited superior crushing strengths, hence formed harder tablets, while the sublimation method tablets were superior in their wetting and disintegration times.
 Keywords: acetaminophen, super-disintegrants, sublimation, tablet parameters
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B. Hamed, Sumaya, and Shaimaa N. Abd Alhammid. "Formulation and Characterization of Felodipine as an Oral Nanoemulsions." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 30, no. 1 (2021): 209–17. http://dx.doi.org/10.31351/vol30iss1pp209-217.
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Felodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Results of characterization showed that felodipine nanoemulsion (F3) with (oleic acid 10%) ,(Smix 60% of tween80 :ethanol in a ratio of 3:1), (DDW 30%) was selected as the best formula, since it has a particle size of (17.01)nm, low PDI (0.392), zeta potential (-22.34mV), good dilution without drug precipitation , higher percent of drug content (99.098%) with acceptable viscosity , and complete release of the drug after (45 min.) with significantly higher (P<0.05) dissolution rate in comparison with the pure drug powder. The selected formula (F3) subjected to further investigations as drug and excipient compatibility study by Fourier transform infrared spectroscopy (FTIR) The outcomes of the (FTIR) explain that the distinctive peaks for felodipine were not affected by other components and displayed the same functional group's band with very slight shifting. This indicates that there was no interaction between felodipine and other NE components. Therefore, these excipients were found to be compatible with felodipine. In conclusion, the NE was found to be an efficient method to enhance the dispersibility and permeatioins of drugs that have poor water solubility (lipophilic drugs).
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P, Vijayanand, Deepa A., and Bhagavan Raju M. "DEVELOPMENT, CHARACTERIZATION AND EVALUATION OF SOFT ORAL EDIBLE GEL USING GELLAN GUM." International Journal of Applied Pharmaceutics 9, no. 5 (2017): 73. http://dx.doi.org/10.22159/ijap.2017v9i5.19921.
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Objective: The objective of present research work was to formulate and evaluate a novel oral edible gel dosage form using gellan gum as gelling agent and carvedilol as a model drug to ease the administration to dysphagic and geriatric patients.Methods: Oral edible gels were prepared using gelling agent low acetylated gellan gum and sodium citrate in different concentrations. The prepared edible gel formulations were evaluated for gelation time, appearance, texture, viscosity, pH, syneresis, drug-excipient compatibility studies by fourier transform infrared FTIR and percentage of drug release from the gel formulation.Results: Formulation containing gellan gum (0.4 % w/v) and sodium citrate (0.3 % w/v)) was found to be “spoon thick” in consistency that is accepted for dysphagic patients as per national dysphagia diet task force. This formulation showed more than 95 % drug release within 12 min and found to be stable for 6 mo. All other parameters tested were optimal. Hence, this formulation was considered optimized.Conclusion: From this study, it can be concluded that the novel edible gel dosage form containing Carvedilol can be formulated and this dosage form may prove to be more efficacious in the treatment of hypertension in dysphagic patients.
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Vanitha, Kondi, Mohan Varma, and Alluri Ramesh. "Floating tablets of hydralazine hydrochloride: optimization and evaluation." Brazilian Journal of Pharmaceutical Sciences 49, no. 4 (2013): 811–19. http://dx.doi.org/10.1590/s1984-82502013000400021.
Full textAbstract:
Hydralazine hydrochloride has a half-life of 2 to 4 hours with an oral bioavailability of 26-50%. Since hydralazine has a demethylating effect on various suppressor genes, it can be used in various types of cancer to support chemotherapy. The purpose of this study was to optimize and evaluate floating tablets of hydralazine hydrochloride designed to prolong the gastric residence time and to provide controlled release of the drug for 14 h. The floating tablets of hydralazine hydrochloride were prepared by the wet granulation method. Semi-synthetic polymers of hydroxy propyl methyl cellulose (HPMC K100M) and ethyl cellulose were used as the release retarding agents. A 2² factorial design was applied to systematically optimize the drug release profile. The concentrations of HPMC K100M and ethyl cellulose were optimized to provide controlled release of hydralazine for 14h. Non-Fickian diffusion release transport was confirmed as the release mechanism for the optimized formulation and the predicted values agreed well with the experimental values. Drug excipient compatibility studies were investigated by FTIR, DSC and XRD. These data indicate that there were no chemical interactions between the drug and the polymer. In vivo X-ray imaging showed floating tablet performance in rabbits.
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Divya, B., J. Sreekanth, and D. Satyavati. "Development of Extended Release Formulations of Ilaprazole Tablets." Journal of Drug Delivery and Therapeutics 9, no. 3 (2019): 8–12. http://dx.doi.org/10.22270/jddt.v9i3.2811.
Full textAbstract:
Extended release products are designed to release their medication in a controlled manner at a predetermined rate, duration, and location to achieve and maintain optimum therapeutic blood levels of a drug. The objective of the study is to formulate and evaluate Ilaprazole Controlled release tablets comparable to the innovator product. F1-F9 formulations were prepared using varying concentrations of super disintegrates like Crospovidone, Croscarmellose sodium and Sodium starch glycolate in different concentrations. Based on the hardness, friability, weight variation, drug content, F6 formulation was found to be optimised. The selected F6 formulation was sub coated with HPMC P 50 and followed by enteric coating with Acryl-EZE-80 (Eudragit L100-55). 3 formulations (F10-F12) were prepared by using coating. Among the three formulations, F11 formulation was found to be best. FTIR studies were carried out to find out drug and excipient compatibility studies, the studies revealed that there were no interactions. DSC studies also carried out to demonstrate any changes in physical forms of the drug molecule.
 Keywords: Ilaprazole, Extended release tablets, Crospovidone, Croscarmellose sodium, Sodium starch glycolate, HPMC P 50, Acryl-EZE-80.
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Di, Li, Edward H. Kerns, Hong Chen, and Susan L. Petusky. "Development and Application of an Automated Solution Stability Assay for Drug Discovery." Journal of Biomolecular Screening 11, no. 1 (2005): 40–47. http://dx.doi.org/10.1177/1087057105281363.
Full textAbstract:
Screening of solution stability provides an early alert on potential liabilities of drug candidates so that strategies can be developed to overcome the challenges. Afully automated solution stability assay has been developed to accelerate traditionalmanual operation. The assay uses the advanced capabilities of a high-performance liquid chromatography instrument that is present in many pharmaceutical research laboratories. The samples are prepared automatically by a temperature-controlled autosampler. The samples are delivered to the stability matrices, mixed, incubated, and injected at selected time points during the reaction time course. This automated process occurs without operator intervention, thus allowing 96 experiments to be run with0.5hof a scientist's time compared to 8 h for the same studywhenperformedmanually. Automationnotonly eliminates themanual operation but also improves accuracy and throughput. The assay protocol has been optimized to achieve homogenous mixing and eliminate carryover. The assay is robust, flexible, and high throughput. It can be used to study stability for a large number of samples undermultiple incubation conditions and has awide range of applications in drug discovery and development, such as screening compound stability in biological assaymedia, obtaining a stability-pH profile, surveying compound stability in physiological fluids, and performing development forced degradation and excipient compatibility.
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Mandava, Kiranmai, Kruthika Lalit та Venu Madhav Katla. "Formulation and Evaluation of Ketoprofen Using β-Cyclodextrin Capped Silver Nanoparticles". International Journal of Pharmaceutical Sciences and Nanotechnology 14, № 3 (2021): 5501–7. http://dx.doi.org/10.37285/ijpsn.2021.14.3.7.
Full textAbstract:
The objective of the study was to develop silver nanoparticles loaded with Ketoprofen (Ag-KP) for increasing the drug solubility and thereby its bioavailability. Ag-KP were prepared by the solvent evaporation method using β-Cyclodextrin as a biodegradable polymer. Different formulations of Ag-KP were characterized for the drug entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), particle size analysis, X-ray diffraction studies (XRD), scanning electron microscopy (SEM) and in-vitro dissolution studies. The optimized formulation (F6) has shown an average particle size of 167.8 ± 3.46 nm,zeta potential of -23.7 ± 1.46 mV. FTIR revealed that the drug showed good excipient compatibility. XRD studies showed that the drug has changed from crystalline to amorphous state. In all formulations, F6 formulation (optimized) exhibited high drug entrapment efficiency (∼93%). SEM studies indicated the shape of Ag-KP was roughly spherical with smooth surface. In vitro dissolution studies showed that Ag-KP from F6 formulation was 94.3 ± 4.9% but for the marketed formulation, it is only 84.6 ± 3.7% in 12 hours and F6 was found to be found stable for three months at both refrigerated and room temperature (RT).
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Sharma, Deepak. "Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate for Respiratory Disorders." ISRN Pharmaceutics 2013 (July 15, 2013): 1–8. http://dx.doi.org/10.1155/2013/674507.
Full textAbstract:
Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of salbutamol sulphate for respiratory disorders for pediatrics. As precision of dosing and patient's compliance become important prerequisites for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation were undertaken with a view to develop a fast disintegrating tablet of salbutamol sulphate which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as sodium starch glycolate was optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. It was concluded that fast disintegrating tablets of salbutamol sulphate were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance.
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Sharma, Deepak, Mankaran Singh, Dinesh Kumar, and Gurmeet Singh. "Formulation Development and Evaluation of Fast Disintegrating Tablet of Cetirizine Hydrochloride: A Novel Drug Delivery for Pediatrics and Geriatrics." Journal of Pharmaceutics 2014 (February 18, 2014): 1–8. http://dx.doi.org/10.1155/2014/808167.
Full textAbstract:
Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of Cetirizine Hydrochloride for allergic and respiratory disorders. As precision of dosing and patient's compliance become important prerequisite for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation was undertaken with a view to develop a fast disintegrating tablet of Cetirizine Hydrochloride which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as Sodium Starch Glycolate were optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug excipient compatibility and accelerated stability study. It was concluded that fast disintegrating tablets of Cetirizine Hydrochloride were formulated successfully with desired characteristics which disintegrated rapidly, provide rapid onset of action, and enhance the patient convenience and compliance.
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Ovenseri, Airemwen Collins, Uwumagbe Michael Uhumwangho, Aiwaguore Johnbull Obarisiagbon, and Chioma Promise Umechukwu. "Formulation of non-effervescent floating matrix tablets of metronidazole using Abelmoschus esculentus gum as binder and 2-camphanone as sublimating agent." Journal of Phytomedicine and Therapeutics 19, no. 1 (2020): 387–97. http://dx.doi.org/10.4314/jopat.v19i1.1.
Full textAbstract:
The aim of this study was to formulate non-effervescent floating drug delivery system of metronidazole tablets using Abelmoschus esculentus (Okra) (AE) gum as a binder and 2-camphanone (camphor®) as the sublimating agent. Granules were prepared by wet granulation technique using varying concentrations of AE gum (2, 4, 6 and 8% w/w) admixed with 1%w/w acrylate methacrylate copolymer. A 30 %w/w of 2-camphanone was used as the sublimating agent. The granules were characterized for micromeritic properties. And thereafter, compressed at a compression pressure of 25 N/m2 using a Manesty single punch tableting machine. The metronidazole tablet was then sintered at 70oC for 12 h. Drug-excipient compatibility study was done using Fourier Transform Infra-red Spectroscopy (FTIR). Tablets were evaluated for floating lag time, in-vitro buoyancy and release kinetics. FTIR studies showed that the excipients and the active pharmaceutical ingredient (API) i.e. metronidazole, were compatible. All the granules were free flowing, with Carr’s index ≤ 15 %, Hausner ratio ≤ 1.18 and angle of repose of ≤ 33.5o. The tablets had hardness and friability values of 5.0-9.5 N and 0.4-0.8% respectively. The floating lag time was 0 s showing that the tablets floated immediately after immersion in the simulated gastric fluid. The maximum % release (m∞) and time to achieve it (t∞) were ≥ 88 % and ≥ 10 h, respectively. Release exponent (n) for all the formulations had values >0.45, hence their release was by non-Fickian diffusion. Non-effervescent floating matrix tablets of metronidazole were formulated using AE gum as the binder and 2-camphanone as the sublimating agent. The formulated floating tablets had increased in-vitro retention time, which indicated potential for sustained release of the drug. If well developed, this may help reduce the oral dosing frequency and encourage patient adherence to the drug therapy.
 Keywords: Non-effervescent, Abelmoschus esculentus, 2-camphanone, floating