Formulation Development and In Vitro Evaluation of Metformin Hydrochloride Matrix Tablets Based on Hydroxypropyl Methyl Cellulose

A. Kabir, Tasbira Jeseem, R. Jahangir, D. M. Rahman, A. S. Rouf
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引用次数: 4

Abstract

An attempt was to formulate the oral sustained release Metformin hydrochloride matrix tablets by using hydroxyl methyl cellulose polymer (HPMC) as rate controlling factor and to evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct compression method. The granules were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity, drug content etc. and showed satisfactory results. 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 8 hours using United States Pharmacopoeia USP 22 (paddle-type dissolution apparatus) in phosphate buffer (pH 7.4) as dissolution media. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The results indicated that 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. Besides, this study explored both of the optimum concentration and the effect of polymer on drug release pattern from the tablet matrix for 8 hours period.
羟丙基甲基纤维素基盐酸二甲双胍基质片的处方研制及体外评价
以羟甲基纤维素聚合物(HPMC)为控释因子,制备口服盐酸二甲双胍缓释片,并采用多种释放动力学模型对药物的释放参数进行评价。采用直接压片法制备。对颗粒的休止角、松散容重、疏通容重、压缩性指数、总孔隙度、药物含量等进行了评价,取得了满意的结果。对所制片剂进行了厚度、重量变化试验、药物含量、硬度、脆性和体外释放试验。体外溶出研究采用美国药典usp22(桨形溶出仪),磷酸盐缓冲液(pH 7.4)为溶出介质,溶出时间8小时。所有片剂均具有可接受的药技术性能,符合药典标准。用零阶、一阶、Higuchi、Korsmeyer和Hixson-Crowell方程对释放机制进行了探讨和解释。结果表明,随着聚合物浓度的增加,药物的释放动力学降低。体外溶出动力学模型揭示了药物释放机制的范围,从扩散控制或菲克转运到异常转运或非菲克转运,这仅取决于所使用的聚合物的类型和数量。所有病例的药物释放均遵循扩散和侵蚀机制。此外,本研究还探讨了最佳浓度以及聚合物对药物在片剂基质中8小时释放模式的影响。
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