Formulation and evaluation of a tablet containing pioglitazone HCl microspheres

IF 0.7 Q4 PHARMACOLOGY & PHARMACY
G. Vambhurkar, A. Jagtap, A. Gavade, D. Randive, M. Bhutkar, S. Bhinge
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引用次数: 2

Abstract

Solubility is an important physicochemical factor for any drug molecule that affects its absorption along with its therapeutic effectiveness. Drug absorption is predominantly dependent upon its prompt dissolution. In the case of poorly water-soluble drugs, dissolution is the rate-limiting step in the process of drug absorption. Microspheres were prepared by solvent evaporation method using polymers namely Eudragit L100 and Eudragit RL100. Direct compression technique was used for the preparation of tablets. Tablets were prepared with MCC and PVP K-30 as polymers using an 8mm punch on a rotary press machine with a constant force. Microspheres and the prepared tablets were evaluated using various evaluation tests. The prepared microspheres showed >80% entrapment efficiency and percent yield. Batch F3 exhibited the highest drug release up to 98.30%. Fourier transform infrared (FT-IR) studies revealed no drug–polymer interaction. The results of SEM exhibited that the microspheres are spherical in shape with an average size 5µm. The result of all batches was within an acceptable limit. F2 batch tablet showed a higher drug release of 98.30% as compared with other batches. It was concluded that microcrystalline cellulose or PVP K-30, when used separately, caused retardation in drug release, whereas when used in combination (1:1) it achieved drug release in a controlled manner.
盐酸吡格列酮微球片剂的研制与评价
溶解度是任何药物分子的重要物理化学因素,影响其吸收及其治疗效果。药物吸收主要取决于其迅速溶解。对于水溶性差的药物,溶解是药物吸收过程中的限速步骤。使用聚合物即Eudragit L100和EudragitRL100通过溶剂蒸发法制备微球。采用直接压片技术制备片剂。以MCC和PVP K-30为聚合物,在旋转压力机上使用8mm冲头以恒定力制备片剂。使用各种评价测试对微球和制备的片剂进行评价。所制备的微球显示出>80%的包封率和%的产率。批次F3表现出最高的药物释放,高达98.30%。傅立叶变换红外光谱(FT-IR)研究显示没有药物-聚合物相互作用。SEM结果表明,微球呈球形,平均尺寸为5µm。所有批次的结果都在可接受的限度内。与其他批次相比,F2批次片剂的药物释放率高达98.30%。得出的结论是,微晶纤维素或PVP K-30单独使用时会导致药物释放延迟,而联合使用(1:1)时会以可控的方式实现药物释放。
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来源期刊
Journal of Reports in Pharmaceutical Sciences
Journal of Reports in Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.40
自引率
0.00%
发文量
0
期刊介绍: The Journal of Reports in Pharmaceutical Sciences(JRPS) is a biannually peer-reviewed multi-disciplinary pharmaceutical publication to serve as a means for scientific information exchange in the international pharmaceutical forum. It accepts novel findings that contribute to advancement of scientific knowledge in pharmaceutical fields that not published or under consideration for publication anywhere else for publication in JRPS as original research article. all aspects of pharmaceutical sciences consist of medicinal chemistry, molecular modeling, drug design, pharmaceutics, biopharmacy, pharmaceutical nanotechnology, pharmacognosy, natural products, pharmaceutical biotechnology, pharmacology, toxicology and clinical pharmacy.
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