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双氯芬酸钠与硫酸软骨素的基质型控释片的设计与评价

Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulphate.

作者信息

Avachat Amelia, Kotwal Vikram

机构信息

Department of Pharmaceutics, Sinhgad College of Pharmacy, Vadgaon (Budruk), Pune - 411041, India.

出版信息

AAPS PharmSciTech. 2007 Oct 19;8(4):E88. doi: 10.1208/pt0804088.

Abstract

The purpose of the present study was to develop and characterize an oral controlled release drug delivery system for concomitant administration of diclofenac sodium (DS) and chondroitin sulfate (CS). A hydrophilic matrix-based tablet using different concentrations of hydroxypropylmethylcellulose (HPMC) was developed using wet granulation technique to contain 100 mg of DS and 400 mg of CS. Formulations prepared were evaluated for the release of DS and CS over a period of 9 hours in pH 6.8 phosphate buffer using United States Pharmacopeia (USP) type II dissolution apparatus. Along with usual physical properties, the dynamics of water uptake and erosion degree of tablet were also investigated. The in vitro drug release study revealed that HPMC K100CR at a concentration of 40% of the dosage form weight was able to control the simultaneous release of both DS and CS for 9 hours. The release of DS matched with the marketed CR tablet of DS with similarity factor (f(2)) above 50. Water uptake and erosion study of tablets indicated that swelling followed by erosion could be the mechanism of drug release. The in vitro release data of CS and DS followed Korsmeyer-Peppas and zero-order kinetics, respectively. In conclusion, the in vitro release profile and the mathematical models indicate that release of CS and DS can be effectively controlled from a single tablet using HPMC matrix system.

摘要

本研究的目的是开发并表征一种用于双氯芬酸钠(DS)和硫酸软骨素(CS)联合给药的口服控释药物递送系统。采用湿法制粒技术,以不同浓度的羟丙基甲基纤维素(HPMC)制备了一种亲水性基质片剂,该片剂含有100 mg的DS和400 mg的CS。使用美国药典(USP)II型溶出装置,在pH 6.8的磷酸盐缓冲液中,对所制备的制剂在9小时内的DS和CS释放情况进行了评估。除了常规的物理性质外,还研究了片剂的吸水动力学和溶蚀程度。体外药物释放研究表明,浓度为剂型重量40%的HPMC K100CR能够控制DS和CS同时释放9小时。DS的释放与市售的DS控释片相匹配,相似因子(f(2))高于50。片剂的吸水和溶蚀研究表明,溶胀后溶蚀可能是药物释放的机制。CS和DS的体外释放数据分别符合Korsmeyer-Peppas模型和零级动力学。总之,体外释放曲线和数学模型表明,使用HPMC基质系统可以有效地从单片制剂中控制CS和DS的释放。

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