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双氯芬酸钠缓释片制剂的制备及体外评价

Preparation and in vitro evaluation of sustained release tablet formulations of diclofenac sodium.

作者信息

Savaşer Ayhan, Ozkan Yalçin, Işimer Aşkin

机构信息

Department of Pharmaceutical Technology, Gülhane Military Medical Academy, Etlik, 06018 Ankara, Turkey.

出版信息

Farmaco. 2005 Feb;60(2):171-7. doi: 10.1016/j.farmac.2004.10.001. Epub 2005 Jan 7.

Abstract

The effects of formulation variables on the release profile of diclofenac sodium (DS) from hydroxypropylmethyl cellulose (HPMC) and chitosan matrix tablets were studied. DS tablets were prepared by wet granulation and direct compression methods and different ratios of HPMC and chitosan were used. Physical properties of the prepared tablets and targeted commercial sustained release (SR) tablet and the drug release were studied in tablets that were placed in 0.1 M HCl for 1 h and phosphate buffer solution was added to reach pH value of 7.5. In vitro studies showed that 20% HPMC contained SR formulation with direct (dry) compression method is the optimum formulation due to its better targeting profile in terms of release. This formulation also exhibited the best-fitted formulation into the zero order kinetics. The precision and accuracy of the analytical method were also checked. The repeatability and reproducibility of the method were also determined.

摘要

研究了制剂变量对双氯芬酸钠(DS)从羟丙基甲基纤维素(HPMC)和壳聚糖基质片剂中释放曲线的影响。采用湿法制粒和直接压片法制备DS片剂,并使用不同比例的HPMC和壳聚糖。在将片剂置于0.1 M盐酸中1小时后加入磷酸盐缓冲溶液以达到pH值7.5的条件下,研究了所制备片剂以及目标商业缓释(SR)片剂的物理性质和药物释放情况。体外研究表明,采用直接(干)压片法的含20% HPMC的SR制剂是最佳制剂,因为其在释放方面具有更好的靶向性。该制剂在零级动力学方面也表现出最佳拟合。还检查了分析方法的精密度和准确度。同时也测定了该方法的重复性和重现性。

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