米诺环素亲水凝胶型缓释骨架片的制备及体外释放度考察

Preparation and Release of Minocycline Hydrophilic Gel Sustained-release Matrix Tablets

目的:制备米诺环素亲水凝胶型缓释骨架片并考察其体外释放度。方法:采用粉末直接压片工艺制备缓释片;采用紫外分光光度法测定其释放度,同时考察羟丙基甲基纤维素(HPMC)的不同规格、用量以及不同释药条件对药物释放速率的影响。结果:所制制剂为黄色片剂,检查项符合2005年版《中国药典》中的相关规定。试验确定了以HPMCK100为缓释骨架材料,处方用量为32%;不同释放介质与释放装置对药物的释放均有显著影响。释放规律符合Higuchi方程。结论:该制剂处方工艺简单,体外释放度测定方法准确易行,制剂具有明显的缓释效果。

OBJECTIVE： To prepare Minocycline Hydrophilic Sustained release Matrix Tablets（MHSMT） and determine their release rate in vitro. METHODS： MHSMT were prepared by direct compression process and the drug release was determined by ultraviolet spectrophotometry. The effects of different specification and amount of HPMC and different releasing conditions on drug release from the matrix tablets were observed. RESULTS： The preparation was yellow tablets with its property up to the standard specified in Chinese Pharmacopeia （2005 edition）. 32% HPMC K100 was proved to be the optimal sustained - release matrix material. Different release media and the releaser had significant effects on drug release. The release behavior was in line with Higuchi equation. CONCLUSIONS： This preparation process of the tablets is simple, and the method for the determination of drug release is accurate and feasible. The tablets had remarkable sustained - release property in vitro.