异烟肼缓释植入剂的制备和体外释放

Preparation of isoniazid sustained release implant and the release behavior in vitro

目的:探讨异烟肼缓释植入剂的制备工艺和体外释放特性。方法:选用最佳处方,采用压模成型法制备。建立异烟肼植入剂的释放度检测方法,用不同方程拟合不同时间段异烟肼植入剂的释放曲线。结果:25%的载药量,以丙酮做溶剂制备的植入剂在80d后,累积释药量达85%以上;最初10d的释放量较大,之后变平稳,Mt/M∞t的相关性良好(r=0.9924,P=0.000)。结论:选用最佳处方制备的植入剂具有良好的缓释效果。

OBJECHVE To prepare isoniazid （INH） implant and evaluate the release behavior in vitro. METHODS Compression molding forming was used to prepare the INH implant, of which prescription was screened; A method of determining INH release from the preparation in vitro was established, and different equations were used to fit the release profiles of INH implant. RESULTS The accumulative release percentage of INH from the implant within 80 d were more than 85%, which was prepared by 25% drug loading and acetone. The release quantities of the implant were greater in first 10 days, and then kept steady. The correlation of accumulative release quantities（Mt/M∞ ） in vitro with release time（t） was good（r = 0. 992 4,P = 0. （100）. CONCLUSION The implant prepared by the best prescription have a better sustained release behavior.