甲硝唑微丸制备工艺及乙基纤维素包衣对其性质的影响

目的]建立甲硝唑包衣微丸制备工艺并筛选包衣液处方.方法]用离心包衣造粒法制备甲硝唑淀粉微丸,观察不同上药方法对甲硝唑微丸上药量的影响以及乙基纤维素包衣对EudragitS100包衣微丸药物释放速度的影响.结果]溶液上药法及粉末上药法的甲硝唑回收率分别为98%±1%,95%±2%,而过筛混合法的甲硝唑回收率为70%±5%.溶液上药法和过筛混合法制备的甲硝唑微丸的载药量较高.随着乙基纤维素包衣质量百分比的提高,甲硝唑自EudragitS100包衣微丸中的释放速率呈明显减慢的趋势.结论]建立采用离心包衣造粒法制备甲硝唑微丸的工艺.

Effects of preparation method and ethyl cellulose coating on the characteristics of metronidazole pellets

OBJECTIVETo establish the coating formulation of metronidazole pellets and screen the (preparation) method.METHODSMetronidazole pellets were prepared by centrifugal granulation method, and the effects of different drug loading method on the loading percentage of metronidazole were observed. And the (effect) of ethyl cellulose coating on the release of metronidazole from the pellets coated with Eudragit S100 was also discussed.RESULTSThe entrapment ratio of metronidazole by solution added, powder added and sieve mixing were 98%±1%, 95%±2% and 70%±5%, respectively. The loading efficiency of metronidazole were little higher prepared by solution added and sieve mixing method. The release of metronidazole from coated (pellets) was reduced apparently when the amount of ethyl cellulose coating increased.CONCLUSIONThe method of preparing metronidazole pellets and formulation of coating solution were preliminary established.