蒿甲醚控释体系制备与体外研究

Preparing and in vitro Evaluating of Artemether Controlled Releasing System

为提高蒿甲醚的生物利用度，达到迅速和持久释药的双重目的，采用溶剂法制成速释和缓释两种固体分散体，差热分析鉴别药物在载体中的存在状态，并以体外溶出度试验选择载体及其与药物的配比，将蒿甲醚制成控释体系。结果：在体外溶出度试验中控释体系在１ｈ内即达到较高浓度，并以溶液形式释放蒿甲醚３７．０４％。在之后的４ｈ内能保持这个浓度，最终的累积释放率为９１．８６％。提示该控释体系具备临床上所需的迅速和持久的释药功能。

Objective: To make a kind of system which can release the drug quickly and for long time by oral to improve the bioavailability of artemether. Method: Use the solvent-coevaporation method to prepare two kinds of artemether solid dispersions, one for fast-releasing and one for slowlyreleasing and then determin whether the crystal of artemether existed in carriers by differential thermal analysis. Systems are formed by mixing the fast-releasing and slowly-releasing solid dispersion in some proportions. From the comparation of the dissolution haracteristic in vitro of these systems, the artemether's controlled releasing system was selected. Result: There wasn't the crystal of artemether in carriers. The results of dissolution in vitro showed the selected system released artemether quickly in an hour and with higher and stable concentration within the following 4 hours. Conclusion: The system greatly improved the releasing of artemether, compared with the ordinary preparation of artemether.