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蒿甲醚控释体系制备与体外研究 |
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黄立峰 赵长文 石静
提要 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1 h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4 h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。
关键词 蒿甲醚；控释体系；固体分散体；溶出度
Preparing and in vitro Evaluating of Artemether Controlled Releasing System
Huang Lifeng, Zhao Changwen, Shi Jing
Department of Pharmacy, Fuzhou General Hospital of
Nanjing Military Command, Fuzhou 350001
Abstract 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.
Key words Artemether;Controlled releasing system;Solid dispersion;Dissolution haracteristic
蒿甲醚(Artemether,HJM)为新一代抗疟药青蒿素的衍生物，具有比青蒿素更强的抗疟活性［1］。但与其他的青蒿素类药物一样，蒿甲醚难溶于水，难于吸收，起效慢，生物利用度低，且代谢快，作用时间短，临床上服用剂量大且复燃率高。为弥补这些缺点，本文采用固体分散技术，改善蒿甲醚在载体中的分散状态，力图提高蒿甲醚的溶解速度，并且设计速释和缓释两种制剂的组合，使蒿甲醚在消化道内迅速释药达到一定浓度，并稳定释放，维持较长的作用，从而能达到较好的治疗效果，而且减少副作用和耐药性的发生。
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