盐酸青藤碱肠溶缓释微丸的处方工艺及体外释放机制研究

Study on the Formulation and Technology of Sinomenine Hydrochloride Enteric Sustained-release Pellets and Release Mechanism in vitro

目的:研究盐酸青藤碱肠溶缓释微丸的处方工艺和体外释放机制。方法:以乙基纤维素(EC)与羟丙基甲基纤维素(HPMC)K50LV的用量比、滚圆速度、滚圆时间为考察因素,以盐酸青藤碱肠溶缓释微丸的成球性和主要时间点的释放度的综合评分为指标,采用正交试验优选处方工艺;并测定不同时间下盐酸青藤碱肠溶缓释微丸的释放度,研究释放机制。结果:优选的处方工艺为盐酸青藤碱-微晶纤维素-EC-HPMCK50LV(25∶50∶15∶10,m/m/m/m),挤出速度为50r/min,滚圆速度为800r/min,滚圆时间为9min;盐酸青藤碱肠溶缓释微丸的体外释放符合Higuchi释药模型,其释放过程为药物的扩散和HPMC溶蚀的共同作用。结论:制备的盐酸青藤碱肠溶缓释微丸有较好的肠溶缓释效果。

OBJECTIVE： To study the prescription and technology of Sinomenine hydrochloride enteric sustained-release pellets and release mechanism in vitro. METHODS： The prescription and technology of the pellets was optimized by orthogonal test with ratio of EC to HPMC KS0 LV, spheronization speed and spheronization time as factors using sphericity and release rate as index. The release rate of the pellets was determined, and its release mechanism was summarized. RESULTS： The optimized formulation and technology was as follows： sinomenine hydrochloride ：MCC ： EC ： HPMC K50 LV of 25 ： 50 ： 15 ： 10 （m/m/m/m）, extrusion speed of 50 r/rain, spheronization speed of 800 r/rain, spheronization time of 9 min. The release mechanism of pellets in vitro were in line with Higuchi model, and the process of drug release was drug diffusion and skeleton corrosion. CONCLUSIONS： The pellets show good enteric sustained-release effect.