论文部分内容阅读
目的比较胆固醇和β-谷甾醇作为囊材制备的盐酸小檗碱囊泡的特性和体外释药差异。方法采用薄膜蒸发法用2种囊材分别制备盐酸小檗碱囊泡,光学显微镜观察比较囊泡形态,微粒分析仪评价囊泡粒径分布差异;采用HPLC测定盐酸小檗碱囊泡包封率和载药量,比较2种囊泡的体外释放情况,并考察温度对囊泡稳定性的影响。结果镜下观察2种囊材制备的囊泡圆整度均较好,粒径分布范围比较相似;用胆固醇和β-谷甾醇制备的囊泡包封率分别为28.5%和25.21%,载药量分别为1.32%和1.26%;体外释放试验中,在人工肠液和人工胃液中的胆固醇囊泡12 h累积释放百分率在50%左右,而β-谷甾醇囊泡的累积释放百分率>70%;40℃以下放置8 h,温度对2种小檗碱囊泡的包封率影响较小,当温度高于40℃时,2种小檗碱囊泡的包封率均显著降低。结论用薄膜分散法制备的2种小檗碱囊泡镜下形态相似,包封率近似;用β-谷甾醇制备的囊泡释药快,释药量多;40℃以下放置稳定性均较好。β-谷甾醇作为载体材料制备囊泡具有可行性。
OBJECTIVE To compare the characteristics of in vitro release of berberine hydrochloride vesicles prepared from cholesterol and β-sitosterol as capsular material. Methods The vesicles of berberine hydrochloride were prepared by thin-film evaporation method. The morphology of vesicles was observed by light microscope. The particle size distribution was evaluated by particle analyzer. The encapsulation efficiency of berberine hydrochloride vesicles And drug loading were compared in vitro release of two kinds of vesicles, and investigate the temperature on the vesicle stability. Results Microscope showed that the vesicle roundness of the two kinds of capsules was better and the distribution of particle size was similar. The encapsulation efficiency of vesicles prepared with cholesterol and β-sitosterol were 28.5% and 25.21% In the in vitro release test, the cumulative release percentage of cholesterol vesicles in artificial intestinal juice and artificial gastric juice was about 50% in 12 h, while the cumulative release percentage of β-sitosterol vesicles was> 70%. Under the temperature below 40 ℃ for 8 h, the entrapment efficiency of two berberine vesicles was less affected by the temperature. When the temperature was above 40 ℃, the entrapment efficiency of two berberine vesicles decreased significantly. Conclusions The two kinds of berberine vesicles prepared by thin-film dispersion method have the similar morphology and the similar encapsulation efficiency. The vesicles prepared with β-sitosterol release fast and the release amount is large. The stability under 40 ℃ it is good. It is feasible to prepare vesicles with β-sitosterol as a carrier material.