巴戟甲素在模拟人体胃肠环境中稳定性试验

Stability of Bajijiasu in Simulated Conditions of Human Stomach and Intestines

目的测定巴戟甲素在模拟人体胃肠环境中的稳定性,为口服剂型的选择提供依据。方法采用HPLC-ELSD法,分别测定巴戟甲素在稀盐酸溶液和人工胃液中2 h以及在pH 6.8磷酸盐缓冲液及人工肠液中12 h的稳定性。结果在稀盐酸溶液和人工胃液中温育30 min后,巴戟甲素在两液中只剩下加入量的67.59%和64.85%,120 min后在稀盐酸溶液和人工胃液中分别为加入量的43.31%和50.41%;加入pH 6.8磷酸盐缓冲液及人工肠液中12 h后,巴戟甲素分别为加入量的90.43%和90.65%。结论巴戟甲素具有在稀盐酸溶液和人工胃液中均不稳定、在pH 6.8磷酸盐缓冲液和人工肠液中稳定性较好的特点,在设计口服给药剂型时应予以重视。

Objective To investigate the stability of Bajijiasu in simulated conditions of human stomach and instestines, which will provide evidence for the design of oral form design. Methods We examined the stability of Bajijiasu in the dilute hydrochloric acid solution for 2 hours, in artificial gastric juice for 2 hours, in buffer phosphate （pH being 6.8） for 12 hours and in artificial intestinal juice for 12 hours with HPLC-ELSD. Results The content of Bajijiasu remained 67.59 % in dilute hydrochloric acid solution and remained 64.85 % in artificial gastric juice after incubation for 30 minutes, and decreased to 43.31% and 50.41%, respectively after incubation for 120 minutes. Af- ter incubation for 12 hours in buffer phosphate （pH being 6.8） and in artificial intestinal juice, the content of Bajijiasu remained 90.43 % and 90.65 %, respectively. Conclusion It is indicated that Bajijiasu is unstable in dilute hydrochloric acid solution and in artificial gastric juice, but stable in buffer phosphate （pH being 6.8） and in artificial intestinal juice. So the effect of human body gastric juice should be taken into account for the design of oral form of Bajijiasu.