摘要
目的测定雷公藤甲素的表观油水分配系数,通过大鼠肠灌流实验印证其在体内吸收情况的预测。方法采用摇瓶法测定雷公藤甲素的表观油水分配系数,采用大鼠在体肠灌流实验对雷公藤甲素在各肠段的吸收特性进行研究。结果在正辛醇-水体系中,雷公藤甲素的表观油水分配系数logP=0.58,在正辛醇-缓冲液中分配系数受溶液的pH值影响不大。雷公藤甲素在大鼠肠道内有较好的肠吸收,各肠段的有效渗透系数(P*eff)和10cm肠段吸收百分比(10cm%ABS)之间无显著性差异(P>0.05)。结论应用摇瓶法能准确测定雷公藤甲素的表观油水分配系数,由此推测的体内吸收情况通过大鼠肠灌流实验得到印证。
OBJECTIVE To determine the apparent oil/water partition coefficient oftriptolide and to investigate its absorption by in situ perfused rat intestinal model. METHODS A shake flask method was established to determine n-octanol/water partition coefficient of triptolide; the intestine absorption characters were detected by the in situ perfused rat intestinal model. RESULTS The log P of triptolide in octanol/water system was 0.58 and the pH of buffer solution had no influence on its distribution coefficient. Triptolide was well absorbed in general intestinal tract and the Peff and 10 cm%ABS had no significant difference (P〉0.05) among four different regions of rat intestine. CONCLUSION The shake flask method can be used to determine the apparent oil/water partition coefficient of triptolide accurately and the prediction of its intracorporal absorption has been proved by in situ perfused rat intestinal model.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第20期1560-1563,共4页
Chinese Pharmaceutical Journal
基金
中医药行业科研专项(200707008)
关键词
雷公藤甲素
表观油水分配系数
在体肠灌流模型
吸收
triptolide
apparent oil/water partition coefficient
in situ perfused rat intestinal model
absorption