何洁英,王汝上
HE Jieying,WANG Rushang

• 1:佛山市第一人民医院中山大学附属佛山医院
• 2:广州康臣药物研究有限公司

摘要(Abstract)：

目的研究毛蕊异黄酮葡萄糖苷自微乳在大鼠体内的药代动力学及对大鼠肠吸收的作用。方法单剂量给予大鼠毛蕊异黄酮葡萄糖苷自微乳及毛蕊异黄酮葡萄糖苷混悬液,采用高效液相色谱(HPLC)法测定血浆中毛蕊异黄酮葡萄糖苷质量浓度,运用DAS2.1.1程序拟合药物浓度-时间曲线,计算药代动力学参数及生物利用度;以离体大鼠外翻肠囊模型研究毛蕊异黄酮葡萄糖苷自微乳的肠吸收部位和促进吸收效果,HPLC法测定毛蕊异黄酮葡萄糖苷浓度并计算累积吸收率。结果毛蕊异黄酮葡萄糖苷自微乳和混悬液的tmax分别为0.83 h及1.0 h,cmax分别为2.046 mg·L~(-1)及1.232 mg·L~(-1),AUC0-24h分别为3.063mg·h·L~(-1)及2.157 mg·h·L~(-1),毛蕊异黄酮葡萄糖苷自微乳相对于混悬液的生物利用度为142.0%;自微乳的吸收率明显高于混悬液,各肠段吸收率比较:回肠>空肠>十二指肠>结肠。结论与毛蕊异黄酮葡萄糖苷混悬液相比,毛蕊异黄酮葡萄糖苷自微乳能显著提高毛蕊异黄酮葡萄糖苷在大鼠体内的生物利用度并改善肠吸收。
OBJECTIVE To study the pharmacokinetics of Calycosin-7-glucoside microemulsion in rats and its effect on intestinal absorption. METHODS Rat Calycosin-7-glucoside microemulsion and Calycosin-7-glucoside suspension were administered by single dose. Plasma concentration of Calycosin-7-glucoside was determined by HPLC. DAS2. 1. 1 procedure was used to fit the drug concentration-time curve,The pharmacokinetic parameters and bioavailability were calculated. Calycosin-7-glucoside was used to determine the intestinal absorption site of self-microemulsion and promote the absorption effect. The concentration of Calycosin-7-glucoside was determined by HPLC,and calculate the absorptivity. RESULTS tmaxof Campanulin self-microemulsion and suspension were 0.83 h and 1.0 h,cmaxwere 2.046 mg·L~(-1) and 1.232 mg·L~(-1),AUC0-24 hwere 3.063 mg·h·L~(-1) and 2.157 mg·h·L~(-1),respectively. The bioavailability of Campanulin self-microemulsion relative to Campanulin suspension was 142.0%. The absorption rate of microemulsion was significantly higher than that of suspension,and the absorption rate of each intestine was: ileum > jejunum > duodenum > colon.CONCLUSION With Calycosin-7-glucoside suspension liquid ratio,Calycosin-7-glucoside from microemulsion can significantly improve Calycosin-7-glucoside in rats in vivo bioavailability and improve the intestinal absorption.

关键词(KeyWords)： 毛蕊异黄酮葡萄糖苷;自微乳;药代动力学;生物利用度;肠吸收
calycosin-7-glucoside;self-microemulsion;pharmacokinetics;bioavailability;intestinal absorption

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 何洁英,王汝上
HE Jieying,WANG Rushang

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