五酯胶囊对茚地那韦在比格犬体内药代动力学的影响

Effects of Wuzhi capsule on pharmacokinetics of indinavir

目的：研究五酯胶囊对茚地那韦（IDV）药代动力学影响。方法：实验动物为比格犬,本实验采用自身对照法,6只比格犬按单给硫酸茚地那韦片和连续给五酯胶囊后再给硫酸茚地那韦片分为单用茚地那韦组和五酯胶囊组。给药（硫酸茚地那韦片）前禁食不禁水12 h,给药前及给药后按设定时间点于比格犬前肢静脉采血800μl,分离出血浆,血浆经乙酸乙酯萃取2次,合并上清,氮气吹干,复溶,使用LC/MS/MS法检测比格犬血浆中茚地那韦浓度。结果：IDV在比格犬血浆中的药物浓度线性范围为20～10 000μg/L,线性关系良好（r〉0.99）,最低定量限为20μg/L。比较单用硫酸茚地那韦片和连续给药五酯胶囊后给药硫酸茚地那韦片的药代动力学参数,连续给药五酯胶囊7 d后给药茚地那韦片时茚地那韦的AUC0-t及Cm ax均有显著性提高。结论：本方法灵敏度高,特异性好,适用于血浆样品检测。结果显示五酯胶囊会影响茚地那韦在比格犬体内药代动力学过程。

Objective： To investigate effects of Wuzhi capsule on pharmacokinetics of indinavir（IDV）. Methods： Selfcontrol method was used, Six beagles were given peroral indinavir sulfate tablet （ IDV 400 mg） before and after WZ po for successive 7 days. The concentration of IDV in beagle＇s plasma was measured by LC/MS/MS. Results： The concentration curve of IDV in plasma was linear in the range of 20 - 10 000 μg/L（ r 〉 0.99 ）, the lowest limit of quantitation being 20 μg/L. AUC0.4 and Cmax of IDV were varied significantly before and after administration of WZ. Conclusions： The method is simple, rapid, sensitive, reliable and is applicable to assay IDV in plasma. The results showed that there are interactions between Wuzhi capsule and indinavir.