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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 study the influence of Wuzhi capsule on the pharmacokinetics of indinavir (IDV). Methods: The experimental animals were Beagle dogs. In this experiment, self-control method was used. Six beagle dogs were given indinavir sulfate tablets and five consecutively to five ester capsules and then indinavir sulfate tablets were divided into single-use indene Denaturation group and five ester capsule group. Administration (indinavir sulphate tablets) before fasting can not help but water 12 h, before administration and after administration according to the set point in the beagle dog forelimb venous blood 800μl, the plasma was separated, the plasma was extracted with ethyl acetate 2 Times, the supernatant was combined, dried under nitrogen, reconstituted, and the concentration of indinavir in Beagle dog’s plasma was determined by LC / MS / MS. Results: The linear range of IDV in Beagle dog plasma was 20 ~ 10 000 μg / L, the linearity was good (r> 0.99), and the lowest limit of quantification was 20 μg / L. The pharmacokinetic parameters of indinavir sulphate tablets were compared with those of indinavir sulphate tablets and continuous administration of pentaprylcapsules. After continuous administration of penta ester capsules for 7 days, There was a significant increase in AUC0-t and Cm ax for darunavir. Conclusion: The method is sensitive and specific and suitable for the detection of plasma samples. The results show that the five ester capsules affect the pharmacokinetics of indinavir in Beagle dogs.