单剂量口服芍药苷微乳在大鼠体内的药动学研究

Pharmacokinetic study of paeoniflorin microemulsions in rats after a single oral administration

目的研究大鼠口服芍药苷微乳后芍药苷在大鼠体内的药动学特征,评价芍药苷微乳的相对生物利用度。方法将12只SD大鼠随机分成芍药苷微乳实验组和芍药苷混悬液对照组,运用高效液相色谱法测定不同时间点血浆中芍药苷的质量浓度,计算药动学参数和相对生物利用度。结果经口服给予芍药苷微乳和混悬液后,其t_(1/2)分别为(3.71±1.08)h和(2.36±0.17)h,ρmax分别为(11.20±0.89)mg·L^(-1)和(7.61±0.48)mg·L^(-1),AUC_(0-∞)分别为(40.56±4.33)mg·h·L^(-1)和(22.78±1.25)mg·h·L^(-1),统计分析结果表明,芍药苷微乳与芍药苷混悬液的t_(1/2)、ρmax、AUC_(0-∞)、CL、MRT之间均有显著性差异。结论与芍药苷混悬液对比,芍药苷微乳能够显著提高芍药苷在大鼠体内的生物利用度。

Objective To determine the pharmacokinetic parameters of paeoniflorin microemulsions and paeoniflorin suspensions after oral administration in rats and to evaluate the relative bioavailability of paeoniflorin microemulsions.Methods Twelve SD rats were randomly divided into control group with paeoniflorin suspensions and experimental group with paeoniflorin microemulsions.Plasma concentrations of paeoniflorin in rats were assayed using HPLC method.The pharmacokinetic parameters and relative bioavailability were calculated.Results The main parameters of paeoniflorin microemulsions and paeoniflorin suspensions:t1/2 were(3.71±1.08)h and(2.36±0.17)h,respectively;ρmax were(11.20±0.89)mg·L-1 and(7.61±0.48)mg·L-1 respectively;AUC0-∞were(40.56±4.33)mg·h·L-1 and(22.78±1.25)mg·h·L-1 respectively.There were statistically significant differences in pharmacokinetic parameters of paeoniflorin including the t1/2,ρmax,AUC0-∞,CL and MRT among the oral administration of paeoniflorin microemulsions and paeoniflorin suspensions in rats.Conclusions The paeoniflorin microemulsions improves the bioavailability of paeoniflorin in rats significantly compared with that of paeoniflorin suspensions.