芍苓消银缓释片Beagle犬体内药物动力学评价

Pharmacokinetics of paeoniflorin and astilbin after oral administration of Shaoling Xiaoyin sustained-release tablets in Beagle dogs

目的:比较Beagle犬口服芍苓消银片或其缓释片后血清芍药苷、落新妇苷的药动学差异,评价缓释制剂效果。方法:采用单剂量、两周期交叉试验,给定时间采血,HPLC法测定血清中芍药苷、落新妇苷药物浓度,DAS 2.0软件处理数据。结果:口服普通片或缓释片,芍药苷AUC_((0-t))分别为(1 029.35±26.97)μg·h·L^(-1)和(2 305.85±28.85)μg·h·L^(-1);MRT_((0-t))分别为(2.43±0.02)h和(5.99±0.04)h;t_(1/2)分别为(0.98±0.01)h和(6.85±1.38)h;落新妇苷:AUC_((0-t))分别为(2 938.92±19.03)μg·h·L^(-1)和(4 195.67±30.65)μg·h·L^(-1);MRT_((0-t))分别为(2.31±0.05)h和(6.04±0.24)h;t_(1/2)分别为(0.73±0.14)h和(9.08±3.06)h。结论:芍苓消银缓释片可显著提高芍药苷、落新妇苷的生物利用度,有效降低血药波动,提高患者顺应性。

OBJECTIVE To compare differences of paeoniflorin or astilbin pharmacokinetics between Shaoling Xiaoyin and its sustained-release tablets in Beagle dogs, and evaluate pharmaceutical effects.METHODS Three Beagle dogs respectively received conventional Shaoling Xiaoyin tablets or its sustained-release tablets, two weeks apart. The concentrations of paeoniflorin and astilbin in Beagle plasma were determined by HPLC. Then the pharmacokinetic parameters were computed by software program DAS2.0.RESULTS The main pharmacokinetic parameters of conventional Shaoling Xiaoyin tablets and sustained-release tablets were as follows：paeoniflorin：AUC（0-t）, （1 029.35±26.97） μg·h·L^-1d （2 305.85±28.85） μg·h·L^-1RT（0-t）, （2.43±0.02） h and （5.99±0.04） h; t1/2, （0.98±0.01） h and （6.85±1.38） h; astilbin：AUC（0-t）, （2 938.92±19.03） μg·h·L^-1d （4 195.67±30.65） μg·h·L^-1RT（0-t）, （2.31±0.05） h and （6.04±0.24） h; t1/2, （0.73±0.14） h and （9.08±3.06） h.CONCLUSION Shaoling Xiaoyin sustained-release tablets can obviously improve the bioavailaility of paeoniflorin and astilbin, effectively reduce undulation of blood concentration, and promote compliance of patients.