奥昔布宁渗透泵控释片在犬体内的单剂量和多剂量生物等效性研究

 目的研究自制奥昔布宁渗透泵控释片与市售普通片以及进口控释片在犬体内的单剂量和多剂量生物等效性。方法利用液相-质谱检测血药浓度,采用随机、交叉实验设计对自制控释片、进口控释片和市售普通片进行对照研究。结果单剂量给药后奥昔布宁自制控释片、进口控释片和市售普通片的峰浓度(ρ_max)、达峰时间(t_max)、血药浓度曲线下面积AUC分别为:(1.77±0.51),(1.67±0.27)和(5.89±2.04)μg·L^-1,(10.00±2.14),(10.50±2.07)和(0.84±0.23)h,(50.69±11.83),(48.63±6.33)和(22.74±7.06)μg·h·L^-1。多剂量给药后分别为:(2.39±0.55),(2.07±0.41)和(7.80±1.56)μg·L^-1,(6.12±1.55),(8.12±1.88)和(0.62±0.19)h,(44.92±10.63),(41.50±9.05)和(21.92±4.37)μg·h·L^-1,达稳态时血药浓度波动系数(DF)分别为(0.76±0.17),(0.52±0.17)和(2.55±0.39)。结论经方差分析和双单侧t检验,自制片与进口片和普通片生物等效。

Syudy on Bioequivalence of Oxybutynin Osmotic Pump Tablets in 8 Dogs After a Single and Multiple Oral Administration

OBJECTIVE To study the bioequivalence of self-prepared osmotic pump tablets(OPT),imported OPT and immediate-release(IR) tablets of oxybutynin in dogs.METHODS LC-MS method was developed to detect the plasma drug concentration in 9 dogs.Two one-sided t-test and analysis of variance were performed to evaluate the bioequivalence of the formulations.RESULTS The pharmacokinetic parameters of self-prepared OPT,imported OPT and IR were listed as follows for single-dose study: ρ_max were(1.77±0.51),(1.67±0.27) and(5.89±2.04)μg·L^{-1,tmax were(10.00±2.14),(10.50±2.07) and(0.84±0.23)h,AUC were(50.69±11.83),(48.63±6.33) and(22.74±7.06)μg·h·L-1,respectively.The pharmacokinetic parameters were as follows for multiple-dose study:ρ_max were(2.39±0.55),(2.07±0.41) and(7.80±1.56)μg·L-1,t_max were(6.12±1.55),(8.12±1.88) and(0.62±0.19)h,AUC were(44.92±10.63),(41.50±9.05) and(21.92±4.37)μg·h·L-1,DF were(0.76±0.17),(0.52±0.17) and(2.55±0.39),respectively.CONCLUSION The results showed that two preparations were bioequivalent.}