摘要
目的:研究两种环孢素微乳化口服溶液在健康人体内的药动学及生物等效性。方法:20名健康男性志愿者按自身交叉对照设计,单剂量口服环孢素微乳化口服溶液供试制剂和参比制剂各500 mg。采用HPLC法测定不同时间点全血中环孢素的药物浓度,用DAS软件处理数据,计算主要药动学参数和相对生物利用度,评价其生物等效性。结果:供试制剂和参比制剂的cmax分别为(2.48±0.44)、(2.58±0.43)μg/mL;tmax分别为(1.80±0.60)、(2.00±0.80)h,t1/2分别为(5.04±1.20)、(5.89±1.31)h;AUC0~24 h分别为(15.48±2.42)、(15.24±2.50)μg.h.mL-1;AUC0~∞分别为(16.10±2.70)、(16.09±2.68)μg.h.mL-1;F0~24 h、F0~∞分别为(102.9±15.7)%、(101.6±18.0)%。结论:两制剂具有生物等效性。
Objective: To study the pharmacokineties and evaluate bioequivalence of two ciclosporin microemulsion oral solutions in healthy volunteers. Methods: Twenty healthy male volunteers were randomly administed with an oral single dose of 500 mg test or reference ciclosporin microemulsion oral solution in a crossover study. The whole blood was then collected from volunteers to measure concentrations of ciclosporin by HPLC method. The pharmacokinetic parameters and relative bioavailability of the microemulsion preparations were calculated by DAS 2.0 software, and the bioequivalence was evaluated. Results: The pharmacokinetie parameters of test and reference preparations were as follows: Cmax (2. 48± 0. 44) and (2.58 ± 0.43) ug/ mL, tmax(1. 80±0. 60) and (2. 00±0. 80) h, t1/2(5.04±1.20) and (5. 89±1.31) h, AUC0-24 h(15.48±2. 42) and (15.24±2.50) ug·h·mL^-1 , AUC0-∞ (16. 10±2.70) and (16.09±2.68)ug·h·mL^-1 ,respectively. Relative bioavailability F0-24 h and F0-∝ were ( 102.9 ± 15.7) % and ( 101.6 ± 18.0)%, respectively. Conclusion : The two preparations were bioequivalent.
出处
《药学服务与研究》
CAS
CSCD
2009年第2期137-139,共3页
Pharmaceutical Care and Research
关键词
环孢素
微乳
生物等效性
药代动力学
色谱法
高压液相
cielosporin
microemulsion
bioequivalence
pharmacokineties
chromatography,high pressure liquid