托拉塞米胶囊与片剂在健康人体内的药动学和生物等效性

Pharmacokinetics and bioequivalence of torasemide capsules and tablets in healthy volunteers

目的:研究托拉塞米试验制剂(胶囊)和参比制剂(片剂)的人体药动学和生物等效性。方法:20名健康受试者随机交叉口服托拉塞米胶囊(试验制剂)和托拉塞米片(参比制剂),剂量均为10mg。血样加入内标(呋塞米)经预处理后采用HPLC法测定。结果:试验胶囊、参比片剂的主要药动学参数Cmax分别为(1160.1±188.0),(1271.2±326.8)μg.L-1;Tmax分别为(1.1±0.4),(1.0±0.4)h;t1/2分别为(4.1±1.0),(4.0±1.0)h;AUC0→t分别为(3662.3±782.2),(3783.2±1390.1)μg.h.L-1。以AUC0→t计算的试验胶囊的相对生物利用度为(100.6±23.9)%。结论:经方差分析及双单侧t检验结果显示,试验制剂和参比制剂具有生物等效性。

OBJECTIVE To study the pharmacokinetics and bioequivalence of torasemide test capsules and reference tablets in healthy volunteers. METHODS A single oral dose of 10mg the test or the reference preparation was given to 20 healthy volunteers in a randomized two-period crossover study. HPLC-UV was performed to detect torasemide with furosemide as the internal standard （IS）. RESULTS The main pharmacokinetic parameters of test capsules and reference tablets were as follows： Cmax were （1160. 1± 188. 0） and （1 271.2 ±326. 8）μg·L^-1 ; Tmax were （1.1±0. 4） and （1.0 ± 0. 4）h; t1/2 were （4. 1 ± 1.0） and （4. 0 ±1.0）h;AUC0→t were （3 662. 3 ± 782. 2） and （3 783.2 ±1 390. 1）μg·h·L^-1 , respectively. The relative bioavalability of the test capsules was （100. 6±23.9）%. CONCLUSION The results show that the test capsules of torasemide and the reference tabtets are bioequivalent.