托拉塞米胶囊与注射剂在健康人体内的药动学和生物等效性研究

摘要

Objective To study the pharmacokinetics and bioequivalence of torasemide capsules and injection in healthy volunteers.Methods A single oral dose of 10 mg of torasemide capsules or injection was given to 24healthy volunteers in a randomized two-period crossover study.high-performance liquid chromatography (HPLC) was performed to detect torasemide.Results The main pharmacokinetic parameters of torasemide capsules and injection were as follows:peak concentration(Cmax)was (1123 ± 104) and (1362 ±258) μg/L; peak time(tmax)was (1.2 ±0.3) and (1.0 ±0.3)h;t1/2 was (4.1 ±1.0) and (4.0±1.0)h; area under concentration-time curve(AUC)0-twas (3583 ±365)and (3844 ±362) μg/(h · L) ;AUC0-∞ was (3838 ±482)and (3999 ±463) μg/(h · L).The relative bioavailability of capsules was (97.0 ± 20.5) ％.Conclusion Torasemide capsules and injection are bioequivalent in healthy volunteers.%目的 研究托拉塞米胶囊和注射剂在健康人体内的药动学和生物等效性.方法 24名健康受试者随机交叉口服托拉塞米胶囊和注射托拉塞米注射液,剂量均为10 mg.血样经预处理后采用高效液相色谱(HPLC)法测定.结果 试验胶囊、注射液的Cmax分别为(1123±104),(1362±258) μg/L；tmax分别为(1.2±0.3),(1.0±0.3)h；t1/2分别为(4.1±1.0),(4.0±1.0)h；AUC0-t分别为(3583±365),(3844±361)μg/(h·L)；AUC0-∞分别为(3838±482)、(3999±463) μg/(h·L)；不同剂型之间差异均无统计学意义(P＞0.05).以AUC0-t计算的试验胶囊的相对生物利用度为(97.0±0.5)％.结论 托拉塞米胶囊和注射剂在健康人体内具有生物等效性.