洛美利嗪片剂与胶囊剂的人体生物等效性比较

Bioequivalence of lomerizine tablets vs capsules

目的:评价洛美利嗪片与参比制剂(洛美利嗪胶囊)是否生物等效。方法:男性健康受试者20名,随机分成2组,交叉口服受试制剂(洛美利嗪片)和参比制剂各40 mg,用高效液相色谱紫外检测法测定人血清中洛美利嗪浓度,所得数据经BECS软件处理得到主要药动学参数。结果:洛美利嗪片与参比制剂洛美利嗪胶囊的t_(max)分别为:(2．7±s 0．3)h和(2．6±0-3)h,c_(max)分别为:(93±11)μg·L^(-1)和(90±11)μg·L^(-1),用梯形法计算所得的AUC_(0-t)分别为(435±71)μg·h·L^(-1)和(432±77)μg·h·L^(-1)。对经对数转换后的c_(max),AUC_(0-t),进行方差分析和双单侧t检验及90％可信限判断,洛美利嗪片的c_(max)落在参比制剂的963％～11 1．7％范围内,AUC_(0-T)落在参比制剂的91．7％～110．6％范围内,t_(max)经非参数检验法检验无显著差异,洛美利嗪片AUC_(0-t) 的相对生物利用度为(101±12)％。结论:2种制剂具有生物等效性。

AIM： To evaluate the bioequivalence of lomerizine tablets and capsules. METHODS： A total of 20 healthy male volunteers were divided randomly into two groups,administering with two preparations of lomerizine respectively in an open randomized two cross-over test. A single oral dose of the test and reference preparation was 40 mg for each alternatively. Lomerizine concentrations in the serum were determind by high perfermance liquid chromatography,and the pharmacokinetic parameters of lomerizine were obtained by using BECS software. RESULTS： Lomerizine parameters of the tablets and the reference preparation were obtained, tmax：（2.7 ±s 0.3） h vs（2.6 ± 0.3） h; cmax： （93 ± 11）μg·L^-1 us （90 ± 11）μg·L^-1, AUG0-1 （435 ± 71）μg·h·L^-1 vs （432 ± 77） μg·h·L^-1. The results of statistical analysis showed that there was no significant differences between cmax,A UC0-1 and tmax of the two preparations.The relative bioavailability of lomerizine tablets was （ 101 ± 12） %. CONCLUSION： The lomerizine tablets and capsules were bioequivalent.