氯唑西林片剂与胶囊剂的人体生物等效性

目的评价氯唑西林片剂与胶囊剂在人体内的生物等效性。方法20名健康男性受试者随机交叉给药,单剂量口服500 mg受试制剂氯唑西林片和参比制剂氯唑西林钠胶囊,采用反相高效液相色谱法测定氯唑西林的血药浓度,用3P97软件进行药动学参数计算和生物等效性评价。结果受试制剂和参比制剂的主要药动学参数:t_(1/2)分别为(1.3±s 0.3)和(1.21±0.26)h,c_(max)分别为(14±4)和(15±4) mg·L~(-1),t_(max)分别为(0.73±0.26)和(0.74±0.17)h,AUC_(0～t)分别为(23±5)和(24±6)mg·h·L~(-1),AUC_(0～∞)分别为(23±5)和(25±6)mg·h·L~(-1),经方差分析和双单侧t检验显示,主要药动学参数无显著差异;受试制剂的相对生物利用度为(98±27)%。结论2种氯唑西林制剂具有生物等效性。

Bioequivalence of cloxacillin tablets and capsules in healthy volunteers

AIM To evaluate the bioequivalence of the tablets (test preparation) and capsules(reference preparation) of cloxacillin in human body.METHODS A randomized two-period crossover study of 20 healthy male volunteers was taken with two kinds of 500 mg cloxacillin formulation already mentioned orally for each individual and their blood concentrations in vivo were conducted.The main pharmacokinetic parameters (AUC, c_(max) and t_(max)) and bioequivalence effects were evaluated using 3P97 software program.RESULTS The main pharmacokinetic parameters of the tested and referenced groups including t_(1/2),c_(max),AUC_(0-t),AUC_(0-∞)were (1.3±s 0.3) vs (1.21±0.26) h;(14±4) vs (15±4) mg·L~(-1);(23±5) vs (24±6) mg·h·L~(-1);(23±5) vs (25±6) mg·h·L~(-1),respectively,showing no significant differences between the two groups by analysis variance and two one-side t-tests.The relative bioavailability of the tested group was (98±27)%.CONCLUSION The cloxacillin tablets and capsules are bioequivalent.