阿奇霉素胶囊的人体生物等效性研究

目的:研究2种阿奇霉素胶囊在健康人体内的药动学,并评价其生物等效性。方法:采用随机、双交叉自身对照试验设计,19名健康受试者单剂量口服阿奇霉素胶囊受试制剂与参比制剂500mg,服药后0～144h间隔取血,用液-质联用法测定阿奇霉素在血浆中的浓度,采用DAS2.0.1药动学软件计算药动学参数并进行生物等效性评价。结果:参比制剂与受试制剂的tmax分别为(2.658±0.914)、(2.816±1.193)h,Cmax分别为(248.579±89.395)、(236.737±62.668)ng·mL-1,AUC0～144分别为(3121.862±750.631)、(3006.864±784.840)ng.h.mL-1,AUC0～∞分别为(3446.478±834.751)、(3484.274±968.909)ng.h.mL-1。受试制剂的相对生物利用度为(99.2±26.7)%。结论:2种制剂生物等效。

Bioequivalence of Azithromycin Capsules in Healthy Volunteers

OBJECTIVE： To study the pharmacokinetics and evaluate the bioequivalence of azithromycin capsules in healthy volunteers. METHODS： By a randomized cross-over controlled trial design, the test vs. reference azithromycin capsules at the single oral dose of 500 rag were given to 19 healthy volunteers. Blood samples were collected at 0--144 h. The plasma concentration of azithromycin was analyzed by LC - MS. The pharmacokinetic parameters were computed using DAS2.0.1 pharmacokinetic software and the bioavailability of the capsules was evaluated. RESULTS： The main pharmacokinetic parameters of the reference vs. the test formulations were as follows： tmax（2.658± 0.914） h vs.（2.816± 1.193） h; Cmax （248.579± 89.395） ng mL 1 vs. （ 236. 737 ± 62.668） ng·mL^-1; AUC0 - 144（ 3 121.862± 750.631 ）ng·h·mL^-1 vs. （3 006.864± 784.840）ng·h·mL^-1. AUC0-∞ （3 446.478±834.751） ng·h·mL^-1 vs. （3 484.274± 968.909）ng·h·mL^-1. The relative bioavailability of the test capsule was （99.2± 26.7）%. CONCLUSION： The two formulations are proved to be bioequivalent.