2种阿奇霉素制剂的人体生物等效性研究

Study on Bioequivalence of 2 Kinds of Azithromycin Preparations in Healthy Volunteers

目的:研究2种阿奇霉素制剂的人体生物等效性。方法:18名男性健康志愿者采用随机、自身对照、交叉法单剂量口服阿奇霉素分散片(受试制剂)与阿奇霉素胶囊(参比制剂)后,采用微生物法测定血浆中阿奇霉素的血药浓度,利用3p97软件计算主要药动学参数,并进行生物等效性评价。结果:受试制剂与参比制剂的药动学参数分别为:tma(x2.40±0.48)、(2.29±0.55)h,Cmax(0.34±0.06)、(0.30±0.06)μg·mL-1,AUC0～14(42.80±0.80)、(2.82±1.44)μg·h·mL-1,AUC0～∞(2.95±0.67)、(2.91±1.68)μg·h·mL-1。2种制剂的主要药动学参数无显著性差异(P>0.05)。阿奇霉素分散片的相对生物利用度(F)为(99.29±3.85)%。结论:2种阿奇霉素制剂具有生物等效性。

OBJECTIVE：To study the bioequivalence of 2 kinds of azithromycin preparations.METHODS：18 male healthy volunteers were enrolled in randomized controlled crossover design and given a signal oral dose of azithromycin dispersible tablet（test preparation） and azithromycin capsule（reference preparation）.Plasma concentration of azithromycin was detected by microbiological method and pharmacokinetic parameters were calculated using 3p97 software.Bioequivalence of 2 kinds of azithromycin preparations were evaluated.RESULTS：Main pharmacokinetic parameters of test preparation vs.reference preparation were as follows：Cmax（0.34±0.06）μg·mL^-1 vs.（0.30±0.06）μg·mL^-1;tmax（2.40±0.48）h vs.（2.29±0.55）h;AUC0～144（2.80±0.80）μg·h·mL^-1 vs.（2.82±1.44）μg·h·mL^-1;AUC0～∞（2.95±0.67） μg·h·mL^-1 vs.（2.91±1.68） μg·h·mL^-1.There was no significant difference between pharmacokinetic parameters of 2 kinds of preparations（P〉0.05）.The relative bioavailability of azithromycin dispersible tablets was（99.29±3.85）%.CONCLUSION：2 kinds of azithromycin preparations are bioequivalent.