阿奇霉素肠溶片的人体药动学与生物等效性研究  

Pharmacokinetics and Bioequivalence of 2 Dosage Forms of Azithromycin Tablets in Healthy Volunteers

作　　者：夏春华[1] 闵盛云 戴群[1] 章新晶[1] 熊玉卿[1] 

机构地区：[1]江西医学院临床药理研究所,南昌330006 [2]江西省监狱管理局中心医院,南昌330100

出　　处：《医药导报》2006年第8期753-755,共3页Herald of Medicine

摘　　要：目的建立测定阿奇霉素血药浓度的微生物法,并评价阿奇霉素肠溶片与普通阿奇霉素片的生物等效性。方法采用微生物法,测定24例健康受试者单剂量交叉口服受试制剂阿奇霉素肠溶片或参比制剂普通阿奇霉素片500 mg后不同时间点的血浆药物浓度,计算药动学参数和相对生物利用度,评价两制剂的生物等效性。结果阿奇霉素肠溶片与普通阿奇霉素片AUC0→144 h分别为(21.021±4.053)和(20.597±3.850)mg.h-1.L-1,Cmax分别为(0.583±0.073)和(0.603±0.061)mg.L-1,tmax分别为(3.900±0.800)和(3.000±0.700)h,t1/2分别为(29.799±1.935)和(28.850±1.598)h。两制剂主要药动学参数差异无显著性。结论该实验所建立的方法简便快捷,两制剂具有生物等效性,但受试制剂阿奇霉素肠溶片在人体内的吸收速度较参比制剂阿奇霉素普通片慢。Objective To develop a microbiological method for the determination of the blood concentration of azithromycin so as to assess the bioequivalence of the enteric-coated azithromycin tablets and reference azithromycin tablets in healthy volunteers. Methods The azithromycin concentrations in the blood plasma were determined with by a microbiological method at different time points after a single oral dose of 500 mg of tested azithromycin enteric-coated tablets and ordinary azithromycin tablets given respectively to each of the 24 healthy male volunteers in an open randomized crossover design. The pharmacokinetic parameters and relative bioavailability were calculated for the assessment of the bioequivalence of the 2 dosage forms. Results The AUC（0→144h） hof the tested asithromycin enteric-coated tablets and ordinary asithromycin tablets were （21. 021 ±4.053） and （20.597 ±3.850） mg·h^-1·L^-1 ,Cmax were（0.583 ±0.073）and（0.603 ±0.061） mg ·L^-1 ,tmax were（3.900 ± 0. 800） and （ 3. 000 ± 0. 700） h, t1/2 were （29.799 ± 1. 935 ） and （ 28. 850 ± 1. 598 ） h, respectively. These main pharmacokinetic parameters showed that the differences between the 2 dosage forms of the drug were not statistically significant. Conclusion The method was simple, convenient and rapid. The 2 dosage forms of azithromycin were bioequivalent. The absorption of the tested azithromycin enteric-coated tablets in the human body, however, was slower than that of the reference tablets.

关 键 词：阿奇霉素 微生物法 药动学 生物等效性 

分 类 号：R977.6[医药卫生—药品] R978.15[医药卫生—药学]