摘要
目的 :研究阿奇霉素国产分散片与进口片剂人体相对生物利用度及药物动力学。方法 :12名健康受试者自身交叉单剂量口服阿奇霉素国产分散片和进口片剂各 5 0 0mg ,定时取血 ,用微生物法测定血药浓度。结果 :受试制剂国产阿奇霉素分散片与参比制剂进口片剂的血药浓度时间曲线基本一致 ,符合一级吸收二房室模型。国产分散片、进口片两种制剂的主要药动学参数分别为 :消除半衰期t1/ 2 β:(45 .2± 10 .3)h ,(45 .7± 9.2 )h ;Tmax:(1.3± 0 .6 )h ,(2 .0± 1.0 )h ;Cmax:(414.7± 12 3.8) μg·L-1,(35 2 .5± 92 .1) μg·L-1。药动学参数经配对t检验 ,P >0 .0 5 ,差异均无显著性。两种制剂的药时曲线下面积AUC0→tn平均值分别为 :国产分散片 (480 4.2± 95 7.6 ) μg·L-1·h-1,进口片剂 :(5 10 9.8± 10 10 .5 ) μg·L-1·h-1;国产分散片的相对生物利用度为 :F =(94.7± 13.4) %。结论 :统计学结果表明受试制剂国产阿奇霉素分散片与参比制剂生物等效。
OBJECTIVE:The pharmacokinetics and bioavailabilites of domestic azithromycin dispersible tablets (tested) and imported tablets (reference) were studied.METHODS:A single dose of 500mg azithromycin was given, in a randomized,two way crossover study,in 12 healthy male volunteers.The concentrations in plasma were determined by microbiological assay.RESULTS:Both concentration time curves of domestic and imported products fitted to a two compartment open model with a first order absorption.The main pharmacokinetics parameters were as followings: t 1/2β :( 45.2 ± 10.3 )h,( 45.7 ± 9.2 )h; T max :( 1.3 ± 0.6 )h,( 2.0 ± 1.0 )h; C max :( 414.7 ± 123.8 )μg·L -1 ,( 352.5 ± 92.1 )μg·L -1 ; AUC 0→tn :( 480 4.2 ± 957.6 )μg·L -1 ·h -1 ,( 510 9.8 ± 101 0.5 )μg·L -1 ·h -1 .There are no significant difference between pharmacokinetics parmeters of two preparations ( P > 0.05 ).The relative bioavailability of the domestic dispersible tablets was ( 94.7 ± 13.4 )%.CONCLUSIONS:The results of statistical analysis show that two formulations are bioeqivalent. [
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2000年第10期592-594,共3页
Chinese Journal of Hospital Pharmacy
关键词
阿奇霉素
分散片
生物利用度
药物动力学
azithromycin
dispersible tablets
bioavailability
pharmackinetics
microbiological assay
