国产阿奇霉素分散片的人体生物利用度及其药动学  

Pharmacokinetics and relative bioavailability of domestic azithromycin dispersible tablets in healthy volunteers

作　　者：储小曼[1] 周燕[1] 曹小梅 曹文[1] 卓海通[1] 凌树森[1] 李宝林 刘欣 詹美 

机构地区：[1]南京军区南京总医院,江苏南京210002

出　　处：《中国医院药学杂志》2000年第10期592-594,共3页Chinese Journal of Hospital Pharmacy

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. [

关 键 词：阿奇霉素 分散片 生物利用度 药物动力学 

分 类 号：R978.15[医药卫生—药品] R969.1[医药卫生—药学]