国产阿奇霉素人体药代动力学及生物等效性研究

Pharmacokinetics and relative Bioavailability of Azithromycin in Healthy Volunteers

对１２ 名健康男性志愿者单剂量空腹口服供试品阿奇霉素分散片及对照品阿奇霉素胶囊进行了药代动力学研究。采用微生物法测定受试者服药后不同时间点血尿药物浓度，计算其药代动力学参数及相对生物利用度。结果表明两药体内过程均符合血管外一级吸收的二房室模型。Ｃｍ ａｘ分别为（０３６±０１４）和（０３３±０１２） ｍ ｇ／Ｌ，ｔ１／２β分别为（４１８２±４７９）和（３９３１±６０１）ｈ，ＡＵＣ分别为（５４０±１８８）和（５３９±１９１） ｈ·ｍ ｇ／Ｌ，两者间差别均无统计学意义（Ｐ＞ ００５）。与对照品比较，供试品阿奇霉素分散片的相对生物利用度为（１００４０±６６３）％ 。口服阿奇霉素分散片１４４ ｈ 尿药排出率为给药量的１１０９％ 。

The pharmacokinetics of azithromycin was assessed in 12 healthy volunteers after single oral doses administration of azithromycin 500 mg tablets for trial and capsules for control.Blood and urine azithromycin concentrations were determined microbiologically,and the pharmacokinetics and relative biological availability were calculated.The results showed that the metabolic process of the two drugs in vivo accorded with a two compartment open model with an extravascular first order absorption.The C max of tablet and capsule were 0.36±0.14 and 0.33±0.12 mg·L -1 respectively ,T 1/2β were 41.82±4.79 h and 39.31±6.01 h respectively and AUC were 5.40±1.88 and 5.39±1.91 mg·L -1 ·h respectively.There was no significant difference.The relative bioavailability of azithromycin tablet to capsule was 100.04±6.63%.It is suggested from these results that the pharmacokinetics and bioavailability of azithromycin showed no statistically significant difference between tablet and capsule.The cummulative excretion of tablet from urine in 144 h was 11.09%.