阿奇霉素分散片人体药动学及生物等效性研究.PDFVIP

·40· Chin JMAP, 2010 January, Vol.27 No.1 中国现代应用药学 2010 年 1 月第 27 卷第 1 期 阿奇霉素分散片人体药动学及生物等效性研究 刘建明，温金华，张红，隋双明，张娟，熊玉卿*(南昌大学医学院临床药理研究所，南昌 330006) 摘要：目的 研究阿奇霉素分散片健康人体的药动学与生物等效性。方法 20 名男性健康志愿者随机交叉口服阿奇霉素 分散片受试制剂和参比制剂各 500 mg，采用高效液相色谱-质谱法(LC-MS)测定血药浓度。以 DAS 2.0 软件计算其药动学 参数，考察其生物等效性。结果 受试制剂和参比制剂阿奇霉素 AUC0-168 分别为(8.98±1.74) ?g·h·mL?1 和(8.75±1.60) ?g·h·mL?1，Cmax 分别为(0.81±0.14) ?g·mL?1 和(0.80±0.14) ?g·mL?1，t1/2 分别为(48.16±11.10) h 和(51.1±7.60) h，Tmax 分别为 (1.80±0.86) h 和(1.82±0.92) h，受试制剂相对于参比制剂的生物利用度为(103.4±20.2)%。结论 阿奇霉素分散片受试制剂 和参比制剂具有生物等效性。 关键词：阿奇霉素；药动学；生物等效性；高效液相色谱-质谱法 中图分类号：R945 文献标志码：A 文章编号：1007-7693(2010)01-0040-03 Study on Pharmacokinetics and Bioequivalence of Azithromycin Dispersible Tablets in Healthy Volunteers LIU Jianming, WEN Jinhua, ZHANG Hong, SUI Shuangming, ZHANG Juan, XIONG Yuqing*(Institute of Clinical Pharmacology, Medical College Nanchang University, Nanchang 330006, China) ABSTRACT: OBJETIVE To study the pharmacokinetics and bioequivalence of azithromycin dispersible tablets in healthy volunteers. METHODS A single oral dose of 500 mg test or reference formulations was given to 20 male healthy volunteers in a randomized cross-over design. The concentration of azithromycin in plasma was determined by HPLC-MS. Pharmacokinetic parameters and relative bioavailability were calculated by DAS 2.0 software. RESULTS The main pharmacokinetic parameters of test and reference azithromycin were as the followings: AUC0-168 (8.98±1.74) ?g·h·mL?1 and (8.75±1.60) ?g·h·mL?1; Cmax (0.81±0.14) ?g·mL?1 and (0.80±0.14) ?g·h·mL?1; t1/2 (48.16±11.10) h and (51.1±7.60) h; Tmax (1.80±0.86) h and (1.82±0.92) h. The relative bioavailability of test to reference preparation was (103.4±20.2)%. CONCLUSION The test and reference formulations were bioequivalent. KEY WORDS: azithromycin; pharmacokinetics; bioequivalence; LC-MS 阿奇霉素是新一代大环内醋类抗生素，其通 过阻碍细菌转肽过程，从而抑制细菌蛋白质的合 成，作用机制与红霉素相同，主要与细菌核糖体 的 50S 亚