阿奇霉素胶囊在中国健康受试者中的生物等效性研究  

Pharmacokinetics and pharmacodynamics studies of azithromycin capsules inhealthy Chinese subjects

作　　者：谢朋飞[1,2] 陈元璐 陈菡 周燕 杨鹏 年立忠 左莉英 张永东[1] XIE Peng-fei;CHEN Yuan-lu;CHEN Han;ZHOU Yan;YANG Peng;NIAN Li-zhong;ZUO Li-ying;ZHANG Yong-dong(PhaseⅠClinical Centre,Chenzhou No.1 People’s Hospital,Chenzhou 423000,Hunan Province,China;Research Institute of Hospital Management,University of South China,Chenzhou 423000,Hunan Province,China;Anhui Center for Drug Evaluation&Inspection,Hefei 230000,Anhui Province,China;Anhui Wanbang Pharmaceutical Technology Co.,Ltd.,Hefei 230000,Anhui Province,China;Bengbu BBCA Tushan Pharmaceutical Co.,Ltd.,Bengbu 233050,Anhui Province,China)

机构地区：[1]郴州市第一人民医院Ⅰ期临床研究室,湖南郴州423000 [2]南华大学医院管理研究所,湖南郴州423000 [3]安徽省药品审评查验中心,安徽合肥230000 [4]安徽万邦医药科技股份有限公司,安徽合肥230000 [5]蚌埠丰原涂山制药有限公司,安徽蚌埠233050

出　　处：《中国临床药理学杂志》2024年第1期97-101,共5页The Chinese Journal of Clinical Pharmacology

基　　金：郴州市科技发展计划基金资助项目(yfzx201912);南华大学医院管理研究所基金资助项目(2020YJGL06)。

摘　　要：目的评价阿奇霉素胶囊受试制剂与参比制剂在中国健康受试者中的生物等效性。方法本研究采用随机、开放、两周期交叉试验设计,共入组48例受试者。受试者单次空腹口服阿奇霉素胶囊受试制剂或参比制剂250 mg。以液相色谱-串联质谱联用法测定人血浆样品中阿奇霉素的血药浓度,用WinNon⁃Lin8.1计算和分析阿奇霉素主要药代动力学参数,并进行生物等效性评价。结果空腹条件下单剂量口服阿奇霉素胶囊受试制剂与参比制剂的主要药代动力学参数:C_(max)分别为(319.89±127.35)和(330.41±122.11)ng·mL^(-1);AUC0-192 h分别为(2423.04±587.15)和(2489.97±685.73)ng·h·mL^(-1);AUC0-∞分别为(2753.40±644.96)和(2851.71±784.05)ng·h·mL^(-1);tmax分别为(2.60±1.11)和(2.62±1.13)h;t1/2分别为(76.76±15.14)和(79.83±17.14)h。空腹条件下,受试制剂与参比制剂C_(max)、AUC0-192 h、AUC0-∞几何均值的90%置信区间分别为87.52%~107.18%、91.46%~105.80%和91.17%~105.06%。结论空腹条件下阿奇霉素胶囊受试制剂与参比制剂具有生物等效性。Objective To evaluate the bioequivalence of the test preparation and reference preparation of azithromycin capsules in healthy Chinese subjects.Methods A total of 48 subjects were enrolled in this study using a randomized,open,two-sequence,cross design.Each subject received a single oral dose of azithromycin capsules test drug(T)or reference drug(R)for 250 mg.The concentrations of azithromycin in plasma were determined by Liquid Chromatograph Mass Spectrometer,and the pharmacokinetic parameters were calculated by WinNonlin 8.1 software to evaluate the bioequivalence.Results The main pharmacokinetic parameters of azithromycin after a single fasting dose of the test drug and the reference drug were as follows:the C_(max) were respectively(319.89±127.35)and(330.41±122.11)ng·mL^(-1);AUC0-192 h were respectively(2423.04±587.15)and(2489.97±685.73)ng·h·mL^(-1);AUC0-∞were respectively(2753.40±644.96)and(2851.71±784.05)ng·h·mL^(-1);tmax were respectively(2.60±1.11)and(2.62±1.13)h;t1/2 were respectively(76.76±15.14)and(79.83±17.14)h.The 90%confidence inte rv als for the geometric mean ratios of C_(max),AUC0-192 h and AUC0-∞of T and R were 87.52%-107.18%,91.46%-105.80%and 91.17%-105.06%,respectively.Conclusion The test preparation of azithromycin capsule was bioequivalent to the reference preparation under fasting condition.

关 键 词：阿奇霉素胶囊 药代动力学 生物等效性 安全性 

分 类 号：R97[医药卫生—药品]