盐酸莫西沙星片在中国健康受试者体内的生物等效性研究  

Bioequivalence of moxifloxacin hydrochloride tablets in healthy Chinese subjects

作　　者：陈文静 欧阳冬生 黄洁[1] 崔畅 杨双[1] 邹志 唐智 阳国平[1] 阳晓燕[1] 管志美[3] CHEN Wen-jing;OUYANG Dong-sheng;HUANG Jie;CUI Chang;YANG Shuang;ZOU Zhi;TANG Zhi;YANG Guo-ping;YANG Xiao-yan;GUAN Zhi-mei(Center of Clinical Pharmacology,the Third Xiangya Hospital of Central South University,Changsha 410013,Hunan Province,China;Changsha Duxact Biotech Co,Ltd.,Changsha 410000,Hunan Province,China;Hunan Drug Evaluation and Certification and Adverse Reaction Monitoring Center,Changsha 410013,Hunan Province,China)

机构地区：[1]中南大学湘雅三医院临床药理中心,湖南长沙410013 [2]长沙都正生物科技有限公司,湖南长沙410000 [3]湖南省药品审评认证与不良反应监测中心,湖南长沙410013

出　　处：《中国临床药理学杂志》2021年第14期1771-1775,共5页The Chinese Journal of Clinical Pharmacology

基　　金：“十三五”国家“重大新药创制”科技重大专项基金资助项目(2020ZX09201010);国家自然科学基金资助项目(81673519)。

摘　　要：目的研究中国健康受试者空腹和餐后口服盐酸莫西沙星片后的药代动力学特征,并评价受试制剂和参比制剂的生物等效性与安全性。方法采用单剂量、随机、开放、两周期、自身交叉设计,空腹组和餐后组受试者分别入组24例,每周期口服受试或参比制剂0.4 g,用LC-MS/MS法测定莫西沙星血药浓度,WinNonlin 7.0软件计算药代动力学参数,进行生物等效性评价。结果空腹组受试与参比制剂的药代动力学参数分别为C_(max)(3491.26±920.72)和(3718.08±1054.13)ng·mL^(-1),AUC_(0-t)(54742.36±10785.97)和(54409.12±9957.62)h·ng·mL^(-1),AUC_(0-∞)(56530.17±11047.87)和(56003.64±10183.45)h·ng·mL^(-1)。餐后组受试参比制剂的药代动力学参数分别为C_(max)(3526.69±866.80)和(3530.78±804.87)ng·mL^(-1),AUC_(0-t)(49211.56±8875.29)和(49138.14±8599.44)h·ng·mL^(-1),AUC_(0-∞)(50829.82±8969.24)和(50930.20±8744.10)h·ng·mL^(-1)。结论空腹和餐后状态下盐酸莫西沙星受试和参比制剂具有生物等效性。Objective To study the pharmacokinetic characteristics of moxifloxacin hydrochloride tablets administered orally under fasting and fed conditions in healthy Chinese volunteers,and to evaluate the bioequivalence and safety of test preparations(T)and reference preparations(R).Methods The study was designed as single dose,randomized,open,two cycles,self-crossover,and twenty-four healthy volunteers were recruited respectively in fasting and fed conditions.Subjects were assigned to receive a single oral of the test or reference formulation per period at a dose of 0.4 g.The plasma moxifloxacin concentration was analyzed by LC-MS/MS.The major pharmacokinetic parameters were calculated by WinNonlin 7.0 and the bioequivalence was evaluated.Results The main pharmacokinetic parameters of a single oral moxifloxacin under fasting condition for T and R were as follows:C_(max)were(3491.26±920.72)and(3718.08±1054.13)ng·mL^(-1),AUC_(0-t)were(54742.36±10785.97)and(54409.12±9957.62)h·ng·mL^(-1),AUC_(0-∞)were(56530.17±11047.87)and(56003.64±10183.45)h·ng·mL^(-1).The main pharmacokinetic parameters of a single oral moxifloxacin under fed condition for T and R were as follows:C_(max)were(3526.69±866.80),(3530.78±804.87)ng·mL^(-1);AUC_(0-t)were(49211.56±8875.29),(49138.14±8599.44)h·ng·mL^(-1);AUC_(0-∞)were(50829.82±8969.24),(50930.20±8744.10)h·ng·mL^(-1).Conclusion The test preparation of moxifloxacin hydrochloride tablets is bioequivalent to the reference preparation under both fasting and fed conditions.

关 键 词：莫西沙星 生物等效 药代动力学 

分 类 号：R97[医药卫生—药品]