头孢克肟片在健康人体内的药动学和生物等效性研究  

Pharmacokinetics and bioequivalence study of cefixime tablets in Chinese healthy volunteers

作　　者：郭伟一 冯仕银 蔡林芮[1,2,3] 邹琴 陈卓[1,2,3] 苏旭 杜丹[1,2,3] 余勤[1,2,3] CUO Wei-yi;FENG Shi-yin;CAI Lin-rui;ZOU Qin;CHEN Zhuo;SU Xu;DU Dan;YU Qin(Institute of Drug Clinical Trial·GCP,West China Second University Hospital,Sichuan University,Chengdu 610041,China;Key Laboratory for Technical Research on Drug Products In Vitro and In Vivo Correlation,West China Second University Hospital,Chengdu 610041,China;Key Laboratory of Birth Defects and Related Disease of Women and Children,Ministry of Education,West China Second University Hospital,Chengdu 610041,China)

机构地区：[1]四川大学华西第二医院国家药物临床试验机构,成都610041 [2]药物制剂体内外相关性技术研究重点实验室,成都610041 [3]四川大学出生缺陷与相关妇儿疾病教育部重点实验室,成都610041

出　　处：《中国新药杂志》2024年第2期146-150,共5页Chinese Journal of New Drugs

摘　　要：目的:评价健康受试者空腹和餐后条件下单剂量服用头孢克肟片受试制剂和参比制剂的生物等效性.方法:空腹/餐后各34例健康受试者口服头孢克肟片受试制剂或参比制剂Suprax®,采用随机、开放、单剂量、自身交叉设计,用UPLC-MS/MS法检测血浆中头孢克肟浓度,使用Phoenix WinNonlin 8.0软件及SAS 9.4软件分析生物等效性.结果:空腹组34例健康受试者分别单次空腹服用头孢克肟片受试制剂或参比制剂200 mg后,Cmax,AUC0-t及AUC0-∞的几何均值比及其90%置信区间分别为105.85%(98.73%,113.48%),103.47(96.34%,111.13%)和103.23%(96.28%,110.69%),均落在等效区间80.0%~125.00%范围内.餐后组34例健康受试者分别于高脂餐后单次服用受试制剂和参比制剂200 mg后,Cmax,AUC0-t及AUC0-∞的几何均值比及其90%置信区间分别为101.42%(96.88%,106.16%),99.64%(95.26%,104.23%)和99.68%(95.54%,104.00%),均落在等效区间80.0%~125.00%范围内.结论:2种制剂在空腹和餐后条件下具有生物等效性.Objective:To evaluate the bioequivalence between a single test and reference dose of cefixime tablets in healthy volunteers under fasting and fed conditions.Methods:A randomized,open-label,single-dose,self-crossover design was adopted.UPLC-MS/MS was applied to detect the concentrations of cefixime in the plasma samples of healthy subjects under fasting and fed conditions.Phoenix WinNonlin 8.0 and SAS 9.4 software were used for PK parameters calculation and bioequivalence analysis,respectively.Results:Under fasting condition,34 healthy subjects took 0.2 g test and reference preparation.The ratio of the geometric mean and 90%confidence interval of Cmax,AUC0-t and AUC0-∞were 105.85%(98.73%,113.48%),103.47(96.34%,111.13%),and 103.23%(96.28%,110.69%),respectively.All the data fell within the equivalent range of 80.0%~125.00%.Under fed condition,34 healthy subjects took 0.2 g test and reference preparation.The ratio of the geometric mean and 90%confidence interval of Cmax,AUC0-t and AUC0-∞were 101.42%(96.88%,106.16%),99.64%(95.26%,104.23%),and 99.68%(95.54%,104.00%),respectively.All the data fell within the equivalent range of 80.0%~125.00%.Conclusion:The two preparations are bioequivalent under fasting and fed conditions.

关 键 词：头孢克肟片 空腹 餐后 生物等效性研究 药动学 

分 类 号：R969.1[医药卫生—药理学]