利福平胶囊在中国健康受试者中的生物等效性研究  

Bioequivalence study of rifampicin capsules in Chinese healthy subjects

作　　者：杨涛 朱恩圆 石国琳 郑远航 李挺[2] 乐艳 宋燕红 孙纪元 YANG Tao;ZHU En-yuan;SHI Guo-lin;ZHENG Yuan-hang;LI Ting;LE Yan;SONG Yan-hong;SUN Ji-yuan(Zhejiang SUKEAN Pharmaceutical Co.,Ltd.,Hangzhou 31000,Zhejiang Province,China;Clinical Research Center,The Second Affiliated Hospital of Wenzhou Medical University,Wenzhou 325000,Zhejiang Province,China;Hangzhou Bio-Science Pharma-Tech Corp.,Ltd.,Hangzhou 310000,Zhejiang Province,China)

机构地区：[1]浙江苏可安药业有限公司,浙江杭州310000 [2]温州医科大学附属第二医院临床研究中心,浙江温州325000 [3]杭州百杏生物技术有限公司,浙江杭州310000

出　　处：《中国临床药理学杂志》2023年第19期2819-2823,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究不同晶型利福平胶囊在中国健康人体内的生物等效性。方法空腹试验24例健康受试者,按单剂量、自身交叉设计、双周期口服利福平胶囊受试制剂或参比制剂150 mg,用液相色谱-质谱法测定血浆中利福平的血药浓度,用WinNonlin 7.0软件计算药代动力学参数及相对生物利用度,判定两制剂是否等效。结果在空腹实验中,利福平胶囊受试制剂(Ⅰ晶型)与参比制剂(Ⅱ晶型)的C_(max)分别为(2822.05±825.02)和(2596.52±666.47)ng·mL^(-1),AUC_(0-t)分别为(1.07×10^(4)±2632.78)和(1.05×10^(4)±3072.12)ng·mL^(-1)·h,AUC_(0-∞)分别为(1.13×10^(4)±2866.09)和(1.10×10^(4)±3386.96)ng·mL^(-1)·h,C_(max)、AUC_(0-t)、AUC_(0-∞)的几何均值比的90%置信区间均在生物等效性的等效范围要求(80.00%~125.00%)内。结论不同晶型的利福平胶囊在中国健康受试者体内生物等效。Objective To evaluate the bioequivalence of rifampicin capsules with different crystal forms in Chinese healthy volunteers.Methods In the fasting test,24 healthy subjects were given 150mg of rifampicin capsule test preparation or reference preparation according to a design of single dose,self-cross and dual cycle oral administration.The plasma concentration of rifampicin was determined by liquid chromatography-mass spectrometry.The pharmacokinetic parameters and relative bioavailability were calculated by WinNonlin 7.0 software to determine whether the two preparations were equivalent.Results Under fasting state,the C_(max)of rifampicin capsule test(crystal formⅠ)and reference(crystal formⅡ)were(2822.05±825.02)and(2596.52±666.47)ng·mL^(-1),AUC_(0-t)were(1.07×10^(4)±2632.78)and(1.05×10^(4)±3072.12)ng·mL^(-1)·h,AUC_(0-∞)were(1.13×10^(4)±2866.09)and(1.10×10^(4)±3386.96)ng·mL^(-1)·h,respectively.The 90%confidence interval of the geometric mean ratio of C_(max),AUC_(0-t),AUC_(0-∞)is within the requirements of the equivalent range of bioequivalence(80.00%-125.00%).Conclusion Rifampicin capsules with different crystal forms are bioequivalent in Chinese healthy subjects.

关 键 词：利福平胶囊 生物等效性 药代动力学 晶型 液相色谱-串联质谱法 

分 类 号：R978.3[医药卫生—药品]