中国临床药理学杂志2024，Vol.40Issue(3)：425-429,5.DOI:10.13699/j.cnki.1001-6821.2024.03.025
特立氟胺片在健康中国受试者体内的药代动力学及生物等效性研究
Pharmacokinetics and bioequivalence study of teriflunomide tablets in healthy Chinese subjects
林莉莉 1胡伟 1蒋燕 1章钦 1秦慧玲 1张茜 1许杨 2梁伟 3孟林英 3储昭兴3
作者信息
- 1. 安徽医科大学第二附属医院药物临床试验研究中心,安徽合肥 230601
- 2. 安徽万邦医药科技股份有限公司,安徽合肥 230601
- 3. 合肥恩瑞特药业有限公司,安徽合肥 230601
- 折叠
摘要
Abstract
Objective To compare the pharmacokinetic profiles of the two teriflunomide tablets in healthy Chinese subjects under fasting and fed conditions and to evaluate their bioequivalence and safety.Methods A randomized,open,single-dose,parallel trial design was used to enroll 31 and 32 healthy Chinese male subjects in the fasting and fed groups,who were randomized to a single oral dose of 14 mg of either reference or test preparation of teriflunomide tablets.The plasma concentrations of teriflunomide were determined using liquid chromatography-tandem mass spectrometry method,and Phoenix WinNonlin 8.1 software was used to calculate pharmacokinetic parameters and perform bioequivalence analysis.Results Subjects received a single oral dose of the reference and test formulations of teriflunomide.The main pharmacokinetic parameters of teriflunomide in the fasting group were as follows:Cmax were(2.14±0.27)and(2.27±0.33)μg·mL-1,AUC0-72h were(105.70±11.20)and(107.72±11.77)μg·mL-1·h,tmax was 1.49 and 0.99 h;the main pharmacokinetic parameters of teriflunomide in the fed group were as follows:Cmaxwere(1.83±0.17)and(1.75±0.22)μg·mL-1,AUC0-72h were(102.66±9.18)and(101.57±13.01)μg·mL-1·h,tmax was 4.01 and 4.99 h.The 90％confidence intervals for the geometric means of Cmax and AUC0-72h for reference and test preparations in the fasting and fed groups were in the range of 80％to 125％.Conclusion The pharmacokinetic characteristics of the 2 formulations were similar under fasting and fed administration conditions,with good bioequivalence and safety;Postprandial administration may delay the time to peak of the drug.关键词
特立氟胺片/生物等效性/药代动力学/安全性/食物影响Key words
teriflunomide tablet/pharmacokinetics/bioequivalence/food effect分类
医药卫生引用本文复制引用
林莉莉,胡伟,蒋燕,章钦,秦慧玲,张茜,许杨,梁伟,孟林英,储昭兴..特立氟胺片在健康中国受试者体内的药代动力学及生物等效性研究[J].中国临床药理学杂志,2024,40(3):425-429,5.
