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目的:比较健康受试者空腹、餐后单剂量口服吡非尼酮胶囊的药动学.方法:健康受试者12名(男女各半),随机交叉空腹、餐后单剂量口服吡非尼酮胶囊400 mg,HPLC法测定其血药浓度,DAS v2. 0软件计算药动学参数.结果: 空腹和餐后单剂量口服吡非尼酮胶囊的药时曲线均符合一级吸收的一室模型.空腹和餐后服药的药动学参数:t1 2分别为(2. 16 ± 0. 47), (2.05 ±0.42)h;tmax分别为(0.69 ±0.16),(1.46 ±0.40)h;Cmax分别为(12.95 ±1.79),(9.16 ±2.87)mg·L-1;AUC0-12分别为(44.97 ±15.06),(36.19 ±14.44)mg·h·L-1;AUC0-∞分别为(46.55 ±16.79),(37.41 ±15.43)mg·h·L-1.与空腹给药组比较,餐后服用吡非尼酮胶囊可以显著延长药物tmax(P<0. 001),降低其Cmax(P<0. 001)和AUC(P<0. 01).结论:进食对吡非尼酮胶囊药动学具有显著影响,可减慢其吸收速率,并降低其吸收程度,与患者耐受性更好相关.“,”Objective: To compare the pharmacokinetics and bioavailability of pirfenidone in the fasted and fed states in healthy volunteers. Methods: An open-label, randomized crossover study was conducted in 12 healthy subjects. Food effects were examined by comparing pharmacokinetic data of pirfenidone after administration of a single oral 400 mg dose under fasted or fed conditions. Plas-ma pirfenidone concentration was determined by an HPLC method and its pharmacokinetic parameters were calculated with DAS v2. 0 software. Results: Under fasted and fed conditions, the concentration-time profiles of pirfenidone were fitted a one-compartment model and the pharmacokinetic parameters were as follows: t1/2were (2. 16 ± 0. 47) and (2. 05 ± 0. 42) h;tmaxwere(0. 69 ± 0. 16)and (1. 46 ± 0. 40)h;Cmaxwere (12. 95 ± 1. 79) and (9. 16 ± 2. 87) mg·L-1;AUC0-12were (44. 97 ± 15. 06) and (36. 19 ± 14. 44) mg·h·L-1;AUC0-∞were (46. 55 ± 16. 79) and (37. 41 ± 15. 43) mg·h·L-1, respectively. When compared with that of the fasted group, tmaxwas significantly increased (P<0. 001) while Cmaxand AUC were remarkedly decreased in the fed group (P<0. 001 and P<0. 01, respectively). Conclusion: Concomitant food intake significantly influences the pharmacokinetics and bioavail-ability of pirfenidone as indicated by reducing its extent and rate of absorption, which is associated with better tolerability.