异福酰胺胶囊的人体药代动力学和相对生物利用度  

Pharmacokinetic and relative bioavailability of combination isoniazid, rifampicin, pyrazinamide capsule in healthy volunteers

作　　者：陈光亮[1] 许建明[2] 魏伟[3] 徐新华[2] 胡咏梅[2] 张磊[2] 徐叔云[3] 

机构地区：[1]安徽中医学院药理学教研室,合肥230038 [2]安徽医科大学附属医院,合肥230022 [3]安徽医科大学临床药理研究所,合肥230032

出　　处：《安徽医科大学学报》2001年第6期426-429,共4页Acta Universitatis Medicinalis Anhui

摘　　要：目的　研究异福酰胺胶囊的人体药代动力学和相对生物利用度 ,以判断两种制剂是否具有生物等效性。方法　18名健康志愿者采用随机分组交叉自身对照给药。以卫非特片 (Rifater)为参比药物 ,用HPLC法测定血清中药物浓度。结果　两制剂的血药浓度经时变化和药代动力学参数相近 ,异福酰胺胶囊中异烟肼、利福平、吡嗪酰胺的主要药代动力学参数 :T1/2 为 (2 37± 1 0 9)h ,(4 6 3± 0 6 7)h ,(13 43± 2 98)h ;Cmax 为 (8 78± 3 6 3)mg/L ,(11 93±2 6 8)mg/L ,(36 2 8± 9 17)mg/L ;AUCo -t为 (2 8 77±2 0 74)mg/L .h ,(84 6 3± 18 0 1)mg/L·h ,(5 44 87±10 0 17)mg/L·h。相对生物利用度分别为 96 79%±2 6 98% ,97 0 8%± 15 12 % ,10 0 0 3%± 16 0 2 %。结论　异福酰胺胶囊与卫非特片具有生物等效性。Objective To compare the pharmacokinetics and relative bioavailability between combination isoniazid, rifampicin, pyrazinamide capsule and rifater in healthy volunteers. Methods Serum concentration of isoniazid, rifampicin and pyrazinamide were measured by HPLC following single oral doses of the two preparations given to 18 healthy volunteers in a randomized 2-way crossover study. Results The serum concentration-time curves and pharmacokinetics of the two products were similar. Main pharmacokinetic parameters of isoniazid, rifampicin, pyrazinamide in the capsule were:T 1/2 (2.37±1.09) h,(4.63±0.67) h,(13.43±2.98) h;C max (8.78±3.63) mg/L,(11.93±2.68) mg/L,(36.28±9.17) mg/L; AUC o-t (28.77±20.74) mg/L·h,(84.63±18.01) mg/L·h,(544.87±100.17) mg/L·h. Relative bioavailability was 96.79%±26.98%(INH),97.08%±15.12%(RFP),100.03%±16.02%(PZA). Conclusion The two one-sided statistical test showed that the two formulations were bioequivalent.

关 键 词：异烟肼 利福平 吡嗪酰胺 药代动力学 异福酰胺 

分 类 号：R978.3[医药卫生—药品]