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

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.