异福酰胺片人体生物利用度和药代动力学研究

Study on the Bioavailability and Pharmacokinetics of Compound Rifampicin Tablets in Healthy Volunteers

目的 :研究异福酰胺片的药代动力学和相对生物利用度。方法 :用高效液相色谱法测定不同时间点血浆中利福平、异烟肼和吡嗪酰胺的浓度 ,并根据血药浓度 -时间数据 ,求算有关药代动力学参数和受试制剂的相对生物利用度。结果 :受试制剂中利福平、异烟肼和吡嗪酰胺的主要药代动力学参数为 :Tmax 分别为 (1 69±0 60)h、(0 94±0 57)h、(2 36±1 10)h ;Cmax 分别为(9 86±2 09) μg/ml、(5 36±1 77) μg/ml、(16 20±4 85) μg/ml;T1/2 分别为 (3 43±0 72)h、(2 98±0 75)h、(9 26±1 58)h ;AUC0～t 分别为 (59 34±13 17) μg/(ml·h)、(21 87±14 29) μg/(ml·h)、(212 97±71 52) μg/(ml·h)。参比制剂中利福平、异烟肼和吡嗪酰胺的主要药代动力学参数为 :Tmax 分别为 (1 83±0 66)h、(0 86±0 38)h、(2 08±0 97)h ;Cmax 分别为 (9 98±1 63) μg/ml、(5 60±2 01) μg/ml、(17 79±4 57) μg/ml ;T1/2 分别为 (3 97±1 58)h、(3 15±0 88)h、(9 36±1 85)h ;AUC0～t 分别为 (62 46±14 02) μg/(ml·h)、(21 39±14 53) μg/(ml·h)、(227 09±70 91) μg/(ml·h)。受试制剂相对参比制剂的生物利用度分别为 (98 47±15 00) %、(103 76±15 80) %、(94 38±12 07) %。结论 :AUC0～t和Cmax

OBJECTIVE:To study the pharmacokinetics and relative bioavailability of compound rifampicin tablets MET_HODS:Plasma levels of rifampicin(RFP),isoniazid(INH)and pyrazinamid(PZA) at different time were determined by HPLC methods,then we drew the time-concentration curves and got the pharmacokinetic parameters and relative bioavailability of test-tablets based on the curves RESULTS:The main pharmacokinetic parameters of RFP,INH and PZA in test-tablets were:Tmax,(1 69±0 60)h,(0 94±0 57)h and(2 36±1 10)h;Cmax,(9 86±2 09)μg/ml,(5 36±1 77)μg/ml and (16 20±4 85)μg/ml;T1/2,(3 43±0 72)h,(2 98±0 75)h and(9 26±1 58)h;AUC0～t,(59 34±13 17)μg/(ml·h),(21 87±14 29)μg/(ml·h) and(212 97±71 52)μg/(ml·h) respectively The main pharmacokinetic parameters of RFP,INH and PZA in control tablets were Tmax,(1 83±0 66)h,(0 86±0 38)h and (2 08±0 97)h;Cmax,(9 98±1 63)μg/ml,(5 60±2 01)μg/ml and (17 79±4 57)μg/ml;T1/2,(3 97±1 58)h,(3 15±0 88)h and (9 36±1 85)h;AUC0～t,(62 46±14 02)μg·h/ml,(21 39±14 53)μg/(ml·h) and (227 09±70 91)μg/(ml·h) respectively The relative bioavailability of test-tablets were (98 47±15 00)%,(103 76±15 80)% and (94 38±12 07)% CONCLUSION:The results of two one-sided tests and rank sum test showed that two formulae were statistically bioequivalent