国产异福酰胺生物等效性研究  

STUDY OF PHARMACOKINETIC AND BIOAVAILABILITY OF A COMBINATIN RIFAMPICIN TABLET IN HEALTHY VOLUNTEERS

作　　者：卓海通[1] 雷勇 王承[3] 曹文[1] 何秀平 凌树森[1] 许劲秋[1] 曹晓梅[1] 

机构地区：[1]南京军区南京总医院临床药理科,南京210002 [2]新疆纺织医院药剂科 [3]大庆油田总医院药剂科,大庆163001 [4]河南新乡医学院一附院药剂科,新乡453100

出　　处：《中国临床药理学杂志》1999年第6期425-430,共6页The Chinese Journal of Clinical Pharmacology

摘　　要：12名男性健康受试者采用随机分组交叉自身对照给药方案。单剂量口服(内含利福平(RFP)480mg,吡嗪酰胺(PZA)1000mg,异烟肼(INH)320mg)参比药进口异福酰胺和国产试验药各4片 ,对国产复方利福平片与进口异福酰胺作人体生物利用度比较。用HPLC法分别测定利福平,吡嗪酰胺和异烟肼血药浓度。用3P97计算机程序求药代动力学参数。试验药中利福平 ,吡嗪酰胺和异烟肼的主要药代动力学参数:T1/2 3.89±1.16h,11.02±1.62h和2.39±1.03h;Tmax 1.08±0.36h,0.52±0.25h和0.42±0.22h;Cmax 7.49±1.27mg·L-1 ,28.71±6.57mg·L-1 和10.18±2.04mg·L-1;AUC为46.48±10.35mg·h·L -1,347.06±28.78mg·h·L -1和26.55±13.21mg·h·L -1。相对于参比药的生物利用度为103.84 %±0.68 %,97.55 %±10.84 %和105.93 %±5.67 %。AUC和Cmax 经双单侧t检验结果显示两种制剂为生物等效制剂。The pharmacokinetic and bioavailability of domestic and imported co_rifampicin tablet were studied in 12 healthy volunteers. A single oral dose containing 480 mg of rifampicin (RFP), 1000 mg of pyrazinamid (PZA) and 320 mg of isoniazid (INH) was given to 12 volunteers in an randomized crossover study . Concentrations of RFP, PZA and INH in plasma were determined by HPLC method.The plasma concentration_time curves of two products were all fitted to a one_compartment model. The pharmacokinetic parameters of domestic drug were: T1/2 3.89±1.16 h (RFP), 11.02 ±1.62 h(PZA) and 2.39±1.03 h(INH); Tmax 1.08±0.36 h(RFP) , 0.52±0.25h (PZA) and 0.42 ±0.22h( INH); Cmax 7.49±1.27 mg·L-1(RFP), 28.71±6.57 mg·L-1 (PZA)and 10.18 ±2.04 mg·L-1(INH); AUC 46.48±10.35 mg·h·L-1(RFP), 347.06±28.78 mg·h·L-1 (PZA) and 26.55±13.21 mg·h·L-1(INH). Relative bioavailability were 103.84 ±10.68% for RFP, 97.55±10.84% for PZA , and 105.93±5.67% for INH. The results of two one_sided tests statistical analysis showed that two formulations were bioequivalent.

关 键 词：生物等效性 高效液相色谱法 异福酰胺 

分 类 号：R978.3[医药卫生—药品]