国产复方利福平片与进口rifater在中国志愿者的药动学与相对生物利用度的研究(英文)  

Studies on the pharmacokinetics and relative bioavailability of domestic compound rifampin tablet and imported rifater in Chinese volunteers

作　　者：洪诤[1] 王浴生[1] 夏培元[1] 王正荣[1] 

机构地区：[1]华西医科大学,成都610044

出　　处：《中国抗生素杂志》2001年第5期375-379,共5页Chinese Journal of Antibiotics

摘　　要：本试验对 12名男性志愿受试者签署知情同意书 ,按随机双交叉设计口服国产复方利福平片 (华北制药康欣有限公司研制 ,含利福平 12 0 mg,异烟肼 80 mg,吡嗪酰胺 2 5 0 mg)与相同处方的美国进口 rifater片各 4片后 ,定时抽取血样并分别对利福平、异烟肼和吡嗪酰胺的血药浓度和药代动力学参数进行比较。血药浓度用 HPL C法检测 ,用 3P87和 NDST程序 ,按非室模型进行药代动力学分析。结果表明 ,口服国产复方利福平片 (又称异福酰胺片 )和进口 rifater片各 4片后 ,利福平的 AUC分别为 (73.90±2 3.41)与 (72 .84± 2 5 .5 8) mg· h/ L ,Cmax为 (16 .7± 3.6 )与 (16 .6± 3.6 ) mg/ L ,Tmax为 (1.8± 0 .3)与 (1.8± 0 .2 ) h;异烟肼的 AUC分别 (4 0 .74± 16 .11)与 (4 3.2 6± 17.99) mg· h/ L ,Cmax为 (9.9± 3.4)与 (10 .0± 2 .8) mg/ L ,Tmax为 (1.7± 0 .4)与 (1.7± 0 .4) h;吡嗪酰胺的 AUC分别为 (4 99.35± 194.35 )与 (5 15 .6 9± 198.931) mg· h/ L,Cmax为 (4 0 .4± 13.2 )与 (4 0 .6± 12 .4) mg/ L,Tmax为 (1.6± 0 .4)与 (1.6± 0 .4) h。以进口的 rifater片为 10 0 % ,华北制药康欣有限公司提供的利福平三联片口服后三成分的相对生物利用度 :利福平为 10 1.45 % ,异烟肼为 94.17%和吡嗪?The ingredients of domestic antituberculous compound rifampin tablets (CRFP) were the same as US made rifater (USRF) which is composed of rifampin (R) 120mg, isoniazid (H) 80mg and pyrazinamide (P) 250mg. Twelve Chinese healthy volunteers [(20.9±1.0)y, (61.9±3.5)kg] participating in this study after providing informed consent were given a single dose of 4 tablets orally according to a double cross design. The plasma drug concentrations of each ingredient were measured by HPLC assay individually. The plasma concentration time curves of them could be well described by an open one compartment model. Results revealed that the pharmacokinetic parameters of R, H, and P in CRFP and USRF were very similar. AUC: R, (73.90±23.41) and (72.84±25.58)mg·h/L; H, (40.75±16.11) and (43.26±17.99)mg·h/L; P, (499.35±194.35) and (515.69±198.93)mg·h/L; C max : R, (16.7±3.6) and (16.6±3.6)mg/L; H, (9.9±3.4) and (10±2.6)mg/L; P, (40.4±13.2) and (40.6±12.4)mg/L; T max : R, (1.8± 0.3 ) and (1.8±0.2)h; H, (1.7±0.4) and (1.7±0.4)h; P, (1.6±0.4) and (1.6±0.4)h, respectively. The relative bioavailability of each ingredient in CRFP compared with USRF (100%) were as follows: R, 101.45%; H, 94.17%; P,96.83%. These results suggested CRFP could be used with the same dosage schdule as USRF to TB patients.

关 键 词：复方利福平片 Rifater 血药浓度 药动学 生物利用度 

分 类 号：R978.3[医药卫生—药品] R969.1[医药卫生—药学]