诺氟沙星注射剂和胶囊剂的人体药代动力学  

COMPARISON OF THE PHARMACOKINETICS OF NORFLOXACIN INJECTION AND NORFLOXACIN CAPSULE IN NORMAL HUMAN VOLUNTEERS

作　　者：栾立标[1] 朱家壁[1] 

机构地区：[1]中国药科大学药剂学教研室,南京210009

出　　处：《药学学报》2000年第2期147-150,共4页Acta Pharmaceutica Sinica

摘　　要：目的:考察自制的肌注诺氟沙星注射剂在体内的动态行为,并与诺氟沙星胶囊剂进行比较。方法:用HPLC法测定这两种制剂在人体的血药浓度,并用非线性最小二乘法迭代程序进行数据处理。结果:注射剂在体内的过程可用开放型二室模型描述,其主要体内参数为:AUC=584h·μg·mL-1,Tmax=035h,Cmax=114μg·mL-1,MRT=732h;而胶囊剂则符合一室模型,主要体内参数为:AUC=429h·μg·mL-1,Tmax=128h,Cmax=072μg·mL-1,MRT=616h。结论:注射剂较胶囊剂生物利用度高,起效快,峰浓度高,作用持久。AIM: The pharmacokinetic profile of a new injection formulation of 124 mg norfloxacin (I) after intramuscular injection was studied and compared with that of a 124 mg marketed oral I capsule. METHODS: The norfloxacin intramuscular injection and the oral norfloxacin capsule were given to 8 healthy male subjects (aged 20～30 years) in a randomized crossover study. The determination of the I serum concentration was carried out by high performance liquid chromatography. RESULTS: The pharmacokinatic profiles of the norfloxacin intramuscular injection and the oral norfloxacin capsule may be fitted to a two and one compartment open model, respectively. The pharmacokinetic parameters were estimated by using the nonlinear least square computer program on basis of the compartment model. The noncompartmental pharmacokinetic parameters were also calculated on basis of the statistic moment theory. The injection (im) gave an area under the curve (AUC) 1 34 fold higher, a peak concentration ( C max ) 1 5 fold bigger and a time to C max ( T max ) 3 5 fold shorter than those of the capsule ( po ) ( P <0 05). The systemic clearance (Cls) and mean residence time (MRT) for injection (im) was 21 80 L·h -1 and 7 32 h respectively, compared with 31 15 L·h -1 and 6 16 h for the capsule ( po ) ( P <0 1). CONCLUSION: The intramuscular norfloxacin injection (im) was better and more rapidly absorbed and more slowly eliminated than the oral capsule ( po ).

关 键 词：诺氟沙星注射液 诺氟沙星胶囊 药代动力学 

分 类 号：R978.19[医药卫生—药品] R969.1[医药卫生—药学]