摘要
报道用改进的高效液相色谱法测定利福喷丁在大鼠血液、组织、胆汁、粪和尿中的药物浓度。结果表明,大鼠口服三种剂量(100,50,10mg/kg)后在144h的血液浓度仍分别为11.97±3.11,0.95±0.51,0.16±0.04μg/ml;大鼠口服50mg/kg后在144h时,肝、肺、肾等主要脏器的浓度平均为1.41±0.24,0.66±0.21,0.77±0.31μg/g显示出一定的长效性。大鼠口服三种剂量后的半衰期分别为53.61±7.42,25.69±3.69,24.35±1.09h,提示剂量在50mg和10mg/kg时,利福喷丁的体内过程呈现一级动力学模型,而在剂量100mg/kg时,则表现出非线性动力学的特征。
Concentrations of a new antituberculous drug, rifapentine in plasma, tissue, bile, feoes and urine of male rats were determined by an improved high performance liquid chroma tographie method (HPLC). 144 hours after po treatment with 100, 50, 10mg/kg of rifapentin, plasma concentrations were detected at 12±3, 1.0±0.5, 0.16±0.04μg/ml (x±SD) respectively. Concentrations of rifapentine in liver, lung and kidneys were 1.41 ±0.24, 0.66±0.21, 0.8±0.3μg/g at 144 hours after po administration of 60 mg/kg of rifapentine, indicating a prolonged duration of action. Elimination of rifapentine from bleed tuggests first-order kinetics with a mean half-life of 26+4 hours (50mg/kg) and 24.4 ± 1.1 hours (10 mg/kg). However, at a high dose of 100 mg/kg, the elimination phase was characterized by non-liner dose-related kinetics, with a mean half-time of 54 ±7 hours.
出处
《上海医科大学学报》
CSCD
1990年第2期139-143,共5页
Journal of Fudan University(Medical Science)
关键词
利福喷丁
药代动力学
色谱法
rifapentine
pharmacokinetics
compartment models
