小鼠非布司它的血药浓度和药代动力学测定
Measurement of Plasma Concentration and Pharmacokinetic Parameters of Febuxostat in Mice
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摘要: 目的建立测定非布司它血浆药物浓度的液相色谱-质谱联用(LC-MS)分析方法,研究非布司它在小鼠体内的药代动力学.方法分别尾静脉(10 mg/kg)或口服(50 mg/kg)给予BALB/c小鼠非布司它,然后用LC—MS法测定血浆中非布司它浓度.用DAS软件计算非布司它的药代动力学参数,而绝对生物利用度(F)根据静注和口服的药时曲线下面积(AUC)之比来计算.结果非布司它在0.01～200 mg/L浓度范围内线性关系良好(r=0.9997,P<0.01),样品在血浆中的回收率大于85%,日内和日间RSD小于15%.小鼠静注10 mg/kg非布司它后药代动力学参数药时曲线下面积、半衰期、血浆分布容积、血浆清除率分别为:(62.91±4.68)mg/(L.h)、(12.35±1.06)h、(3.45±0.83)L/kg、(0.12±0.074)L/(h.kg);小鼠口服50 mg/kg非布司它后药代动力学参数药时曲线下面积、半衰期、达峰时间、峰浓度分别为(130.97±9.36)mg/(L.h)、(10.68±1.63)h、(1.5±0.11)h、(15.32±2.64)mg/L,在小鼠体内的绝对生物利用度为41....Abstract: Objective To establish a LC-MS method to measure the concentration of febuxostat in plasma and to investigate pharmacokinetic profile and absolute bioavailability of the drug in BALB/c mice.Methods Febuxostat was given intravenously to mice at 10 mg/kg or orally at 50 mg/kg,respectively.Blood samples were collected at various time following drug administration.Plasma concentration of febuxostat in mice was determined by LC-MS.Pharmacokinetics parameters were calculated by DAS software,and absolute bioavaila...
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Key words:
- Febuxostat /
- LC-MS /
- Pharmacokinetics /
- Bioavailability
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