放射性同位素标记法研究加替沙星在小鼠体内的吸收、分布和排泄

Using radioactive isotope labeling method study absorption, distribution and elimination of Gatifloxacin in mice

本文用3H标记的方法研究加替沙星在小鼠体内的吸收、分布和排泄。小鼠静脉注射3H-加替沙星三个剂量:4mg/Kg、8mg/Kg、16mg/kg,用液体闪烁谱仪测定不同时间血药浓度,建立血药浓度-时间关系。结果显示:静脉注射3H-加替沙星在小鼠体内代谢符合二房室开放模型,分布相半衰期T1/2α分别为0.16h,0.15h和0.19h;消除相半衰期T1/2β分别为55.55h,45.75h,和52.11h;表观分布容积V分别为0.77L.Kg-1,0.62L.Kg-1和0.95L.Kg-1;曲线下面积AUC分别为74.08μg.h.L-1,89.28μg.h.L-1和211.88μg.h.L-1。3H-加替沙星在小鼠体内分布很广,没有发现特异性组织积累。

Absorption, distribution and elimination of Gatifloxacin in mice are studied using ^3H labeling method. After iv injection of 4mg（9.25MBq）/Kg, 8mg（18.5MBq）/Kg and 16mg（37MBq）/Kg ^3H-Gatifloxacin ^3H-Gatifloxacin concentration in blood is determinated with liquid scintillation analyzer. The results show that concentration-time curve after iv injection are fitted to a 2-compartment open model, Distribution phase half life T1/2α is 0.16, 0.15, 0.19h, respectively, elimination phase half life T1/2β is 55.55, 45.75, 52.11h respectively, the appearance volume of distribution V is 0.77, 0.62, 0.95 L·Kg^-1 respectively, area under curve AUC is 74.08, 89.28, 211.88 μg·h·L^-1 ^3H-Gatifloxacin is distributed extensively in various tissue and organ in mice but is not found accumulation in special tissue and organ.