Brunt E, Limberg J, Derendorf H
College of Pharmacy, Department of Pharmaceutics, J. Hillis Miller Health Center, University of Florida, Gainesville 32610.
J Pharm Biomed Anal. 1990;8(1):67-71. doi: 10.1016/0731-7085(90)80008-d.
A rapid technique for sample preparation and HPLC was developed to study in vitro the erythrocyte binding and plasma protein binding of fleroxacin in the concentration range 0.2-15 micrograms ml-1. The red blood cell partition coefficient of fleroxacin was 1.45 +/- 0.18 at 25 degrees C and was independent of concentration, incubation time and temperature. The in vitro plasma protein binding of fleroxacin in humans, determined by two independent methods, was 47-51%. Partition studies using erythrocytes as a simple in vitro model may be useful to predict the degree of tissue uptake and the volume of distribution.
开发了一种用于样品制备和高效液相色谱的快速技术,以体外研究氟罗沙星在0.2 - 15微克/毫升浓度范围内的红细胞结合和血浆蛋白结合情况。氟罗沙星在25℃时的红细胞分配系数为1.45±0.18,且与浓度、孵育时间和温度无关。通过两种独立方法测定,氟罗沙星在人体中的体外血浆蛋白结合率为47 - 51%。使用红细胞作为简单体外模型的分配研究可能有助于预测组织摄取程度和分布容积。