Perkins R J, Liu W, Drusano G, Madu A, Mayers M, Madu C, Miller M H
Department of Medicine, Albany Medical College, New York 12208, USA.
Antimicrob Agents Chemother. 1995 Jul;39(7):1493-8. doi: 10.1128/AAC.39.7.1493.
The purpose of this study was to evaluate the pharmacokinetics of ofloxacin in serum and vitreous humor samples from albino and pigmented rabbits by using a recently described animal model which permits robust estimation of parameter values. The drug was administered to rabbits intravenously, multiple vitreous humor and serum samples were taken from each rabbit, and the vitreous humor and serum samples were assayed by high-pressure liquid chromatography. The pharmacokinetic parameters were determined with RSTRIP, an iterative, nonlinear, weighted, least-squares regression program. Eight New Zealand White rabbits and eight Dutch Belted rabbits (split into single-dose and multiple-dose groups) were investigated in this study. The value of penetration into the vitreous humor of albino rabbits (n = 6) was 32.6% +/- 2.12%, with terminal-elimination half-life values of 3.21 and 2.39 h, respectively, for vitreous humor and serum. In pigmented rabbits after a single dose (n = 3) and with a steady-state concentration of drug in serum (n = 4), penetration values were similar, at 30.4% +/- 2.98% and 30.0% +/- 4.12%, respectively (P > 0.10). Following a single dose of ofloxacin, pigmented animals had elimination half-life values from serum and vitreous humor of 2.64 and 4.32 h, respectively. After steady state was achieved, half-life values for serum and vitreous humor were 3.12 and 6.05 h, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
本研究的目的是通过使用一种最近描述的动物模型来评估氧氟沙星在白化和有色家兔血清及玻璃体液样本中的药代动力学,该模型能够可靠地估计参数值。将药物静脉注射给家兔,从每只家兔采集多个玻璃体液和血清样本,并通过高压液相色谱法对玻璃体液和血清样本进行分析。药代动力学参数通过RSTRIP(一种迭代、非线性、加权、最小二乘回归程序)来确定。本研究中调查了8只新西兰白兔和8只荷兰带兔(分为单剂量组和多剂量组)。白化家兔(n = 6)玻璃体液的渗透值为32.6% +/- 2.12%,玻璃体液和血清的终末消除半衰期值分别为3.21小时和2.39小时。在有色家兔中,单剂量给药后(n = 3)以及血清中药物达到稳态浓度时(n = 4),渗透值相似,分别为30.4% +/- 2.98%和30.0% +/- 4.12%(P > 0.10)。单剂量给予氧氟沙星后,有色动物血清和玻璃体液的消除半衰期值分别为2.64小时和4.32小时。达到稳态后,血清和玻璃体液的半衰期值分别为3.12小时和6.05小时。(摘要截断于250字)