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Pharmacokinetic studies with benoxaprofen in man: prediction of steady-state levels from single-dose data.

机译:苯诺沙洛芬在人体中的药代动力学研究:单剂量数据预测稳态水平。

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摘要

1 Plasma levels of benoxaprofen were measured in eight subjects 2-168 h after a single oral dose of 100 mg. Pharmacokinetic parameters were estimated by the NON-LIN computer programme using the two-compartment open model. Mean half-lives of absorption, distribution and elimination were respectively 0.4, 4.8 and 37.6 hours. Volumes of distribution were 6.8 and 3.2 litres for the central and peripheral compartments respectively. 2 Eleven subjects in groups of three or four were given 25 mg/day, 50 mg/day or 100 mg two times daily for 11 days. Their plasma levels were compared with those predicted from the above parameters, which were adjusted for individual body weights and elimination half-lives. Steady-state plasma levels were predicted in each case, and a resonable degree of accuracy (mean 91%) achieved. 3 There was no tendency for observed and predicted levels to diverge as the dose was increased, and there was no evidence of any change in the disposition of benoxaprofen on repeated dosing. 4 The pharmacokinetic parameters were used to predict steady state plasma levels for various dosage regimens.
机译:1在单次口服100 mg剂量后2-168小时,在8位受试者中测量了苯甲洛芬的血浆水平。使用两室开放模型通过NON-LIN计算机程序估计药代动力学参数。吸收,分布和消除的平均半衰期分别为0.4、4.8和37.6小时。中央室和外围室的分配容积分别为6.8升和3.2升。 2分为三或四组的11名受试者每天服用25毫克/天,50毫克/天或100毫克,连续11天。将他们的血浆水平与根据上述参数预测的血浆水平进行比较,并针对各个体重和消除半衰期进行了调整。在每种情况下都可以预测稳态血浆水平,并且可以达到合理的准确度(平均91%)。 3没有观察到和预测的水平随剂量增加而发生变化的趋势,并且也没有证据表明重复给药后贝诺沙芬的处置有任何变化。 4药代动力学参数用于预测各种剂量方案的稳态血浆水平。

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