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苯恶洛芬在人体的药代动力学研究:根据单剂量数据预测稳态血药浓度

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

作者信息

Chatfield D H, Tarrant M E, Smith G L, Speirs C F

出版信息

Br J Clin Pharmacol. 1977 Oct;4(5):579-83. doi: 10.1111/j.1365-2125.1977.tb00789.x.

DOI:10.1111/j.1365-2125.1977.tb00789.x
PMID:303114
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1429156/
Abstract

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.

摘要
  1. 在8名受试者单次口服100毫克后2至168小时测量了贝诺洛芬的血浆水平。使用两室开放模型通过NON-LIN计算机程序估算药代动力学参数。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。中央室和周边室的分布容积分别为6.8升和3.2升。2. 将11名受试者按三或四人一组,给予25毫克/天、50毫克/天或100毫克,每日两次,共11天。将他们的血浆水平与根据上述参数预测的水平进行比较,这些参数已根据个体体重和消除半衰期进行了调整。每种情况下都预测了稳态血浆水平,并达到了合理的准确度(平均91%)。3. 随着剂量增加,观察到的和预测的水平没有出现偏离趋势,并且没有证据表明重复给药后贝诺洛芬的处置有任何变化。4. 药代动力学参数用于预测各种给药方案的稳态血浆水平。

相似文献

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Pharmacokinetic studies with benoxaprofen in man: prediction of steady-state levels from single-dose data.苯恶洛芬在人体的药代动力学研究:根据单剂量数据预测稳态血药浓度
Br J Clin Pharmacol. 1977 Oct;4(5):579-83. doi: 10.1111/j.1365-2125.1977.tb00789.x.
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本文引用的文献

1
Preliminary studies of absorption and excretion of benoxaprofen in man.苯恶洛芬在人体中的吸收与排泄的初步研究。
Br J Clin Pharmacol. 1977 Oct;4(5):585-90. doi: 10.1111/j.1365-2125.1977.tb00790.x.