首页> 外文期刊>Asian journal of drug metabolism and pharmacokinetics >Pharmacokinetics of 4-dichlorophenyl-propenoyl-sec. -butylamine (7903) in rats
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Pharmacokinetics of 4-dichlorophenyl-propenoyl-sec. -butylamine (7903) in rats

机译:4-二氯苯基-丙烯酰基-sec的药代动力学。丁胺(7903)在大鼠中

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Aim To investigate the pharmacokinetics of 3,4-dichlorophenyl-propenoyl-sec.- butylamine (7903) after three single oral doses and a multiple oral dose in rates. Methods The plasma concentration of 7903 in rats were measured by HPLC method and pharmacokinetics parameters were estimated by program 3p97. Results The results indicated that the plasma concentration-time courses of 7903 were best fitted to one-compartment open models. The major average pharmacokinetic parameters of 7903 were as following: T_(max):3.10, 3.60, and 5.00h; C_(max) 3.27, 5.10, and 8.09 mugcentre not mL~(-1); t_(1/2) 2.12 , 3.07, and 4.16 h; AUC_(0-t) 15.01, 49.62 and 124.69 mugcentre notmL~(-1)-h, respectively. Moreover, after multiple oral administration of 100 mgcentre notkg~(-1)7903, the pharmacokinetic parameters of 7903 including C_(max)(4.60 mugcentre notmL~(-1)), and AUC (50.75 mugcentre notmL~(-1)centre noth) were not significantly different, compared with the results of the single oral dose, but T_(max) (8.0 h) and t_(1/2) (5.42 h) were somewhat prologeded. Conclusion The results shown that 7903 was absorbed in gastro-intestinal tract and two peak plasma concentrations were exhibited. The parent drug was eliminated rapidly from rats plasma. The plasma concentrations of 7903 were increased as dose-dependent manner within the range of 50-200 mgcentre notkg~(-1).
机译:目的研究3,4-二氯苯基-丙烯酰基-仲丁胺(7903)在单次口服3次和多次口服后的药代动力学。方法采用HPLC法测定大鼠血浆7903浓度,用程序3p97估算药代动力学参数。结果结果表明,7903血浆浓度-时间过程最适合单室开放模型。主要平均药代动力学参数为7903,如下:T_(max):3.10、3.60和5.00h; C_(最大值)3.27、5.10和8.09马克杯,而不是mL〜(-1); t_(1/2)2.12、3.07和4.16小时; AUC_(0-t)15.01、49.62和124.69杯中心分别不mL〜(-1)-h。此外,在多次口服100 mgcentnotkg〜(-1)7903后,7903的药代动力学参数包括C_(max)(4.60 mugcentremL〜(-1))和AUC(50.75 mugcentnotnotmL〜(-1)centre)。与单次口服剂量的结果相比,noth)没有显着差异,但是在一定程度上增加了T_(max)(8.0 h)和t_(1/2)(5.42 h)。结论结果表明7903在胃肠道中被吸收,并且出现两个峰值血浆浓度。母体药物迅速从大鼠血浆中清除。 7903的血浆浓度在50-200 mgcentnotkg〜(-1)范围内呈剂量依赖性增加。

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