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单次口服双肼屈嗪后人体受试者的血浆浓度及药代动力学

Plasma concentrations and pharmacokinetics of dihydralazine after single oral doses to human subjects.

作者信息

Waller A R, Chasseaud L F, Taylor T, Darragh A, O'Kelly D A

出版信息

Biopharm Drug Dispos. 1979 Oct-Dec;1(2):59-64. doi: 10.1002/bdd.2510010203.

DOI:10.1002/bdd.2510010203
PMID:552862
Abstract

After single oral doses of 20 mg of a suspension of dihydralazine sulphate to human subjects, the peak of mean plasma concentrations of dihydralazine of 47.0 ng ml-1 +/- 11.0 standard deviation (S.D.) (n = 7) was reached at 1 h. Mean concentrations declined biphasically with apparent half-lives of 0.57 and 4.96 h respectively. Dihydralazine was partly converted to hydralazine. The peak of mean plasma concentrations of the latter drug of 3.9 ng ml-1 +/- 1.7 S.D. (n = 7) occurred at 1-2 h after dosing with dihydralazine sulphate and declined to 1.5 ng ml-1 +/- 1.5 S.D. at 6 h. Of the seven subjects studied, three were classified as fast and four as slow acetylators. Mean clearances appeared to be slightly more rapid in fast acetylators (1.63 l min-1 +/- 0.32 S.D.) when compared to slow acetylators (1.31 l min-1 +/- 0.31 S.D.) but this difference and differences in plasma concentrations and in areas under the plasma drug concentration-time curves were not significant (p > 0.1).

摘要

给人体受试者单次口服20mg硫酸双肼屈嗪混悬液后,双肼屈嗪的平均血浆浓度在1小时达到峰值47.0ng/ml±11.0标准差(S.D.)(n = 7)。平均浓度呈双相下降,表观半衰期分别为0.57小时和4.96小时。双肼屈嗪部分转化为肼屈嗪。后者药物的平均血浆浓度峰值为3.9ng/ml±1.7 S.D.(n = 7),在给予硫酸双肼屈嗪后1 - 2小时出现,6小时时降至1.5ng/ml±1.5 S.D.。在研究的7名受试者中,3名被归类为快速乙酰化者,4名被归类为慢速乙酰化者。与慢速乙酰化者(1.31l/min±0.31 S.D.)相比,快速乙酰化者的平均清除率似乎稍快(1.63l/min±0.32 S.D.),但这种差异以及血浆浓度和血浆药物浓度 - 时间曲线下面积的差异均无统计学意义(p>0.1)。

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