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口服硝苯地平的药代动力学——一项群体研究。

The pharmacokinetics of oral nifedipine--a population study.

作者信息

Renwick A G, Robertson D R, Macklin B, Challenor V, Waller D G, George C F

机构信息

Clinical Pharmacology Group, University of Southampton.

出版信息

Br J Clin Pharmacol. 1988 Jun;25(6):701-8. doi: 10.1111/j.1365-2125.1988.tb05256.x.

DOI:10.1111/j.1365-2125.1988.tb05256.x
PMID:3203042
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1386447/
Abstract
  1. The pharmacokinetics and metabolism of nifedipine have been studied in a population of 59 young male volunteers following administration of a 10 mg capsule. 2. The area under the plasma concentration-time curves (AUC) for nifedipine demonstrated a skewed but not a bimodal distribution (mean 154 ng ml-1 h; range 54-306 ng ml-1h). 3. Calculation of the ratio of the AUC of nifedipine to the AUC of its nitropyridine metabolite did not separate those individuals with high AUC values of nifedipine from the remainder of the population. 4. Similarly there was no evidence for bimodality in the excretion of the major urinary metabolite. Those subjects with high plasma AUC values for nifedipine excreted similar amounts to the remainder of the population. 5. In contrast to a previous study using a 20 mg oral dose, there was no evidence of polymorphism in the pharmacokinetics or metabolism of nifedipine following a single 10 mg oral dose.
摘要
  1. 在59名年轻男性志愿者群体中,口服10毫克胶囊后对硝苯地平的药代动力学和代谢情况进行了研究。2. 硝苯地平的血浆浓度-时间曲线下面积(AUC)呈偏态分布而非双峰分布(均值为154纳克·毫升⁻¹·小时;范围为54 - 306纳克·毫升⁻¹·小时)。3. 计算硝苯地平AUC与其硝基吡啶代谢产物AUC的比值,未能将硝苯地平AUC值高的个体与其余人群区分开来。4. 同样,主要尿代谢产物的排泄也没有双峰现象的证据。硝苯地平血浆AUC值高的受试者排泄量与其余人群相似。5. 与之前使用20毫克口服剂量的研究不同,单次口服10毫克硝苯地平后,其药代动力学或代谢过程中没有多态性的证据。

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本文引用的文献

1
Nifedipine kinetics and bioavailability after single intravenous and oral doses in normal subjects.硝苯地平在正常受试者单次静脉注射和口服后的动力学及生物利用度。
J Clin Pharmacol. 1983 Apr;23(4):161-70. doi: 10.1002/j.1552-4604.1983.tb02720.x.
2
Liquid chromatographic determination of nifedipine in plasma and of its main metabolite in urine.血浆中硝苯地平及其尿液中主要代谢物的液相色谱测定法。
J Chromatogr. 1984 Jun 8;308:209-16. doi: 10.1016/s0021-9673(01)87547-6.
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The first pass metabolism of nifedipine in man.硝苯地平在人体中的首过代谢。
Br J Clin Pharmacol. 1984 Dec;18(6):951-4. doi: 10.1111/j.1365-2125.1984.tb02569.x.
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Cytochrome P-450-dependent oxidation of felodipine--a 1,4-dihydropyridine--to the corresponding pyridine.
Xenobiotica. 1984 Sep;14(9):719-26. doi: 10.3109/00498258409151470.
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Variability in nifedipine pharmacokinetics and dynamics: a new oxidation polymorphism in man.
Biochem Pharmacol. 1984 Nov 15;33(22):3721-4. doi: 10.1016/0006-2952(84)90165-5.
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[Clinical study on the pharmacokinetics of radioactively labelled 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester].[放射性标记的4-(2'-硝基苯基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸二甲酯的药代动力学临床研究]
Arzneimittelforschung. 1972 Feb;22(2):330-4.
7
Food and nifedipine pharmacokinetics.食物与硝苯地平的药代动力学
Br J Clin Pharmacol. 1987 Feb;23(2):248-9. doi: 10.1111/j.1365-2125.1987.tb03040.x.
8
The effects of food and posture on the pharmacokinetics of a biphasic release preparation of nifedipine.食物和体位对硝苯地平双相释放制剂药代动力学的影响。
Br J Clin Pharmacol. 1986 Nov;22(5):565-70. doi: 10.1111/j.1365-2125.1986.tb02936.x.
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Polymorphic drug oxidation: pharmacokinetic basis and comparison of experimental indices.多态性药物氧化:药代动力学基础及实验指标比较
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10
Nifedipine: kinetics and hemodynamic effects in patients with liver cirrhosis after intravenous and oral administration.硝苯地平:肝硬化患者静脉注射和口服后的动力学及血流动力学效应
Clin Pharmacol Ther. 1986 Jul;40(1):21-8. doi: 10.1038/clpt.1986.134.