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氘标记辅酶Q10在人体中的药代动力学研究。

Pharmacokinetic study of deuterium-labelled coenzyme Q10 in man.

作者信息

Tomono Y, Hasegawa J, Seki T, Motegi K, Morishita N

出版信息

Int J Clin Pharmacol Ther Toxicol. 1986 Oct;24(10):536-41.

PMID:3781673
Abstract

The pharmacokinetics of coenzyme Q10 (CoQ10) in man was studied by utilizing deuterium-labelled coenzyme Q10 (d5-CoQ10). The absence of an isotope effect in the disposition of d5-CoQ10 in man was confirmed from the plasma concentration time curves after simultaneous oral dosing of d5-CoQ10 and unlabelled CoQ10. After oral administration of 100 mg of d5-CoQ10 to 16 healthy male subjects, the mean plasma CoQ10 level attained a peak of 1.004 +/- 0.370 micrograms/ml at 6.5 +/- 1.5 h after administration, and the terminal elimination half-life was 33.19 +/- 5.32 h. In most of the subjects, plasma d5-CoQ10 showed a second peak at 24 h after dosing. This unusual plasma level curve was well described by a newly proposed compartment model based upon the assumption that absorbed CoQ10 is taken up by the liver and then transferred mainly to VLDL and redistributed from the liver to the systemic blood.

摘要

利用氘标记的辅酶Q10(d5-CoQ10)研究了辅酶Q10(CoQ10)在人体中的药代动力学。在同时口服d5-CoQ10和未标记的CoQ10后,根据血浆浓度-时间曲线证实了人体中d5-CoQ10处置过程中不存在同位素效应。对16名健康男性受试者口服100mg d5-CoQ10后,给药后6.5±1.5小时血浆CoQ10平均水平达到峰值1.004±0.370μg/ml,终末消除半衰期为33.19±5.32小时。在大多数受试者中,血浆d5-CoQ10在给药后24小时出现第二个峰值。基于吸收的CoQ10被肝脏摄取然后主要转移至极低密度脂蛋白(VLDL)并从肝脏重新分布至全身血液这一假设,一种新提出的房室模型很好地描述了这种异常的血浆水平曲线。

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