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口服给药后13-顺式视黄酸和N-(2-羟乙基)视黄酰胺在小鼠体内的处置情况。

Disposition of 13-cis-retinoic acid and N-(2-hydroxyethyl)retinamide in mice after oral doses.

作者信息

Kalin J R, Wells M J, Hill D L

出版信息

Drug Metab Dispos. 1982 Jul-Aug;10(4):391-8.

PMID:6126340
Abstract

The concentrations of 13-cis-retinoic acid and N-(2-hydroxyethyl)retinamide in serum and tissues from mice were measured after oral dosing with 10 mg/kg. Serum levels of the drugs reached their maxima within 15-30 min and then declined in an exponential fashion with t1/2 values of 19 min and 2.9 hr, respectively. Tissue levels of 13-cis-retinoic acid reached their maxima within 15-30 min, then declined exponentially with t1/2 values of 11-19 min. Tissue levels of N-(2-hydroxyethyl)retinamide reached their maxima within 30 min to 2 hr, then declined exponentially with t1/2 values of 2.1-4.7 hr. Longer t1/2 values were observed for both 13-cis-retinoic acid and N-(2-hydroxyethyl)retinamide in the bladder (51 min and 7.3 hr, respectively). Only small amounts of the unchanged retinoids were observed in bile and feces, and none was found in urine. Polar materials, however, were present in bile, feces, and urine.

摘要

以10mg/kg的剂量对小鼠进行口服给药后,测定了其血清和组织中13-顺式视黄酸和N-(2-羟乙基)视黄酰胺的浓度。药物的血清水平在15-30分钟内达到最大值,然后呈指数下降,13-顺式视黄酸和N-(2-羟乙基)视黄酰胺的半衰期分别为19分钟和2.9小时。13-顺式视黄酸的组织水平在15-30分钟内达到最大值,然后以11-19分钟的半衰期呈指数下降。N-(2-羟乙基)视黄酰胺的组织水平在30分钟至2小时内达到最大值,然后以2.1-4.7小时的半衰期呈指数下降。在膀胱中观察到13-顺式视黄酸和N-(2-羟乙基)视黄酰胺的半衰期更长(分别为51分钟和7.3小时)。在胆汁和粪便中仅观察到少量未变化的类视黄醇,尿液中未发现。然而,胆汁、粪便和尿液中存在极性物质。

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