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沃克荷瘤大鼠中磺胺醋酰组织分布动力学的变化

Change in the kinetics of sulphacetamide tissue distribution in Walker tumor-bearing rats.

作者信息

Nadeau D, Marchand C

出版信息

Drug Metab Dispos. 1975 Nov-Dec;3(6):565-76.

PMID:1234
Abstract

The effect of Walker tumor on sulphacetamide distribution was studied in rats 21 days after tumor implantation in a hind leg. After oral administration of sulphacetamide (5 and 20 min), the concentration of the drug was found to be lower in the plasma and liver of tumor-bearing rats when compared with that of control group. However, 90 min after sulphacetamide administration, the concentration of the drug in these same tissues was found to be higher in tumor-bearing rats than in control animals. Whereas the tumor had no apparent effect on sulphacetamide concentration in the brain, drug concentrations in the fat tissue of tumor-bearing rats were constantly higher than those of control animals. These changes in sulphacentamide disposition kinetics could be explained in part by delay in gastrointestinal absorption of the drug. Contrary to what was observed after oral administration, constantly higher drug concentrations were found in the plasma of tumor-bearing rats after iv injection of sulphacetamide. Furthermore, the half-life of sulphacetamide in these same animals was much higher than in control animals. It is concluded that, in Walker tumor-bearing rats, there are changes in the kinetics of sulphacetamide which are functions of the route of administration of the drug.

摘要

在大鼠后腿植入沃克肿瘤21天后,研究了该肿瘤对磺胺醋酰分布的影响。口服磺胺醋酰后(5分钟和20分钟),发现荷瘤大鼠血浆和肝脏中的药物浓度低于对照组。然而,在给予磺胺醋酰90分钟后,发现荷瘤大鼠相同组织中的药物浓度高于对照动物。虽然肿瘤对大脑中磺胺醋酰的浓度没有明显影响,但荷瘤大鼠脂肪组织中的药物浓度始终高于对照动物。磺胺醋酰处置动力学的这些变化部分可以用药物胃肠道吸收延迟来解释。与口服给药后观察到的情况相反,静脉注射磺胺醋酰后,荷瘤大鼠血浆中的药物浓度始终较高。此外,磺胺醋酰在这些动物体内的半衰期远高于对照动物。得出的结论是,在荷沃克肿瘤的大鼠中,磺胺醋酰的动力学存在变化,这些变化是药物给药途径的函数。

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引用本文的文献

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The distribution and kinetics of sulphacetamide in leukaemic mice.磺胺醋酰在白血病小鼠体内的分布及动力学
Br J Pharmacol. 1976 Apr;56(4):423-9. doi: 10.1111/j.1476-5381.1976.tb07453.x.
2
P-aminosalicylate metabolism in cancer patients sensitive and resistant to chemotherapy.对化疗敏感和耐药的癌症患者的对氨基水杨酸盐代谢
Br J Cancer. 1977 May;35(5):580-6. doi: 10.1038/bjc.1977.91.