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淋巴成分对大鼠静脉注射地西泮药代动力学的影响

The pharmacokinetics of intravenously administered diazepam in the rat influenced by composition of the lymph.

作者信息

Lamka J, Jindrová O, Rudisar L, Gallová S, Kvĕtina J

机构信息

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University, Hradec Králové.

出版信息

Physiol Bohemoslov. 1989;38(3):259-66.

PMID:2528772
Abstract

Diazepam, a drug with hydrophobic properties, was used as a model drug for the study of its distribution after i.v. administration into the central lymph of the rat. The intestinal lymph, which prevails in the central lymph, was modified for the presence of total lipids chylomicrons by fasting and a normal or an artificial diet (olive oil). Lymphatic levels of diazepam in all three experimental conditions exceeded the corresponding blood levels, being lowest in the fasted group, higher in the normally fed animals and highest in the oil-fed group. Experimental blood and lymphatic data were subjected to pharmacokinetic analysis. The changes in the parameters were found to depend quantitatively upon the presence of chylomicrons in the lymph. Lymphatic availability of diazepam in the central lymph is stimulated by an increased content of the chylomicrons fraction of the lymph.

摘要

地西泮是一种具有疏水性的药物,被用作模型药物来研究其静脉注射后在大鼠中央淋巴中的分布情况。通过禁食以及给予正常饮食或人工饮食(橄榄油),改变了中央淋巴中占主导的肠淋巴中总脂质乳糜微粒的存在情况。在所有三种实验条件下,地西泮的淋巴水平均超过相应的血液水平,禁食组最低,正常喂食动物组较高,而喂食橄榄油组最高。对实验获得的血液和淋巴数据进行了药代动力学分析。发现参数的变化在数量上取决于淋巴中乳糜微粒的存在情况。淋巴中乳糜微粒部分含量的增加会刺激地西泮在中央淋巴中的淋巴可用性。

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