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十二指肠内给药的地西泮在大鼠体内的药代动力学受中央淋巴成分的影响

The pharmacokinetics of intraduodenally administered diazepam in rats as influenced by composition of the central lymph.

作者信息

Lamka J, Jindrová O, Rudisar L, Kohoutek P, 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(5):441-8.

PMID:2533984
Abstract

Diazepam, a drug with hydrophobic properties, was used as a model for studying its distribution (after intraduodenal administration) into the central lymph of rats. The intestinal lymph, which prevails in the central lymph, was modified for the presence of total lipids (chylomicrons) by means of fasting, a normal or an artificial diet (olive oil). The lymphatic levels of diazepam exceeded the corresponding blood levels in the fed and oil-fed group; the levels were steady in the fasted group with the exception of the absorption phase of the curves. The kinetic parameters assessed in the blood and lymph of the individual groups obtained by mathematical evaluation of the concentration curves differed because of quantitative differences in the presence of chylomicrons in the lymph. Lymphatic bioavailability in comparison with i.v. administration was found to be substantially lower.

摘要

地西泮是一种具有疏水性的药物,被用作研究其(十二指肠内给药后)在大鼠中央淋巴中的分布模型。通过禁食、正常饮食或人工饮食(橄榄油),对中央淋巴中占主导的肠淋巴中总脂质(乳糜微粒)的存在情况进行了改变。在喂食组和喂油组中,地西泮的淋巴水平超过了相应的血液水平;在禁食组中,除曲线的吸收阶段外,水平保持稳定。通过对浓度曲线进行数学评估得出的各个组的血液和淋巴中的动力学参数因淋巴中乳糜微粒存在的数量差异而有所不同。与静脉注射给药相比,淋巴生物利用度明显较低。

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