大鼠体内地西泮和去甲基地西泮的淋巴生物利用度。

Lymphatic bioavailability of diazepam and desmethyldiazepam in the rat.

作者信息

Lamka J, Jindrová O

机构信息

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles Univérsity, Hradec Králové, Czech Republic.

出版信息

Physiol Res. 1996;45(1):23-9.

PMID:8884920

Abstract

The lymphatic bioavailability (FL) of diazepam (DZ) and its major metabolite desmethyldiazepam (DDZ) was studied. DZ was administered in intravenous and intraduodenal boluses, and in intravenous infusion in three groups of rats with different total lipid (TL) content in the central lymph. The effect of a) different lipophilicity of DZ and DDZ, b) lymphatic TL content, and c) route of DZ administration on FL was determined. It was found that a) FL values of DZ exceeded the FL values of DDZ and b) FL values of DZ increased with increasing TL content in the lymph (an opposite relation was found in DDZ), and c) the highest FL value of DZ + DDZ sum after intravenous bolus administration was attained contrary to the lowest one after intraduodenal bolus administration.

摘要

研究了地西泮（DZ）及其主要代谢产物去甲基地西泮（DDZ）的淋巴生物利用度（FL）。将DZ以静脉推注、十二指肠推注以及静脉输注的方式给予三组大鼠，这三组大鼠中央淋巴中的总脂质（TL）含量不同。确定了以下因素对FL的影响：a）DZ和DDZ不同的亲脂性；b）淋巴中的TL含量；c）DZ的给药途径。结果发现：a）DZ的FL值超过了DDZ的FL值；b）DZ的FL值随着淋巴中TL含量的增加而升高（在DDZ中发现的情况相反）；c）静脉推注给药后DZ + DDZ总和的FL值最高，与十二指肠推注给药后的最低值相反。