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[一种蓝刺头碱制剂的药代动力学]

[Pharmcokinetics of an echinopsin preparation].

作者信息

Nakova G, Peĭkova R, Mikhaĭlova D, Chobanova I

出版信息

Eksp Med Morfol. 1978;17(1):18-27.

PMID:639743
Abstract

The purpose of the present work is to describe the pharmacokynetic characteristics of the preparation Ehinopsine, which represents N-methyl-gamma-chinoline and is synthetised in NIHFI during 1965. The experiments were carried out on male rats of the strain Wistar with weight of 170 to 190. The authors examine in dynamics plasma and tissues after single intraperitonenal administration of a dose of 30 mg/kg of body weight, plasma after venous administration of 25 mg/kg of body weight and 100 mg/kg of body weight and plasma and tissues-after oral administration of 100 mg/kg of body weight. The excretion of the preparation was examined also in bile, urine and feces after oral administration and there were metabolites in urine. On the basis of the experimental data after oral and venous treatment the respective mathematical models of distribution were determined as well as the basic pharmacokynetic parameters, characterizing the behaviour of Ehinopsine in the organism of rats. The obtained results gave a picture for good resorption of the preparation, quick distribution, weak excretion and wide biotransformation in the organism of the experimental animals.

摘要

本研究的目的是描述制剂埃希诺平的药代动力学特征,该制剂为N-甲基-γ-喹啉,于1965年在苏联医学科学院药物研究所合成。实验在体重170至190克的雄性Wistar大鼠身上进行。作者研究了单次腹腔注射30毫克/千克体重剂量后血浆和组织的动态变化,静脉注射25毫克/千克体重和100毫克/千克体重后血浆的变化,以及口服100毫克/千克体重后血浆和组织的变化。口服给药后还检测了制剂在胆汁、尿液和粪便中的排泄情况,尿液中有代谢产物。根据口服和静脉给药后的实验数据,确定了各自的分布数学模型以及基本药代动力学参数,这些参数表征了埃希诺平在大鼠体内的行为。所得结果表明该制剂在实验动物体内吸收良好、分布迅速、排泄较弱且生物转化广泛。

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