韩国柱, 苏成业, 张毅. 石吊兰素在大鼠体内的吸收、分布和消除以及血浆药物浓度与降压效应的关系J. 药学学报, 1982, 17(8): 572-577.
引用本文: 韩国柱, 苏成业, 张毅. 石吊兰素在大鼠体内的吸收、分布和消除以及血浆药物浓度与降压效应的关系J. 药学学报, 1982, 17(8): 572-577.
HAN Guo-zhu, SU Cheng-ye , ZHANG Yi, . THE ABSORPTION, DISTRIBUTION AND ELIMINATION OF NEVADENSIN IN THE RAT, AND THE RELATIONSHIP BETWEEN PLASMA CONCENTRATION OF THE DRUG AND ITS HYPOTENSIVE EFFECTJ. Acta Pharmaceutica Sinica, 1982, 17(8): 572-577.
Citation: HAN Guo-zhu, SU Cheng-ye , ZHANG Yi, . THE ABSORPTION, DISTRIBUTION AND ELIMINATION OF NEVADENSIN IN THE RAT, AND THE RELATIONSHIP BETWEEN PLASMA CONCENTRATION OF THE DRUG AND ITS HYPOTENSIVE EFFECTJ. Acta Pharmaceutica Sinica, 1982, 17(8): 572-577.

石吊兰素在大鼠体内的吸收、分布和消除以及血浆药物浓度与降压效应的关系

THE ABSORPTION, DISTRIBUTION AND ELIMINATION OF NEVADENSIN IN THE RAT, AND THE RELATIONSHIP BETWEEN PLASMA CONCENTRATION OF THE DRUG AND ITS HYPOTENSIVE EFFECT

  • 摘要: 石吊兰素混悬剂大鼠肠袢或灌胃给药吸收甚差;溶液剂肠袢注入后吸收快而完全,但灌胃后吸收不良。静脉注射后5分钟以肝脏、血浆含量最高,淋巴、肺、心、脑、肾、脾次之,脂肪、肌肉、睾丸最低。按平衡透析法测得本品血浆蛋白结合率为51.3±2.2%(X±SD,下同)。本品可经尿、粪和胆汁排泄。石吊兰素体内代谢旺盛,尿中除其葡萄糖醛酸结合物及硫酸结合物外,尚发现一种极性较大的石吊兰素代谢产物。狗静脉恒速滴注石吊兰素后的血浆药物浓度与其降压效应之间基本呈平行关系,不同狗的最大降压效应与该时血浆药物浓度密切相关。

     

    Abstract: By means of polyamide TLC and UV spectrophotometry the following results were obtained:The absorption of suspension and aqueous solution of nevadensin from rat GI tract following intragastric administration was poor, being poorer than the former preparation.Five minutes after iv administration, highest levels were found in liver and plasma; moderate in lymphatic tissue, lungs, heart, brain, kidneys, and spleen; and lowest in adipose tissue, muscle, and testis. The drug-plasma protein binding rate was found to be 51.3±2.2% (X±SD) using equilibrium dialysis method. In rats, the drug was excreted in urine, bile and faeces.The drug was metabolized rapidly and extensively in rats and mice. In the urine, in addition to nevadensin glucuronide and sulfate, there was Still a more polar metabolite with flavonoid structure similar to nevadensin.The hypotensive effect of the drug in dogs after iv infusion at a constant rate was found to parallel with its plasma level. In addition, the maximal hypotensive effect of the drug for each dog closely correlated with the corresponding plasma level.

     

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