盐酸克仑特罗和沙丁胺醇两种β -拟制剂在狗体内组织分布的比较研究

Journal de pharmacologie Pub Date : 1986-10-01
M C Saux, J Girault, S Bouquet, J B Fourtillan, P Courtois
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引用次数: 0

摘要

特别是由于它们的物理化学性质,特别是它们的脂溶性,比较两种β 2拟交感神经制剂:克伦特罗和沙丁胺醇的组织分布是很有趣的。这项研究是在给狗直接静脉注射盐酸克仑特罗(5微克/公斤)和硫酸沙丁胺醇(50微克/公斤)后进行的。首次采用质谱法测定血浆中两种药物的药代动力学研究。经过三天的清洗后,重复了同样的经历。将动物处死,在肺、支气管、肌肉、心脏和脑组织样本中进行两种β 2拟交感神经的测定。瘦肉精和沙丁胺醇的组织分布是不同的,必须考虑在拟交感神经β 2活性的选择性因素。克仑特罗的神经中枢弥散性高于沙丁胺醇,但心脏分布对沙丁胺醇非常重要。
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[Comparative study of the tissue distribution of two beta-mimetics: clenbuterol and salbutamol in the dog].

Especially because of their physico-chemical properties, and in particular of their lipo-solubility, it was interesting to compare the tissue distribution of two beta 2 sympathomimetics: the clenbuterol and the salbutamol. The study was realised after a direct intravenous administration of clenbuterol chlorhydrate (5 micrograms/kg) and one of salbutamol sulfate (50 micrograms/kg) given to a dog. In a first time, the determination by mass-spectrometry of the two drugs in the plasma allows the pharmacokinetic study in dogs. After a three days wash out, this same experience was repeated. The animals are sacrificed and the assays of the two beta 2 sympathomimetics were effected in lung, bronchial, muscle, heart and brain tissue samples. The tissue distribution was different for clenbuterol and salbutamol and had to be considered as factors of selectivity in the sympathomimetic beta 2 activity. Nervous central diffusion of clenbuterol is higher than salbutamol but cardiac distribution is very important for salbutamol.

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