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用[2-(1,3-二十二烷酰氧基)-丙基]2-乙酰氧基苯甲酸酯(A-45474)对大鼠进行的药理学研究:一种胃刺激性可忽略不计的阿司匹林前药。

Pharmacological studies in the rat with [2-(1,3-didecanoyloxy)-propyl]2-acetyloxybenzoate (A-45474): an aspirin pro-drug with negligible gastric irritation.

作者信息

Carter G W, Young P R, Swett L R, Paris G Y

出版信息

Agents Actions. 1980 Jun;10(3):240-5. doi: 10.1007/BF02025942.

DOI:10.1007/BF02025942
PMID:6967685
Abstract

A triglyceride of aspirin, A-45474: [2-(1,3-didecanoyloxy)-propyl]2-acetyloxybenzoate, was developed to reduce the direct gastric irritant properties of aspirin. Studies in the rat show that oral administration of A-45474 produces anti-inflammatory activity comparable to aspirin with negligible gastric irritation. Compared with aspirin, plasma salicylate levels of A-45474 appeared less rapidly and were more sustained. It is concluded that incorporation of aspirin in the 2-position of a triglyceride bearing n-decanoyl groups in the 1- and 3-positions markedly reduces the gastric irritating properties of aspirin while maintaining its pharmacological effects.

摘要

阿司匹林的一种甘油三酯,A - 45474:[2 - (1,3 - 二癸酰氧基) - 丙基]2 - 乙酰氧基苯甲酸酯,被研发出来以降低阿司匹林直接刺激胃的特性。在大鼠身上进行的研究表明,口服A - 45474产生的抗炎活性与阿司匹林相当,且对胃的刺激可忽略不计。与阿司匹林相比,A - 45474的血浆水杨酸水平上升较慢且维持时间更长。得出的结论是,将阿司匹林引入到1位和3位带有正癸酰基的甘油三酯的2位上,能显著降低阿司匹林对胃的刺激特性,同时保持其药理作用。

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1
Pharmacological studies in the rat with [2-(1,3-didecanoyloxy)-propyl]2-acetyloxybenzoate (A-45474): an aspirin pro-drug with negligible gastric irritation.用[2-(1,3-二十二烷酰氧基)-丙基]2-乙酰氧基苯甲酸酯(A-45474)对大鼠进行的药理学研究:一种胃刺激性可忽略不计的阿司匹林前药。
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2
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