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新型抗炎/抗风湿药物氯那唑酸钙的合成及理化性质

[Synthesis and physico-chemical properties of lonazolac-Ca, a new antiphlogistic/antirheumatic agent].

作者信息

Rainer G, Krüger U, Klemm K

出版信息

Arzneimittelforschung. 1981;31(4):649-55.

PMID:6972771
Abstract

Calcium-[3-(p-chlorophenyl)-1-phenylpyrazole-4]-acetate (Lonazolac-Ca, active principle of Irritren) is a new antiinflammatory/antirheumatic agent whose synthesis and physico-chemical properties are described. The physical parameters measured (pKa, partition coefficient P, saturation concentration Cs, surface activity, protein binding) are held against the corresponding values of indomethacin, diclofenac, and phenylbutazone. The size of the permeability coefficient PM of the passive transport through artificial phospholipid collodion membranes as well as the invasion curves calculated from PM indicate a good absorption of lonazolac in man.

摘要

钙-[3-(对氯苯基)-1-苯基吡唑-4]-乙酸酯(氯那唑酸钙,伊瑞特林的活性成分)是一种新型抗炎/抗风湿药物,本文描述了其合成方法和理化性质。所测得的物理参数(pKa、分配系数P、饱和浓度Cs、表面活性、蛋白结合率)与吲哚美辛、双氯芬酸和保泰松的相应值进行了对比。通过人工磷脂火棉胶膜的被动转运渗透系数PM的大小以及根据PM计算出的侵入曲线表明氯那唑酸在人体中的吸收良好。

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