Loftsson T, Kaminski J J, Bodor N
J Pharm Sci. 1981 Jul;70(7):743-9. doi: 10.1002/jps.2600700708.
Novel activated ester-type prodrugs of aspirin were designed and synthesized. The methylthiomethyl, methylsulfinymethyl, and methylsulfonylmethyl esters of aspirin (acetylsalicylic acid) were cleaved in vitro in plasma to form aspirin rather than the corresponding salicylates. In vitro studies using dogs indicated that at least one aspirin derivative, methylsulfinylmethyl-2-acetoxybenzoate, is a true aspirin prodrug since aspirin was detected in the blood after prodrug administration.
设计并合成了新型阿司匹林活化酯型前药。阿司匹林（乙酰水杨酸）的甲硫基甲酯、甲亚磺酰甲酯和甲磺酰甲酯在体外血浆中会裂解形成阿司匹林，而非相应的水杨酸盐。使用犬类进行的体外研究表明，至少有一种阿司匹林衍生物，即甲亚磺酰甲酯 -2- 乙酰氧基苯甲酸酯，是一种真正的阿司匹林前药，因为在前药给药后血液中检测到了阿司匹林。
