Clayton J P, Cole M, Elson S W, Ferres H, Hanson J C, Mizen L W, Sutherland R
J Med Chem. 1976 Dec;19(12):1385-91. doi: 10.1021/jm00234a007.
Lactonyl esters of ampicillin and other penicillins have been synthesized as prodrugs designed to improve the oral absorption of the parent penicillins. In general, the esters hydrolyzed rapidly in the presence of tissues including blood and certain of the esters were better absorbed than the parent penicillin. The phthalidyl ester of ampicillin [talampicillin (British Pharmacopoeia approved name), BRL 8988] was selected for extended studies. The compound was found to be well absorbed in various animal species and gave ampicillin serum concentrations in fasting human volunteers 2.5-3 times those obtained for ampicillin itself.
氨苄西林和其他青霉素的乳糖基酯已被合成为前药，旨在改善母体青霉素的口服吸收。一般来说，这些酯在包括血液在内的组织存在下会迅速水解，并且某些酯比母体青霉素吸收得更好。氨苄西林的邻苯二甲酰酯[酞氨苄西林（英国药典批准名称），BRL 8988]被选作进一步研究。发现该化合物在各种动物物种中吸收良好，在空腹的人类志愿者中产生的氨苄西林血清浓度是氨苄西林本身的2.5至3倍。
