一、前言所谓前体药物是指某药物经化学修饰,在体内被吸收后,酶或非酶地还原为活性物质(母体化合物),其目的是增加药物的水溶性或脂溶性,改善稳定性、吸收和持续性,并减少异味异臭以及减轻副作用。作为口服抗生素的前体药物,青霉素类的前体药物已经市售,而头孢菌素类的前体药物正处于研制中。本文报道富山化学公司正在开发中的T-2588的研制及其代谢。 I. Preface The so-called prodrug refers to a drug chemically modified, absorbed in the body, the enzyme or non-enzymatic reduction of the active substance (parent compound), its purpose is to increase the drug’s water-soluble or fat-soluble, improve stability , Absorption and persistence, and reduce offensive odor and reduce side effects. As a prodrug of oral antibiotics, prodrugs of penicillins are already on the market, while cephalosporin prodrugs are under development. This article reports the development and metabolism of T-2588 currently under development at Toyama Chemical Company.