前药的合理设计及应用

Rational Design of Prodrugs and Application

前体是指将有生物活性的药物分子经过修饰改造,加上前体基团,形成可以在体内被酶或化学反应激活的化学物质。前药通常没有生理活性,或者活性极低,但可以被酶解或经非酶解转化为具有生理活性的药物。前药可用来增加药物的溶解性,提高生物利用度,改善传递特性及药物动力学特性等。

Prodrug are the modification of biologically active drug molecules, together with prodrug groups, to form chemicals that can be activated by enzymes or chemical reactions in the body. Prodrugs are usually not physiologically active or have very low activity, but can be enzymatically or non-enzymatically converted into physiologically active drugs. Prodrugs can be used to increase the solubility of drugs, improve bioavailability, improve delivery properties and pharmacokinetic properties.