前药是指在体外无活性,在体内经过化学或酶的作用转化成有活性的母体药物而发挥药理作用的化合物。应用前药技术能解决口服药物常见的缺点如水溶性和脂溶性不佳、首过效应强、药效持续时间短、毒副作用大以及口感差等。分别从提高生物利用度、提高靶向性及减小毒性等几个方面综述前药技术在口服药物研发中的应用情况。 Prodrugs are compounds that exhibit in vitro pharmacological effects that are inactive in vivo and are converted to active parent drugs by chemical or enzymatic action in the body. The use of prodrug technology can solve the common shortcomings of oral drugs such as poor water solubility and fat solubility, the first pass effect, short duration of drug efficacy, toxicity and side effects and poor taste. To summarize the application of prodrug technology in the research and development of oral drugs from several aspects such as improving bioavailability, improving targeting and reducing toxicity.