Ferruti P, Tanzi M C
Crit Rev Ther Drug Carrier Syst. 1986;2(2):175-244.
The preparation of polymeric derivatives of drugs, in which drug moieties are covalently linked to polymeric or oligomeric matrices, in such a way that they can be released at the site of action, is one of the most promising ways to achieve results which often can be hardly obtained by other means, such as, for instance, better adsorption by some ways of administration (e.g., oral administration), preferential localization in the body, and longer duration of activity. The aim of this review is to provide an up-to-date picture of the state of art in this field. The synthetic aspects of the preparation of polymeric derivatives of drugs will be discussed, with special emphasis on general methods. The main criteria for selecting a particular type of matrix, and a particular bond between drug and matrix, in order to achieve a given purpose, will be also discussed. The main pharmacological results so far obtained by this technique will be emphasized.
药物聚合物衍生物的制备是最具前景的方法之一，其中药物部分通过共价键连接到聚合物或低聚物基质上，以便它们能够在作用部位释放，而这样的效果往往很难通过其他方式实现，例如，通过某些给药途径（如口服给药）实现更好的吸附、在体内的优先定位以及更长的活性持续时间。本综述的目的是提供该领域的最新技术现状。将讨论药物聚合物衍生物制备的合成方面，特别强调通用方法。还将讨论为实现特定目的而选择特定类型基质以及药物与基质之间特定键合的主要标准。将重点介绍迄今为止通过该技术获得的主要药理学结果。
