Ji Xun, Wang Jiang, Zhang Lei, Zhao Lin-Xiang, Jiang Hua-Liang, Liu Hong
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Yao Xue Xue Bao. 2013 May;48(5):621-34.
Based on the character of the molecular structure, the prodrugs of phosphates and phosphonates were divided into two categories. The first is the drug which contained the phosphate group, introducing protected groups to increase lipophilicity and improve bioavailability. The other one is the drug which had no phosphate group, introducing the phosphate group into molecules to enhance the solubility, regulate the distribution coefficient and enhance the drug-like property. This review focuses on the application of phosphates and phosphonates in drug research and development based on improvement of physico-chemical property, drug safety and the pharmacokinetics.
基于分子结构特点，磷酸盐和膦酸盐前药分为两类。第一类是含有磷酸基团的药物，引入保护基团以增加亲脂性并提高生物利用度。另一类是不含磷酸基团的药物，将磷酸基团引入分子中以提高溶解度、调节分配系数并增强类药性质。本综述基于物理化学性质、药物安全性和药代动力学的改善，重点介绍磷酸盐和膦酸盐在药物研发中的应用。
