PharmaCenter Bonn, University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D-53121 Bonn.
Chem Biodivers. 2009 Nov;6(11):2071-83. doi: 10.1002/cbdv.200900114.
Low water solubility and low bioavailability are frequent problems in drug development, particularly in the area of central nervous system (CNS) drugs. This short review describes selected prodrug approaches which have been developed to enhance the bioavailability of drugs, especially that of poorly soluble drugs. Some of the most successful drugs on the market are prodrugs. With a better understanding of active-transport processes at cell membranes in the gut as well as at the blood-brain barrier, the importance of prodrug approaches will further increase in the future. Prodrug approaches will already be considered in the early phase of drug discovery.
药物开发中经常会遇到水溶性差和生物利用度低的问题，尤其是在中枢神经系统（CNS）药物领域。本综述介绍了一些已被开发出来的前药方法，旨在提高药物的生物利用度，特别是那些水溶性差的药物。一些市场上最成功的药物都是前药。随着人们对肠道和血脑屏障中细胞膜主动转运过程的认识不断加深，前药方法的重要性在未来还将进一步提高。前药方法将在药物发现的早期阶段就被考虑在内。
