摘要
介绍了药物转运蛋白 (drugtransporter)在药物处置过程中的作用 ,探讨了其在新药开发中应用的可能性。通过对药物转运蛋白功能的了解和利用 ,可以增加口服药物的生物利用度 ,开发出对某些器官有靶向性的药物 ,或避免药物分布到某些器官中 ,从而提高药物的疗效 ,降低其的毒副作用 ;也可以控制药物的消除速度。在药物研发过程中可以通过两种手段达到上述目的 ,一是根据需要选择与某些转运蛋白有作用或没有作用的先导化合物 ,另一个则是使用转运蛋白抑制剂。在药物研发的初始阶段 ,就开始重视其药动学特性 ,这一观念近年来已被很多人所接受。对转运蛋白的深入认识和利用 ,建立研究药物转运特性的有效方法 。
The effects of drug transporters on the dr ug disposit ion were introduced and the possible utility in the developing of new drugs was discussed. The properties of the transporters can be used to increase the bioava ilability of the drugs,to deliver the drug to the target organ or avoid distrib ution to other organs,thereby increase the therapeutic effects and reduce the c hance of toxic effects. Forevermore,they can also be used to control the elimin ation speed of the compounds. There are two methods can be utilized to reach the purposes described as above,one is selecting a leading compound does or does n ot interact with special transporters,another is the use of inhibitors of some transporters. It is well accepted in recent years that the pharmacokinetic prope rties of a drug should be studied in its early stage of development. High-throu g hput screening systems established bases on transporters will be an efficient to ols in the new drug developments.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2003年第6期483-486,共4页
Journal of China Pharmaceutical University
