药物化学和生物利用度控制

MEDICINAL CHEMISTRY AND BIOAVAILABILITY MANIPULATIONS

目的 :就 2 1世纪药物化学所关注的 4个问题 ,着重综述药物化学对生物利用度控制的意义。方法 :以实例说明。结果 :药物化学方法有助于防止药物的首过代谢 ,提高其生物利用度 ;获得部位专一传输药物 ;获得部位专一生物活化药物 ;肽类的前药衍生物 ,以克服肽类的传输障碍 ;用大分子载体作为药物寻靶的工具。结论 :是推出新药的简易途径。

OBJECTIVE:The 4 aspects of medicinal chemistry for 21st century was followed with great interest.One of them was bioavailability manipulations, and its significance was reviewed mainly.METHODS: It was discribed with theory and examples.RESULTS: these methods were helpful for (1) preventing first pass metabolism,and raising drug bioavailability;(2) gaining the site-specific delivery drugs;(3) gaining the site specific bioactivation drugs;(4)prodrug derivatives of peptides,overcoming their poor delivery characteristics;(5) macromolecular carriers for drug targeting.CONCLUSION: It is a easier way to present the new drugs.