目的:综述药物透过血脑屏障能力的评价方法。方法:通过查阅国内外相关文献资料,对药物血脑屏障通透性各种评价方法的特点进行分析。结果:体内评价可结合药理作用有效地评价药物的药效;体外评价有利于药物的机制性研究;数学模型可快速、简便的评价药物的通透性。结论:各种评价方法间具有一定的相关性,可有效地用于脑部疾病药物的设计与筛选。 OBJECTIVE: To summarize the evaluation of the drug’s ability to cross the blood-brain barrier. Methods: By referring to relevant literature at home and abroad, the characteristics of various evaluation methods of blood-brain barrier permeability were analyzed. Results: In vivo evaluation can be combined with the pharmacological effects of effective evaluation of drug efficacy; in vitro evaluation is conducive to the mechanism of drug research; mathematical model can quickly and easily evaluate drug permeability. Conclusion: There is a certain correlation between various evaluation methods, which can be effectively used in the design and screening of drugs for brain diseases.