本文以中药小分子为例对小分子药物的跨膜转运研究进展及方法进行了综述，并结合作者研究成果，对小分子药物跨膜转运与作用靶点进行了分析和探讨。目前，研究小分子转运的检测方法有HPLC、 LC/MS，还可以借助其荧光成像利用共聚焦技术进行观测。在研究过程中，确定小分子的转运方式的同时，也要探讨其外排方式，并要确定其有无代谢及其可能的代谢产物。对小分子药物的细胞跨膜转运研究将有助于确定小分子作用的靶点，有助于对其药理作用的探讨和阐释。

In this paper,a research progress on the transmembrane transport of small-molecular drugs,especially natural small-molecular drugs, was summarized.Combined with previous studies in our group,the details in transmembrane transport of small molecules were explained and discussed.Detection methods of transport of small molecules involved HPLC and LC/MS,and fluorescence imaging via confocal observation techniques.During the studies,transportations of small molecules needed to be determined,while efflux means also should be explored to confirm whether accompanying with metabolism and related metabolites.In conclusion,the studies of cell membrane transport of small-molecular drugs may help determine the targets of small molecules and elucidate their pharmacological actions.

科学技术部“重大新药创制”科技重大专项（2012ZX09102-201-008）：国家一类中药新药巴西苏木红素注射剂的研究，负责人：杜力军；清华大学创新基金（LF20103579）：小分子药物跨膜转运的研究，负责人：杜力军。