药用辅料抑制P_糖蛋白外排泵的研究进展_崔升淼.pdf

中国医药工业杂志 Chinese Journal of Pharmaceuticals 2012, 43(9) · 785 · 综述与专论 药用辅料抑制 P- 糖蛋白外排泵的研究进展 崔升淼，叶珍珍，张 建，廖华卫 (广东药学院中药学院，广东广州 510006) 摘要 ：P- 糖蛋白 (P-glycoprotein，P-gp) 是一种 ATP 依赖性药物外排泵，广泛分布在机体的各个组织中，可降低某些药 物的生物利用度，同时也是引起肿瘤细胞产生多药耐药的重要原因之一。一些药用辅料可抑制 P-gp 的外排作用，同时具 有低毒、无药理活性和安全性高的优点。本文着重综述了对 P-gp 外排具有抑制作用的 3 类药用辅料 ( 非离子型表面活性剂、 聚合物和脂质 ) 的研究进展，并简单介绍了 P-gp 的结构、功能和研究模型等。 关键词 ：药用辅料；P- 糖蛋白 ；外排 ；抑制；综述 中图分类号：TQ460.4 文献标志码：A 文章编号：1001-8255(2012)09-0785-05 Progress in Pharmaceutical Excipients with Function of Inhibition of P-glycoprotein Mediated Ef? ux CUI Shengmiao, YE Zhenzhen, ZHANG Jian, LIAO Huawei (School of Traditional Chinese Materia Medica, Guangdong Pharmaceutical University, Guangzhou 510006) ABSTRACT: P-Glycoprotein (P-gp) is an ATP-dependent ef? ux pump that is expressed in various tissues. It can reduce the bioavailability of some drugs, and it is also one of the important causes for multidrug resistance of tumor cells. Some pharmaceutical excipients can inhibit P-gp mediated ef? ux, and they simultaneously have the advantages of low toxicity, no pharmacological activity and high safety. This paper emphasizes on the progress of three kinds of pharmaceutical excipients (non-ionic surfactants, polymers and lipids) with the function of inhibition of P-gy mediated ef? ux. Meanwhile the structure, function and research model of P-gp are brie? y introduced. Key Words: pharmaceutical excipient; P-glycoprotein; ef? ux; inhibition; review P- 糖蛋白 (P-glycoprotein，P-gp) 是一种分 那韦 (saquinavir) 及地高辛 (digoxin) 等。因此，开 子量为 170 000 的跨膜糖蛋白，广泛分布在肝脏、 发 P-gp 抑制