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目的:介绍灯盏花素吸收动力学与促进其吸收策略的研究进展。方法:分析近年相关文献,对灯盏花素及结构修饰物口服、鼻腔给药、肺部给药、经皮给药的吸收特性,以及如何促进吸收采取的措施进行总结。结果:水溶性和脂溶性差、MRP2的外排作用以及胃肠道的首过效应均是导致灯盏花素口服生物利用度低的重要原因。结论:增加水溶性或脂溶性、抑制外排以及采用微粒给药系统均能改善灯盏花素在小肠的吸收;鼻腔、肺部、经皮肤给药也是其可以选择的非侵入性全身治疗给药途径。
Objective: To introduce the research progress of breviscapine absorption kinetics and its absorption strategy. Methods: The related literatures in recent years were analyzed, and the absorption characteristics of breviscapin and its structure modifiers were summarized, including oral administration, nasal administration, pulmonary administration and transdermal administration, and how to promote absorption. Results: The poor water solubility and lipid solubility, the efflux of MRP2 and the first pass effect of gastrointestinal tract were all the important reasons for the low oral bioavailability of breviscapine. Conclusion: The addition of water-soluble or fat-soluble, inhibition of efflux and the use of particulate delivery systems can improve the Breviscapin absorption in the small intestine; nasal, pulmonary, transdermal administration is also its optional non-invasive systemic therapy way.