中药经鼻递药研究.docVIP

中药经鼻递药的研究 　　[摘要]中药经鼻给药历史悠久。现代研究表明，与其他给药途径相比，鼻腔给药吸收迅速、起效快、生物利用度高、脑靶向性好，在无创性递药入脑方面具有突出的优势。然而目前中药经鼻递药的研究尚不够深入。课题组近年来以治疗脑中风的“醒脑静”和“通窍散瘀方”为模型药物，对中药经鼻给药后不同性质成分的体内药物动力学进行了系统研究;以MDCK/MDCK-MDR1细胞模拟血脑屏障，对生理、病理条件下的药物透过行为进行了研究，并从分子生物学角度对复方中芳香开窍药的促透机制进行了探索，证实了复方配伍的合理性和优越性;在此基础上，课题组制备了载药量大、刺激性小的鼻用微乳，以药动学行为和荧光成像实验对微乳不同途径给药的生物利用度和靶向性进行了评价。在刺激性研究方面，课题组采用消化法-免疫磁珠法获得了高纯度的人鼻黏膜上皮细胞（HNEC），对药物的鼻黏膜刺激性进行了评价;以单次及多次给药黏膜的刺激性及可恢复性为指标对鼻用制剂的刺激性进行了初步评价。该文拟对上述研究成果进行综述，为中药经鼻递药的进一步研究提供参考。 　　[关键词]经鼻递药;入脑机制;醒脑静;通窍散瘀 　　Main progress on intranasal administration of 　　traditional Chinese medicine 　　LI Peng-yue， DU Shou-ying*， YANG Bing 　　（School of Chinese Materia Medica， Beijing University of Chinese Medicine， Beijing 100102， China） 　　[Abstract]Traditional Chinese medicine has a long history of intranasal administration. Compared with the other administration routes， intranasal administration has the benefits of fast absorption， high bioavailability， high brain-targeting and non-invasive. In the past few years we take ″Xingnaojing″ and ″Tongqiao Sanyu formula″ as model drug and studied pharmacokinetics of effective components of different polarities. MDCK/MDCK-MDR1 cells were used to simulate blood brain barrier to study the permeate behaviors of different drug and the mechanism of enhancing effects of aromatic medicine. Then a microemulsion （modified by mPEG2000-PLA） was prepared for intranasal administration， and the pharmacokinetics and investigated tissue distribution were studied by fluorescence imaging. The irritation of the drug and different preparations were studied on human nasal epithelial cell （HNEC） cell and living animals. In this paper， we reviewed the achievements and hope that it can provide constructive suggestions for the future research. 　　[Key words]intranasal administration; mechanism of brain delivery; Xingnaojing; Tongqiao Sanyu formula 　　doi：10.4268/cjcm 　　鼻腔递药是指将药物纳入鼻中，经鼻黏膜吸收而发挥局部或全身治疗或预防作用的一种给药方式。 　　中药经鼻给药有着悠久的历史，早在东汉时期，《金匮要略》中即有“薤捣汁，灌鼻中”、“吹皂荚末鼻中”救卒死的记载。此后，