中国中药杂志

2013, v.38(10) 1510-1512

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醒脑静滴鼻液与醒脑静微乳中栀子苷大鼠在体鼻循环吸收比较研究
Comparative study on rat in situ nasal absorption of geniposide of Xingnaojing nasal drop and Xingnaojing microemulsion

陆洋;郝博;温然;李慧云;赵雪姣;杜守颖;
LU Yang1,HAO Bo2,WEN Ran1,LI Hui-yun1,ZHAO Xue-jiao1,DU Shou-ying1(1.School of Chinese Pharmacy,Beijing University of Chinese Medicine,Beijing 100102,China; 2.Chinese Pharmacopoeia Commission,Beijing 100061,China)

摘要(Abstract):

醒脑静是临床用于治疗脑中风急性期的有效药物,与注射给药相比,醒脑静鼻腔给药具有显著的脑靶向性,将醒脑静制成微乳鼻腔给药可以解决大剂量高浓度中药不同极性复方成分的载药问题并能够降低对鼻黏膜的刺激性。该研究以体积校正法,采用改良的大鼠在体鼻循环模型比较醒脑静不同制剂中有效成分栀子苷大鼠鼻腔吸收特性。结果表明,醒脑静滴鼻液中栀子苷吸收速率常数为(2.95±0.25)×10-3min-1,醒脑静微乳中栀子苷吸收速率常数为(2.16±0.21)×10-3min-1,醒脑静不同制剂中栀子苷的大鼠鼻腔吸收符合一级速率过程,为被动吸收,醒脑静滴鼻液中栀子苷的鼻腔吸收较醒脑静微乳快,为醒脑静鼻用制剂的开发提供了一定的依据。
Xingnaojing(XNJ) is an effective clinical drug used to treat acute stroke.Compared with injection administration,its nasal administration has better brain targeting.Therefore,through nasal administration,XNJ microemulsion could help solve the drug load of compound components of different polarities contained in large-dose and high-concentration traditional Chinese medicines,and reduce irritation to nasal mucosa.In this study,the modified volume correction method and the improved rat in situ nasal perfusion model were adopted to compare the nasal absorption of geniposide contained in different XNJ preparations.The results showed that the constant absorption rate of geniposide(GE) in XNJ-D was(2.95±0.25)×10-3 min-1,whereas the constant absorption rate of GE in XNJ-M was(2.16±0.21)×10-3 min-1.This indicated that the rat nasal absorption of GE in different XNJ preparations complied with the first-order process and could be considered as passive absorption.GE in XNJ-D was absorbed faster than that in XNJ-M,which provided basis for the development of nasal preparations of XNJ.

关键词(KeyWords): 醒脑静;滴鼻液;微乳;栀子苷;大鼠在体鼻循环
Xingnaojing(XNJ);nasal drop;microemulsion;geniposide(GE);in situ rat nasal perfusion

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基金项目(Foundation): 国家自然科学基金项目(81073057);国家自然科学基金青年科学基金项目(81102816)

作者(Author): 陆洋;郝博;温然;李慧云;赵雪姣;杜守颖;
LU Yang1,HAO Bo2,WEN Ran1,LI Hui-yun1,ZHAO Xue-jiao1,DU Shou-ying1(1.School of Chinese Pharmacy,Beijing University of Chinese Medicine,Beijing 100102,China; 2.Chinese Pharmacopoeia Commission,Beijing 100061,China)

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