Lu Yang, Hao Bo, Wen Ran, Li Hui-Yun, Zhao Xue-Jiao, Du Shou-Ying
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China.
Zhongguo Zhong Yao Za Zhi. 2013 May;38(10):1510-2.
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) x 10(-3) min(-1), whereas the constant absorption rate of GE in XNJ-M was (2.16 +/- 0.21) x 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.
醒脑静（XNJ）是一种用于治疗急性中风的有效临床药物。与注射给药相比，其鼻腔给药具有更好的脑靶向性。因此，通过鼻腔给药，醒脑静微乳剂有助于解决大剂量、高浓度中药复方成分中不同极性成分的载药量问题，并减少对鼻黏膜的刺激。在本研究中，采用改良体积校正法和改进的大鼠原位鼻腔灌流模型比较不同醒脑静制剂中栀子苷的鼻腔吸收情况。结果表明，醒脑静-D中栀子苷（GE）的恒定吸收速率为（2.95±0.25）×10⁻³ min⁻¹，而醒脑静-M中GE的恒定吸收速率为（2.16±0.21）×10⁻³ min⁻¹。这表明不同醒脑静制剂中GE在大鼠鼻腔的吸收符合一级过程，可视为被动吸收。醒脑静-D中GE的吸收比醒脑静-M中快，这为醒脑静鼻腔制剂的开发提供了依据。
