醒鼻微乳温敏凝胶中丹皮酚在大鼠鼻黏膜吸收研究.docVIP

醒鼻微乳温敏凝胶中丹皮酚在大鼠鼻黏膜吸收研究 　　摘要：目的 通过对醒鼻微乳温敏凝胶中丹皮酚的大鼠鼻黏膜吸收进行研究，评价该药的黏膜吸收情况和剂型选择的合理性。方法 通过大鼠鼻腔给药试验，对不同时间点丹皮酚的血药浓度进行测定。结果 大鼠鼻腔给予醒鼻微乳温敏凝胶后，丹皮酚的生物利用度为78.68%，达到最大浓度（Cmax）0.340 4 ?g/mL的时间为3 min，平均滞留时间为9.23 h；鼻腔给药的血药浓度达到Cmax后的变化情况与尾静脉注射丹皮酚类似；丹皮酚的血药浓度数据符合二室模型，权重为W=1。结论 醒鼻微乳温敏凝胶经鼻给药生物利用度较高，剂型选择合理。 　　关键词：醒鼻微乳温敏凝胶；丹皮酚；鼻腔吸收 　　DOI：10.3969/j.issn.1005-5304.2017.04.022 　　中图分类号：R285.5 文献标识码：A 文章编号：1005-5304（2017）04-0088-04 　　Study on Nasal Mucosa Absorption of Paeonol of Xingbi Microemulsion-based Thermo- sensitive Gel in Rats QIAO Li-fei1， SUN Cheng-tao1， LI Huang1， XU Wei1， CHU Ke-dan1， QUE Jin-hua1， ZHENG Jian2 （1. College of Pharmacy， Fujian University of Traditional Chinese Medicine， Fuzhou 350122， China； 2. Fujian University of Traditional Chinese Medicine， Fuzhou 350122， China） 　　Abstract： Objective To study the nasal mucosa absorption of paeonol of Xingbi microemulsion-based thermo-sensitive gel in rats； To evaluate the nasal mucosa absorption of medicine and the rationality of preparation form. Methods According to the nasal administration method， the blood medicine concentration of paeonol was determined at different time points. Results The nasal administration bioavailability of paeonol in Xingbi microemulsion-based thermo-sensitive gel was 78.68%， the plasma concentration reached the maximum （0.340 4 ?g/mL） after 3 min of administration， and the average residence time was 9.23 h. After reaching Cmax， The plasma concentration changed similar to intravenous administration of paeonol. The concentration data of paeonol in plasma was consistent with a two-compartment model， with a weight of 1. Conclusion Xingbi microemulsion-based thermo- sensitive gel has a higher bioavailability， and the preparation form was reasonable. 　　Key words： Xingbi microemulsion-based thermo-sensitive gel； paeonol； nasal absorption 　　醒鼻方是福建省人民?t院名老中医黄守林主任的鼻腔局部用药经验方，其主要组成为徐长卿、冰片等，具有疏风清热、开窍醒鼻等功效，临床和药理研究均表明其对变应性鼻炎疗效显著[1-6]。方中君药徐长卿具有祛风化湿、止痛止痒等功效，丹皮酚是其主要活性成分，具有抗炎、抗菌、抗变态反应、免疫调节和镇痛等作用[7-8]。本课题组将醒鼻方制