柴黄鼻腔即型凝胶剂的制备与评价  

Preparation and Evaluation of Intranasal in situ Gel of Bupleuri Radix Volatile Oil and Baicalin

作　　者：刘婷婷 郭朋程[1] 刘婧昕 秦晶 蒋新国 傅超美 王建新[1] LIU Ting-ting;GUO Peng-cheng;LIU Jing-xin;QIN Jing;JIANG Xin-guo;FU Chao-mei;WANG Jian-xin(Key Laboratory of Smart Drug Delivery of the Ministry of Education,School of Pharmacy,Fudan University,Shanghai 201203,China;School of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;School of Pharmacy,Heilongjiang University of Chinese Medicine,Harbin 150040,China)

机构地区：[1]复旦大学药学院智能化递药教育部重点实验室,上海201203 [2]成都中医药大学药学院,成都611137 [3]黑龙江中医药大学药学院,哈尔滨150040

出　　处：《四川大学学报（医学版）》2021年第4期585-591,共7页Journal of Sichuan University(Medical Sciences)

基　　金：国家重大新药创制科技重大专项(No.2018ZX09721003-009-010);上海市科技支撑计划项目(No.17401902000)资助。

摘　　要：目的制备含有柴胡挥发油与黄芩苷有效组分的鼻腔给药温度/离子双敏感即型凝胶剂。方法以泊洛沙姆407与去乙酰结冷胶为凝胶基质,10%Pharmasolve与2%聚山梨酯-80为增溶剂,0.8%三乙醇胺为pH调节剂,制备柴黄鼻用即型凝胶鼻腔剂,对制剂外观、相转换温度、黄芩苷释放性能等进行研究,并采用大鼠干酵母致热模型和小鼠耳廓肿胀炎症模型进行药效学评价。结果凝胶剂的相转换温度为36℃,黄芩苷从中的释放具有明显的缓释特征,符合零级动力学方程。大鼠干酵母高热模型和小鼠二甲苯耳廓肿胀炎症模型实验结果显示凝胶剂具有显著的解热和抗炎效果,且均显著优于空白基质和柴黄颗粒对照组。纤毛毒性实验结果显示凝胶剂对蟾蜍上颚黏膜纤毛无明显毒性。结论所制备的柴黄即型凝胶剂具有速效、高效、长效的特点,具有进一步应用开发的前景。Objective To prepare and evaluate a new formulation of thermosensitive and ion-sensitive in situ gel for nasal administration,using the volatile oil of Bupleuri radix and baicalin,the effective component extracted from Scutellariae radix.Methods Formulation of in situ nasal gel of Bupleuri radix volatile oil and baicalin was prepared by using poloxamer 407 and deacetylated gellan gum as the gel base,10%pharmasolve and 2%polysorbate 80 as the solubilizer,and 0.8%triethanolamine as the pH regulator.The physical appearance,phase transition temperature,and baicalin release performance of the prepared gel were examined.The pharmacodynamic evaluation was done with the rat fever model developed with dry yeast and the mouse auricle swelling inflammation model.Results The phase transition temperature of the gel was optimized to be 36℃.The release of baicalin from the gel showed obvious features of sustained release,which accorded well the zero-order kinetics equation.The results of experiments with the rat dry yeast fever model and the mouse xylene auricle swelling inflammation model showed that the gel had significant antipyretic and antiinflammatory effects that were significantly better than those of the groups treated with the blank gel base and the Bupleuri radix and Scutellariae radix granule.Results from the cilia toxicity test showed that the gel did not have obvious toxic effect on toad palate mucosal cilia.Conclusion The in situ nasal gel of Bupleuri radix volatile oil and baicalin prepared in the study had a rapid onset time,high efficiency,and prolonged release of active ingredients,thus showing promises for further applicational development.

关 键 词：柴胡-黄芩药对 柴胡挥发油 黄芩苷 即型凝胶 鼻腔给药 

分 类 号：R283.6[医药卫生—中药学]