辛鹅鼻用温敏原位凝胶的制备  

Preparation of Magnoliae Flos-Centipeda Herba thermosensitive nasal in situ gels

作　　者：袁佳敏[1] 黄星雨 周宇婷 杨琼梁 颜红[1] YUAN Jia-min;HUANG Xing-yu;ZHOU Yu-ting;YANG Qiong-liang;YAN Hong(School of Pharmacy,Hunan University of Chinese Medicine,Changsha 410208,China;Department of Pharmacy,Liuyang Manidpal Hospital of Traditional Chinese Medicine,Liuyang 410300,China)

机构地区：[1]湖南中医药大学药学院,湖南长沙410208 [2]浏阳市中医医院药剂科,湖南浏阳410300

出　　处：《中成药》2018年第12期2656-2662,共7页Chinese Traditional Patent Medicine

基　　金：湖南省教育厅科学研究项目(17K068);中药成药性与制剂制备湖南省重点实验室(湖南省科技厅平台建设项目)(2016TP1017)

摘　　要：目的制备辛鹅鼻用温敏原位凝胶。方法提取辛夷、鹅不食草挥发油后,制备复方提取物。以基质种类与用量、溶剂(1,2-丙二醇)与增溶剂(吐温-80)用量为影响因素,胶凝温度为评价指标,单因素试验优化制备工艺。然后,考察凝胶pH值、黏度、体外释药行为。结果最佳条件为2%复方提取物,0. 4%混合挥发油,基质15%泊洛沙姆407 (P407)和1%泊洛沙姆188 (P188),15%1,2-丙二醇,1%吐温-80,促渗透剂1,2-丙二醇,防腐剂0. 04%苯扎溴铵,胶凝温度(33. 5±0. 06)℃,pH值6. 1±0. 4,黏度平均增加速率(32～34℃) 2 484 m Pa·s/℃。凝胶体外释药行为符合Higuchi方程,药物释放率与凝胶溶蚀率之间的相关性较高。结论辛鹅鼻用温敏原位凝胶制备工艺简单,pH值、胶凝温度、黏度适宜,具有一定缓释作用,可满足鼻腔局部用药需求。AIM To prepare Magnoliae Flos-Centipeda Herba thermosensitive nasal in situ gels. METHODS The compound extract containing volatile oils was made from Magnoliae Flos and Centipeda Herba. With type and consumption of matrix,consumption of solvent(1,2-propanediol) and solubilizer(Tween-80) as influencing factors,gelation temperature as an evaluation index,single factor test was applied to optimizing the preparation process. Subsequently the gels had their pH value,viscosity and in vitro drug release behaviors investigated.RESULTS The optimial conditions were determined to be 2% compound extract,0. 4% mixed volatile oils,15% Poloxamer407(P407) and 1% Poloxamer188(P188) as matrices,15% 1,2-propanediol,1% Tween-80,1,2-propanediol as a penetration enhancer, 0. 04% benzalkonium bromide, the gelation temperature was(33. 5 ± 0. 06) ℃ with the pH value of 6. 1 ± 0. 4 and average viscosity increase rate of 2 484 m Pa·s/℃. The in vitro drug release behaviors of the gels accorded with Higuchi equation,and there existed a high correlation between rates of drug release and gels erosion. CONCLUSION The simple preparation process for Magnoliae Flos-Centipeda Herba thermosensitive nasal in situ gels produces an ideal topical nasal cavity medication in terms of appropriate pH value,gelation temperature,viscosity,and a certain sustained release.

关 键 词：辛夷 鹅不食草 鼻用温敏原位凝胶 制备 单因素试验 

分 类 号：R944[医药卫生—药剂学]