桉叶油羟丙基-β-环糊精包合物-原位凝胶复合系统地制备与评价.PDFVIP

·药 剂· 桉叶油羟丙基-β-环糊精包合物-原位凝胶复合系统的制备与评价 冯瀚洲，胡春晖，朱春燕*( 中国医学科学院 北京协和医学院药用植物研究所，中草药物质基础与资源利用教育部重点实验室，北京 100193) 摘要：目的 制备桉叶油羟丙基-β-环糊精包合物原位凝胶复合给药系统，提高桉叶油的水溶解度，同时达到滞留病灶部 位且缓慢释放的效果。方法 采用水溶液搅拌法制备桉叶油羟丙基-β-环糊精包合物，以海藻酸钠制备空白离子敏感型原 位凝胶，将两者结合后对复合给药系统的体外溶蚀及体内滞留性进行评价。结果 桉叶油羟丙基-β-环糊精包合物的含油 率为(6.45±0.16)% ，包合率(77.42±1.78)% 。体外溶蚀实验表明，包合物原位凝胶复合系统的平均溶蚀率为 (44.62±2.07)mg·cm2 ·h1。体外溶蚀实验结果表明，复合系统在 24 h 溶蚀完全；荧光活体成像系统检测体内滞留性实验 结果表明，复合系统可在裸鼠肺部滞留 12 h 以上。结论 桉叶油羟丙基-β-环糊精包合物原位凝胶复合系统可达到局部 滞留并缓慢释放药物的目的。 关键词：桉叶油；羟丙基-β-环糊精包合物；海藻酸钠；原位凝胶；体外溶蚀；荧光活体成像 中图分类号：R943.4 文献标志码：A 文章编号：1007-7693(2012)02-0142-06 Study on Eucalyptus Oil Hydroxypropyl Cellulose -Cyclodextrin Inclusion Compound/In Situ Gel Combination Delivery System * FENG Hanzhou, HU Chunhui, ZHU Chunyan (The Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences Peking Union Medical College, Beijing 100193, China) ABSTRACT: OBJECTIVE To prepare hydroxypropyl cellulose-β-cyclodextrin (HP-β-CD) inclusion compound combined with sodium alginate in situ gel combination delivery system. And to improve the stability and water solubility of eucalyptus oil, which is a kind of volatile oil extracted from eucalyptus leaves, as well as to retain the drug in lungs of mice and to release it slowly. METHODS The method of agitation in water solution was applied to prepare HP-β-CD inclusion compound of eucalyptus oil, and sodium alginate was used to prepare ion-sensitive in situ gel. The combination delivery system obtained by adding the inclusion compound to the in situ gel followed by physically mixing. The combination deliver