甲磺酸雷沙吉兰鼻用凝胶剂的制备及质量评价  

Preparation and in vitro quality evaluation of rasagiline mesylate nasal gel

作　　者：谷福根[1] 张艺馨[2] 王毅[1] 孟根达来[1] 吴春芝[1] GU Fu-gen ZHANG Yi-xin WANG Yi MENG Gen-da-lai WU Chun-zhi(Affiliated Hospital ,Inner Mongolia Medical University ,Hohhot 010050, China School of Pharmacy, Inner Mongolia Medical University, Hohhot 010110, China)

机构地区：[1]内蒙古医科大学附属医院,呼和浩特010050 [2]内蒙古医科大学药学院,呼和浩特010110

出　　处：《中国新药杂志》2017年第3期351-356,共6页Chinese Journal of New Drugs

摘　　要：目的:制备甲磺酸雷沙吉兰(rasagiline mesylate,RM)鼻用凝胶剂并对其进行质量评价。方法:以外观、涂展性以及释放度为评价指标,采用正交试验优选RM鼻用凝胶剂的处方及制备工艺;对所制备RM鼻用凝胶剂的外观、pH值、药物与防腐剂的含量、释放度以及有关物质等质量指标进行研究。结果:RM鼻用凝胶剂的最佳处方组成为:0.5%的RM,0.4%的卡波姆940,0.05%的尼泊金乙酯,20%的丙二醇,三乙醇胺及水适量;该制剂的理想pH值约为6.5;制剂的外观、pH值、RM与防腐剂的含量以及有关物质等质量指标均符合2010年版《中华人民共和国药典》有关要求。结论:RM鼻用凝胶剂组成合理,制备工艺简单,质量稳定可控,是一种有开发前景的经鼻给药新制剂。Objective：To prepare a nasal gel of rasagiline mesylate（RM） and further evaluate its in vitro quality. Methods：The formulation and preparation process of RM nasal gel were optimized with orthogonal test using appearance,spreading ability and in vitro release as the main evaluation indexes. The RM nasal gel was prepared and its quality items such as appearance,pH value,contents of the drug and preservative,in vitro release and related substances were then evaluated. Results：The optimal formulation of the RM nasal gel consisted of0. 5% RM,0. 4% carbopol 940,0. 05% ethylparaben,20% propanediol,and appropriate amount of triethanolamine and purified water. Its ideal pH value was about 6. 5. Furthermore,the quality items such as the appearance,pH value,contents of the drug and preservative and related substances of the preparation all conformed to the relevant quality requirements in China Pharmacopiea（2010）. Conclusion：The RM nasal gel may be a promising preparation for nasal delivery with reasonable formulation,simple preparation process and controllable quality.

关 键 词：甲磺酸雷沙吉兰 鼻用凝胶剂 处方筛选 正交试验 质量评价 

分 类 号：R971[医药卫生—药品]