利培酮鼻用凝胶剂的制备及质量评价  

Preparation and in Vitro Quality Evaluation of Risperidone Nasal Gel

作　　者：谷福根[1] 马维娜[2] 王毅[1] 解红霞[1] 孟根达来[1] 吴春芝[1] 张艺馨[2] 

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：《中国药学杂志》2016年第6期468-472,共5页Chinese Pharmaceutical Journal

基　　金：内蒙古自然科学基金资助项目(2015MS(LH)0801);内蒙古医科大学科技百万工程项目(YKD2014KJBW012)

摘　　要：目的制备利培酮(risperidone,RIS)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,采用正交实验优选利培酮鼻用凝胶剂的处方及制备工艺;对所制备利培酮鼻用凝胶剂的外观、p H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。结果利培酮鼻用凝胶剂的最佳处方组成为:0.5%的利培酮,0.35%的卡波姆940,0.5%的三氯叔丁醇,20%的丙二醇,15%的DM-β-CD以及适量水;该制剂的理想p H值约为6.0;制剂的外观、p H值、利培酮与防腐剂的含量以及有关物质等质量指标均符合2010年版《中国药典》有关要求。结论利培酮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 risperidone （RIS） and evaluate its in vitro quality. METHODS The formulation and preparation process of RIS nasal gel were optimized with orthogonal test using appearance, spreading ability and in vitro release as main evaluation indexes. The quality items of the optimized RIS nasal gel such as appearance, pH value, contents of RIS and preservative, in vitro release and related substances were then evaluated. RESULTS The optimal formulation of the RIS nasal gel consisted of 0.5% RIS, 0. 35% carbopol 940, 0.5% chlorobutanol, 20% propanediol and 15% DM-β-CD and appropriate amount of purified water. Its ideal pH value was about 6.0. Furthermore, the quality items such as the appearance, pH value, contents of RIS and preservative, in vitro release and related substances of the preparation all conformed to the relevant quality requirements in China Pharmacopiea （2010）. CONCLUSION The RIS nasal gel will be a promising new preparation for nasal administration due to its reasonable formulation, simple preparation process and controllable quality.

关 键 词：利培酮 鼻用凝胶剂 处方筛选 正交实验 质量评价 

分 类 号：R944[医药卫生—药剂学]