抗银屑病药物Y316外用制剂的筛选及处方研究  

Dosage form screening and formulation study of external preparations for a novel anti-psoriasis drug Y316

作　　者：靳茜婷 钟杰敏 张过 李琳丽[1] JIN Xiting;ZHONG Jiemin;ZHANG Guo;LI Linli(Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education,West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China;Guangxi Wuzhou Pharmaceutical（Group）Co.,LTD.,Wuzhou,Guangxi,543002 P.R.China)

机构地区：[1]四川大学华西药学院靶向药物与释药系统教育部重点实验室,四川成都610041 [2]广西梧州制药(集团)股份有限公司,广西梧州543002

出　　处：《华西药学杂志》2018年第4期346-350,共5页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81473140)

摘　　要：目的筛选新型抗银屑病药物Y316的最适剂型及处方。方法通过评价3种Y316外用制剂的质量，筛选最适剂型，考察相关质量检查指标及稳定性，筛选最佳处方。结果Y316乳膏剂优于其凝胶剂和软膏剂药物的溶解性、药效更适宜涂敷患处，为最适剂型。采用丙二醇、白凡士林、十八醇、十六醇、轻质石蜡、SDS、依地酸二钠、羟苯乙酯、单双硬脂酸甘油酯（130：160：30：30：100：5：0．5：1：20）制成的乳膏剂基质，质地细腻，黏稠度适宜，在离心试验和耐寒耐热试验中，外观和涂布性均无明显变化，性质稳定。结论最优处方是以丙二醇、白凡士林、轻质石蜡、单双硬脂酸甘油酯等辅料为基质制得的Y316乳膏剂，所用工艺简单、合理，乳膏剂的性质稳定，适用于该类药物的开发与利用。OBJECTIVE To screen the optimal dosage form and prescription of anti - psoriasis drug Y316. METHODS The optimal dosage form was screened by comparing the quality and pharmacodynamics of Y316 gel, ointment and cream. The quality control indexes and stability were evaluated for screening the best formulation. RESULTS Y316 cream was the optimal dosage from with better efficacy and was easier to dissolve and spread than other two dosage forms. Heat and freeze resistance and centrifugal test showed that the most appropriate base was consisted of propylene glycol, white vaseline, octadecanol, hexadecol, light paraffin, SDS, EDTA - 2Na, ethylparaben and glycerylmonostearate （130 ： 160 ： 30 ： 30 ： 100 ： 5 ： 0.5 ： 1 ： 20）. CONCLUSION The best formulation of Y316 is cream with propylene glycol ,white vaseline ,light paraffin, glyceryl monostearate and so on. It is reasonable and stable, and can be used for drug development and utilization.

关 键 词：银屑病 FLT3 乳膏剂 制备工艺 质量控制 稳定性 小分子药物 处方筛选 

分 类 号：R94[医药卫生—药剂学]