卡维地洛鼻用微乳凝胶的制备及性质考察  

Preparation and Properties Study of Carvedilol Microemulsion-based Nasal Gels

作　　者：张爱武[1] 张友智[1] 

机构地区：[1]武汉科技大学附属天佑医院,武汉430064

出　　处：《中国药房》2016年第28期3992-3995,共4页China Pharmacy

摘　　要：目的:制备卡维地洛鼻用微乳凝胶,考察其性质。方法:通过溶解度和伪三元相图筛选微乳处方的表面活性剂、表面活性剂-助表面活性剂比例(Km)和油相;以胶凝温度、凝胶强度、p H、黏附力和外观筛选凝胶基质泊洛沙姆和卡波姆的用量。考察所制卡维地洛鼻用微乳凝胶的主药含量、体外释放度、凝胶稳定性和纤毛毒性。结果:微乳的乳化剂为聚山梨酯80,聚山梨酯80-二乙二醇单乙基醚的Km为1∶1,油相为油酸聚乙二醇甘油酯,凝胶基质为19%的泊洛沙姆和1%的卡波姆。所制卡维地洛鼻用微乳凝胶的胶凝温度为(33.4±0.4)℃,凝胶强度为(37.5±1.2)s,p H为(5.71±0.03),黏附力为(64.4±0.5)mg/cm2,外观为白色透明状(n=5),主药含量为99.48%(n=3);8 h体外累积释放度为87.11%(n=5);离心、低温、高温、光照下的RSD均小于5%且无分层、破乳现象(n=3);纤毛毒性与生理盐水比较无差异,符合用药要求。结论:所制备的卡维地洛微乳凝胶剂具有性质稳定、纤毛毒性低、可生物黏附的特点,较片剂释放完全,符合鼻用制剂标准。OBJECTIVE： To prepare Carvedilol microemulsion-based nasal gels, and to investigate its properties. METHODS： The surfactant, the ratio of surfactant to cosurfactant （Km） and oil phase of microemulsion prescription were screened by using solubility and pseudo-ternary phase diagram. The amounts of gel matrix as poloxamer and carbomer were screened by using gelation temperature, gel strength, pH, adhesion and appearance. The nasal gels was inspected in respects of the content of main component, release rate in vitro, gel stability and the cilia toxicity. RESULTS： The emulsifier was tween-80; Km of tween-80-diethylene glycol monoethyl ether was 1：1; oil phase was labrafil M-1944; gel matrix were 19% poloxamer and 1% carbomer. The parameters of prepared nasal gel were as follows as gelation temperature of （33.4 ± 0.4） ℃, gel strength of （37.5 ± 1.2） s, pH of （5.71 ± 0.03）, adhesion of （64.4 ± 0.5） mg/cm2, white transparent appearance （n=5）. The content of main component was 99.48% （n= 3）, and 8 h accumulative release rate in vitro was 87.11% （n=5）. RSDs were all lower than 5% and no stratification or demulsification was found under the condition of centrifugation, low temperature, high temperature and light （n=3）. There was no difference in cilia toxicity and normal saline, and they conformed to claim of drug use. CONCLUSIONS： Prepared Carvedilol microemulsion gels show the characteristics of quality stabilization, low cilia toxicity and biological adhensive. Prepared gels can be released completely compared to tablet and in line with the standard of nasal preparations.

关 键 词：卡维地洛 微乳 伪三元相图 鼻用凝胶 体外释放度 

分 类 号：R943[医药卫生—药剂学]