伊维菌素纳米乳注射液的研制与质量安全性评价  

Preparation and Property Evaluation of Ivermectin Nanoemulsion for Injection

作　　者：刘根新[1,2] 张继瑜[3] 吴培星[3] 李剑勇[3] 刘英[1] 周绪正[3] 魏小娟[3] 牛建荣[3] 胡宏伟[1] 

机构地区：[1]甘肃农业大学,兰州730060 [2]甘肃畜牧工程职业技术学院,武威733006 [3]中国农业科学院兰州畜牧与兽药研究所,兰州730050

出　　处：《畜牧兽医学报》2011年第8期1161-1167,共7页ACTA VETERINARIA ET ZOOTECHNICA SINICA

基　　金：国家高技术研究发展计划(863计划)重大课题(2006AA10A203)

摘　　要：本研究旨在研制伊维菌素纳米乳注射液(5%)并对其理化性能、载药量、稳定性和急性毒性进行评价。采用伪三元相图法进行处方筛选,在常温下,以黏度、电导率、折光率、Z电位、平均粒径为指标考察纳米乳的理化性能;在不同的温度、光照和湿度条件下以药物含量为指标考察纳米乳的稳定性;采用HPLC法测定载药量,用小鼠灌胃的方法进行急性毒性研究。结果表明,该纳米乳在透射电镜下观察其乳滴呈球状,平均粒径为70 nm;不同温度、光照和湿度条件下含量无明显变化,稳定性良好;小鼠急性毒性试验表明该纳米乳注射液(0.1%)属于实际无毒。结果提示,本研究研制的伊维菌素纳米乳注射液(5%)制备简单,是一种质量稳定、安全性高的新制剂。This experiment was conducted to study the preparation of ivermectin nanoemulsion（5%） and its physicochemical properties,drug loading efficiency,stability and acute toxicity were evaluated.The physicochemical properties of ivermectin nanoemulsion was tested by the pseudoternary phase diagram method with the idex of viscosity,conductivity,refractive property,Z potentiometer and average diameter in normal temperature;The stability of ivermectin nanoemulsion was investigated with the idex of drug loading efficiency in different temperature,illumination and humidity;The acute toxicity was evaluated with the method of rat oral perfusion while the drug loading efficiency was detected by HPLC method.The results were as follows： 1）The ivermectin nanoemulsion was small spherical drops when observed by the electron microscopy and the average diameter was about 70 nm;2）The ivermectin nanoemulsion was stable in different temperature,illumination and humidity;3）The nanoemulsion（0.1%） was innoxious for mice when tested by the acute toxicity test.These results indicated that the preparation methods of ivermectin nanoemulsion（5%） was simple,and the preparation of ivermectin nanoemulsion was stable and with high safety quality.

关 键 词：伊维菌素 纳米乳 伪三元相图 性能评价 

分 类 号：S859.5[农业科学—临床兽医学]