复方伊维菌素和吡喹酮纳米乳的制备与质量评价  

Preparation and quality evaluation of ivermectin and praziquantel nanoemulsion

作　　者：汤佳莘 欧阳五庆[1] 吴小利[1] 

机构地区：[1]西北农林科技大学动物医学院,陕西杨凌712100

出　　处：《西北农林科技大学学报（自然科学版）》2014年第2期35-40,共6页Journal of Northwest A&F University(Natural Science Edition)

基　　金：陕西省重大科技创新专项(K332020916)

摘　　要：【目的】制备复方伊维菌素和吡喹酮纳米乳,并对其理化性质进行研究。【方法】依据伊维菌素和吡喹酮的溶解度,选择适宜的油相和表面活性剂;依据维持纳米乳体系稳定性的能力大小,筛选助表面活性剂;利用伪三元相图确定表面活性剂与助表面活性剂的质量比(Km值),筛选出复方伊维菌素和吡喹酮纳米乳的配方,并对复方纳米乳的载药量、稳定性、Zeta电位、粒径和安全性进行了分析。【结果】复方伊维菌素和吡喹酮纳米乳各组分的质量分数为:伊维菌素0.03%、吡喹酮5%、蓖麻油10.8%、聚氧乙烯氢化蓖麻油(RH-40)30%、丙二醇7.5%、蒸馏水46.67%。制备的复方伊维菌素和吡喹酮纳米乳稳定性良好,其中伊维菌素的质量浓度为0.3mg/mL,吡喹酮的质量浓度为48mg/mL。透射电子显微镜下观察到该纳米乳乳滴呈球状,平均粒径为15.8nm。小鼠急性经口毒性试验结果表明,该纳米乳的半数致死量(LD50)为3 207mg/kg,属低毒药剂。【结论】成功制备出了复方伊维菌素和吡喹酮纳米乳,该纳米乳是一种安全稳定的药剂。[Objective] This study prepared ivermectin and praziquantel nanoemulsion and investigated its physicochemical characteristics. [Method] Suitable oil phase and surfactant were selected based on the solubility of ivermectin and praziquantel. Suitable co-surfactant was selected based on the sustaining capaci- ty of nanoemulsion system. The pseudo ternary phase diagram was used to determine the ratio of surfactant to co-surfactant （Kin）. Then, the prescription was settled, and drug loading, stability, the zeta potential, particle size, and safety of the nanoemulison were analyzed. [Result] Compound ivermectin and praziquantel nanoemulsion was prepared and the mass fractions of ivermectin, praziquantel, castor oil, polyoxyethylene hydrogenated castor oil （RH-40）, propylene glycol, and distilled water were 0. 03%, 5%, 10. 8%,30%, 7.5% and 46.67% ,respectively. The nanoemulsion was stable with the ivermectin loading of 0.3 mg/mL and praziquantel loading of 48 mg/mL. The nanoemulsion presented as small spherical drops under Trans- mission electron microscope with an average diameter of 15.8 nm. The oral acute toxicity test to mice sug- gested that the nanoemulsion had low toxicity with the LDs0 of 3 207 mg/kg. [Conclusion] The prepared ivermectin and praziquantel nanoemulsion was a safe and stable drug.

关 键 词：伊维菌素 吡喹酮 复方纳米乳 稳定性 安全性 

分 类 号：S859.79[农业科学—临床兽医学]