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0.3 mg/mL,吡喹酮的质量浓度为48 mg/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15.8 nm。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3 207 mg/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。 |
关键词: 伊维菌素 吡喹酮 复方纳米乳 稳定性 安全性 |
DOI: |
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基金项目:陕西省重大科技创新专项(K332020916) |
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Preparation and quality evaluation of ivermectin and praziquantel nanoemulsion |
TANG Jia-xin,OUYANG Wu-qing,WU Xiao-li
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Abstract: |
【Objective】This study prepared ivermectin and praziquantel nanoemulsion and investigated its physicochemica1 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 capacity of nanoemulsion system.The pseudo ternary phase diagram was used to determine the ratio of surfactant to co-surfactant (Km).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 Transmission electron microscope with an average diameter of 15.8 nm.The oral acute toxicity test to mice suggested that the nanoemulsion had low toxicity with the LD50 of 3 207 mg/kg.【Conclusion】The prepared ivermectin and praziquantel nanoemulsion was a safe and stable drug. |
Key words: ivermection praziquantel nanoemulsion compound stability safety |