| 摘要: |
| 【目的】制备硝唑尼特纳米乳，并对其理化性质及安全性进行评价。【方法】以纳米乳的载药量、稳定性和毒性为考察指标，筛选合适的油相、表面活性剂、助表面活性剂和助溶剂，再利用伪三元相图筛选最佳配方并制备硝唑尼特纳米乳。用透射电镜观察硝唑尼特纳米乳的形态，用激光粒度分析仪测定其粒径分布范围、多分散系数(PDI)和Zeta电位，通过留样观察和加速试验考察其稳定性，采用急性毒性试验评估其安全性。【结果】硝唑尼特纳米乳配方中各组分的最佳配比(质量分数)为：二甲基亚砜0.3%，硝唑尼特0.45%，肉桂醛6.0%，1,2-丙二醇5.0%，聚氧乙烯醚蓖麻油 30.0%，蒸馏水58.25%。制备出的硝唑尼特水包油型纳米乳呈规则的圆球型，粒径为5～30 nm，平均粒径13.8 nm，外观澄清透明；稳定性试验结果显示，其在-4 ℃、室温和60 ℃条件下储藏均未出现浑浊、分层或药物析出等现象，稳定性表现良好；急性毒性试验表明，该纳米乳半数致死量(LD50)为5 391 mg/kg，属实际无毒的药物，有良好的安全性。【结论】成功研制了硝唑尼特纳米乳，其稳定性好，安全性高。 |
| 关键词: 硝唑尼特 纳米乳 伪三元相图 急性毒性试验 |
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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 toxicity test of Nitazoxanide nanoemulsion |
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| Abstract: |
| 【Objective】The purpose of this study was to establish nanoemulsion formula and evaluate its quality and acute toxicity.【Method】The appropriate oil phase,surfactant,cosurfactant and cosolvent were selected according to the drug loading,stability and toxicity of nanoemulsion and then the optimum formula was designed using pseudo-ternary phase diagram.The configuration was measured by TEM and the particle size,polydispersity and zeta potential were measured by LPSA.The stability was tested by high speed centrifugation and optic observation while acute toxicity was evaluated by LD50.【Result】The optimum formula of Nitazoxanide nanoemulsion was composed of 0.3%(m/m)DMSO,0.45%(m/m)Nitazoxanide,6.0%(m/m)cinnamaldehyde,5.0%(m/m)1,2-propanediol,30.0% (m/m)EL-40 and 58.25% (m/m)distilled water.The Nitazoxanide nanoemulsion droplet(O/W) was spherical under TEM and the particle size ranged from 5 to 30nm,with the average diameter of 13.8nm.Nitazoxanide nanoemusion remained transparent and clear after high speed centrifuge test and being kept at -4 ℃,room temperature and 60 ℃ ,respectively.The acute toxicity test demonstrated that LD50 was 5 391 mg/kg,which indicated that it was Non toxic.【Conclusion】The Nitazoxanide nanoemulsion was successfully prepared with good stability and high security. |
| Key words: Nitazoxanide nanoemulsion pseudo-ternary phase diagram acute toxicity test |
