| 摘要: |
| 【目的】制备头孢克肟纳米乳，考察其理化性质，并进行体外抑菌活性检测和安全性评价。【方法】利用伪三元相图法筛选头孢克肟纳米乳配方，制备头孢克肟纳米乳，用透射电镜、激光粒度分析仪对其进行形态和粒径分析；采用微量肉汤稀释法，检测头孢克肟纳米乳对致病性大肠埃希菌、金黄色葡萄球菌、沙门氏菌、无乳链球菌和不动杆菌的最小抑菌浓度(MIC)和最小杀菌质量浓度(MBC),通过急性毒性试验考察其安全性。【结果】头孢克肟纳米乳中各组分的质量分数为：EL-40 27.1%、肉桂醛6.8%、头孢克肟2.0%、蒸馏水64.1%。制备的头孢克肟纳米乳为浅黄色澄清透明液体，透射电镜下为规则圆球形，粒径分布在6～20 nm，平均粒径为12.1 nm，多分散系数（PDI）为0.141，分散性良好。体外抑菌试验表明，头孢克肟纳米乳对致病性大肠埃希菌、金黄色葡萄球菌、沙门氏菌、无乳链球菌和不动杆菌的MIC分别为1，4，4，2，8 μg/mL，MBC分别为2，8，8，4，16 μg/mL，抑菌效果明显优于其他对照药物。急性毒性试验表明，头孢克肟纳米乳的LD50为4 116 mg/kg，属于低毒药物，安全性良好。【结论】成功研制了头孢克肟纳米乳，体外抑菌效果明显，属于低毒药物，具有良好的安全性。 |
| 关键词: 头孢克肟 纳米乳 伪三元相图 最小抑菌浓度 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 of cefixime nanoemulsion and determination of its bacteriostatic activity and acute toxicity in vitro |
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| Abstract: |
| 【Objective】Cefixime nanoemulsion was prepared and its quality and in vitro pharmacy and toxicity were evaluated.【Method】The preparation of the cefixime nanoemulsion was optimized by studying the pseudoternary phase diagram.Its configuration and particle size were measured by TEM and LPSA.Broth dilution method was used to determine the MIC and MBC of cefixime nanoemulsion on Enteropathogenic E.coli,cefixime nanoemulsion on Enteropathogenic E.coli,Staphylococcus,Salmonella,Streptococcus agalactiae and Acinetobacter.Toxicity was also evaluated.【Result】The mass fractions of the components in cefixime nanoem ulsion were EL-40 27.1%,cinnamaldehyde 6.8%,cefixime 2.0%,and distilled water 64.1%.The shape of cefixime nanoemulsion was spherical under TEM with an average diameter of 12.1 nm,and the polydispersity index(PDI) was 0.141.The susceptibility test revealed that MICs of cefixime nanoemulsion were 1,4,4,2,and 8 μg/mL,and MBCs were 2,8,8,4,and 16 μg/mL,better than control drug group.Its LD50 was 4 116 mg/kg.【Conclusion】Cefixime nanoemulsion was a clarity solution.The antibacterial effect of cefixime nanoemulsion on above bacteria in vitro was remarkable,and its toxicity was low. |
| Key words: cefixime nanoemulsion pseudoternary phase diagram minimum inhibitory concentration acute toxicity test |
