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药物微乳的特性与抗菌活性研究。

Characterization and antimicrobial activity of a pharmaceutical microemulsion.

机构信息

Department of Food Science and Nutrition, Huajiachi Campus, Zhejiang University, Hangzhou 310029, China.

出版信息

Int J Pharm. 2010 Aug 16;395(1-2):154-60. doi: 10.1016/j.ijpharm.2010.05.022. Epub 2010 May 24.

Abstract

The characterization of a pharmaceutical microemulsion system with glycerol monolaurate as oil, ethanol as cosurfactant, Tween 40 as surfactant, sodium diacetate and water, and the antimicrobial activities against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus niger and Penicillium expansum have been studied. The influence of ethanol and sodium diacetate on oil solubilization capability was clearly reflected in the phase behavior of these systems. One microemulsion formulation was obtained and remained stable by physical stability studies. The antimicrobial assay using solid medium diffusion method showed that the prepared microemulsion was comparable to the commonly used antimicrobials as positive controls. The kinetics of killing experiments demonstrated that the microemulsion caused a complete loss of viability of bacterial cells (E. coli, S. aureus and B. subtilis) in 1 min, killed over 99% A. niger and P. expansum spores and 99.9% C. albicans cells rapidly within 2 min and resulted in a complete loss of fungal viability in 5 min. The fast killing kinetics of the microemulsion was in good agreement with the transmission electron microscopy observations, indicating the antimembrane activity of the microemulsion on bacterial and fungal cells due to the disruption and dysfunction of biological membranes and cell walls.

摘要

已对含有甘油单月桂酸酯作为油相、乙醇作为助溶剂、吐温 40 作为表面活性剂、双乙酸钠和水的药物微乳液系统进行了特性描述,并研究了其对大肠杆菌、金黄色葡萄球菌、枯草芽孢杆菌、白色念珠菌、黑曲霉和扩展青霉的抗菌活性。乙醇和双乙酸钠对油相增溶能力的影响在这些体系的相行为中得到了清晰的反映。通过物理稳定性研究获得了一种微乳液配方,且其保持稳定。采用固体培养基扩散法进行的抗菌试验表明,所制备的微乳液与常用的抗菌剂作为阳性对照相当。杀菌动力学实验表明,微乳液在 1 分钟内可使细菌细胞(大肠杆菌、金黄色葡萄球菌和枯草芽孢杆菌)完全丧失活力,在 2 分钟内可迅速杀灭超过 99%的黑曲霉和扩展青霉孢子以及 99.9%的白色念珠菌细胞,并在 5 分钟内导致真菌完全丧失活力。微乳液的快速杀菌动力学与透射电子显微镜观察结果一致,表明由于生物膜和细胞壁的破坏和功能障碍,微乳液对细菌和真菌细胞具有抗膜活性。

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