硝苯地平微乳的制备及其质量评价
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重庆市自然科学基金资助项目(CSTC2008BB7180);重庆大学研究生科技创新基金个人项目(CDJXS10220003)


Preparation and evaluation of nifedipine microemulsion
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    摘要:

    硝苯地平难溶于水生物利用度低微乳作为难溶性药物的理想载体可增大难溶于水药物的溶解性。将硝苯地平制备成微乳剂型使其溶解性在一定程度上增大其生物利用度也得到了提高。根据溶解在不同表面活性剂、助表面活性剂、油相中的硝苯地平的量及伪三元相图筛选硝苯地平微乳的处方得出制备硝苯地平微乳的最佳质量配比为:乳化剂-OP/无水乙醇/油酸乙酯/水=27∶13.5∶4.5∶55。所制得的微乳淡黄色、澄清、透明、流动性良好加水稀释后在透射电镜下呈圆球形平均粒径为22.89 nm;经高速离心和留样观察发现其外观、质量及粒径未发生明显变化其稳定性良好。用该方法制得的硝苯地平微乳其溶解度相对于水中提高了700多倍且制备方法简单。

    Abstract:

    Nifedipine is poorly soluble in water and has low bioavailability.Microemulsionwhich is the ideal carrier of difficult soluble drugscan increase the solubility of drugs.The study prepares nifedipine into microemulsion typeand thus its solubility is increased and its bioavailability is improved to a certain extent.The formulation of nifedipine microemulsion is optimized via the pseudo-ternary phase diagram and the amount of nifedipine dissolved in different surface active agentssurfactants and oil phases.The optimized nifedipine microemulsion formulation consists of emulsifier OPanhydrous ethanolethyl oleate and water with the weight ratio of 27∶13.5∶4.5∶55.The prepared microemulsion is light yellowcleartransparent and has good mobility.When the microemulsion is diluted by waterits shape is spherical under transmission electron microscopy with an average diameter of 22.89 nm.It shows good stability after high speed centrifuging and reserved sampleand also their content and diameter have no obvious change.The nifedipine microemulsion is easy to prepare by this methodand its solubility is improved more than 700 times.

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罗平,罗丽,刘颖.硝苯地平微乳的制备及其质量评价[J].重庆大学学报,2014,37(5):83-89.

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  • 收稿日期:2013-12-10
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  • 在线发布日期: 2014-06-03
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