摘要
目的为难溶性药物提供合适的注射用微乳载体。方法以中碳链甘油酯作为油相,聚氧乙烯蓖麻油、聚氧乙烯氢化蓖麻油、磷脂、泊洛沙姆单用或合用作为表面活性剂,乙醇、聚乙二醇400单用或合用作为助表面活性剂,建立不同的空白微乳体系并考察其伪三元相图。选取3种具有代表性的空白微乳体系进行粒径、形态学、稳定性评价。将尼莫地平、替尼泊苷、法莫替丁等3种水难溶性药物分别载入3种微乳体系,制备载药微乳并进行性质评价。结果伪三元相图中,随着Km值的增大,微乳区域变大。空白微乳和载药微乳呈略带淡蓝色乳光的澄清透明液体;乳滴呈大小均匀的圆球形;粒径呈高斯分布;空白微乳和载药微乳均可与5%葡萄糖注射液和0.9%氯化钠注射液配伍,稳定性好。结论所建立的空白微乳体系稳定性较高,便于临床使用,可用作难溶性药物的载体。
Objective To find a microemulsion delivery system for water-insoluble drugs.
Methods By using medium chain triglycerides as an oil phase, pseudo-ternary phase diagrams of microemulsions consisting of polyoxyethylated castor oil, polyoxyethylene hydrogenated castor oil, lecithin, poloxamer, or their mixtures as surfactant, and ethanol or their mixtures PEG400 as cosurfactant. The appearance, morphologies, droplet sizes, and stability of three blank and drug-loaded microemulsions were evaluated. Nimodipine, Etoposide and Famotidine, with poor solubility, were loaded in three microemulsion systems. And drug-loaded microemulsions were evaluated, respectively.
Results The area of O/W microemulsion region in the pseudo-ternary phase diagram increased with Km. Both the blank and drug-loaded microemulsions were translucent solutions with visible sky-blue opalescence. The microemulsions consisted of small spherical drops with diameters in Gaussian distribution. The appearance, pH value, concentration, and particle size of the microemulsions were stable, and dilutable with 0.9% sodium chloride injection and 5% glucose injection, respectively.
Conclusion The blank microemulsions are stable and applicable to clinical practice as a microemulsion delivery system for water-insoluble drugs.
出处
《中国医药生物技术》
CSCD
2008年第2期98-102,共5页
Chinese Medicinal Biotechnology
基金
国家自然科学基金(30500666)
清华大学裕元基金(20240000529)
关键词
药物载体
乳状剂
注射
伪三元相图
Drug carriers
Emulsions
Injections
Pseudo-ternary phase diagrams
