目的 制备盐酸布替萘芬微乳温敏凝胶, 并对其质量进行评价。方法 以油酸乙酯为油相,聚山梨酯80为乳化剂,无水乙醇为助乳化剂,泊洛沙姆188和407为温敏材料,制备对体表温度敏感的微乳凝胶,并对其形态、粒径、稳定性进行考察,和市售乳膏进行透皮吸收速度和皮内滞留量的对比。结果 微乳凝胶最终处方为:油酸乙酯-聚山梨酯80-无水乙醇-P407-P188-纯化水=4∶15∶10∶16.33∶5.68∶71。所得的微乳为水包油型,透射电镜下乳滴呈圆球形,平均粒径91.03 nm,PDI为0.246,自制微乳凝胶透皮速度较市售乳膏快,皮肤内药物滞留量为市售乳膏的5倍。结论 该实验制备得到的温敏微乳凝胶具有良好的温度敏感性和透皮滞留效果,能够以较快速度进入皮肤内层形成药物贮库,提高局部药物浓度,增强抗菌效果。
Abstract
OBJECTIVE To prepare butenafine hydrochloride thermosensitive microemulsion-based hydrogel and evaluate the quality. METHODS A series of temperature sensitive microemulsion gels with different gelation temperatures were prepared,using ethyl oleate as oil phase, Tween 80 as surfactant, ethanol as co-surfactant, and poloxamer as temperature-sensitive material. The morphology,particle size,Zeta potential,percutaneous absorption speed and skin retention were evaluated. RESULTS The best formulation was composed of ethyl oleate-Tween 80-ethanol-poloxamer 407-poloxamer 188-distilled water at ratios of 4∶15∶10∶16.33∶5.68∶71. The oil/water microemulsion exhibited a spherical shape without adhesion or aggregation observed by TEM. The average diameter was 91.03 nm and the PDI was 0.246. The transdermal speed of microemulsion gel was faster than the marketed cream, and the drug retention in the skin was 5 times of the marketed cream. CONCLUSION The hydrogel exhibits good temperature sensitivity and skin retention effect, and can penetrate skin cutin and act as a depot thus increase the local drug concentration and enhance the antibacterial effect.
关键词
盐酸布替萘芬 /
温度敏感 /
微乳 /
凝胶 /
伪三元相图
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Key words
butenafine hydrochloride /
temperature sensitivity /
microemulsion /
hydrogel /
pseudoternary
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中图分类号：
R944
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参考文献
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脚注
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基金
济宁医学院2013年度校级科研计划项目(JY2013KJ012);地方高校国家级大学生创新创业训练计划项目(201610443020);济宁医学院大学生创新训练计划项目(cx2016020)
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