摘要
目的:找到复方莪术油脂质体凝胶(zedoary turmeric oil compound liposomes gel,ZTOC-LG)的最佳制备工艺并进行体外透皮性能研究及其稳定性考察。方法:采用乙醇注入法制备复方莪术油脂质体(zedoary turmeric oil compound liposomes,ZTOC-L),再以卡波姆-940为基质制备脂质体凝胶剂,通过单因素实验和正交实验,以脂质体凝胶剂的成型性、光泽度、均匀度、黏度、pH、涂展性、稳定性等组成的综合评分为评价指标,优选ZTOC-LG的制备工艺。采用Franz扩散池比较ZTOC-LG和普通凝胶的指标物质经皮渗透性和皮肤滞留量。通过温度、光照、湿度实验对ZTOC-LG的稳定性进行了考察。结果:最优基质处方为卡波姆0.2 g,甘油3.5 g,三乙醇胺0.1 g。体外透皮实验表明,ZTOC-LG中的吉马酮和维A酸的24 h累积渗透量和渗透速率均小于普通凝胶,皮肤滞留量均大于普通凝胶。稳定性实验表明ZTOC-LG对温度和光照敏感,对湿度不敏感。结论:该脂质体凝胶剂的制备工艺简单可行,质量可控,且能提高药物在局部皮肤中的滞留量从而达到长效缓释的作用。
Objective： To optimize the preparation process of zedoary turmeric oil compound liposomes gel（ ZTOC-LG） and study its in vitro transdermal properties and stability. Methods： Ethanol injection method to prepare the zedoary turmeric oil compound liposomes（ ZTOC-L） in this study,and the Carbopol-940 was added as matrix for the preparation of ZTOC-LG. The ZTOC-LG were prepared through the single factor tests and orthogonal design to optimize the prescription,in which the comprehensive score composed by forming property,glossiness,uniformity,viscosity,p H,spreadable property and stability as indexes. Franz diffusion pool was employed to compare the permeation rate of ZTOC-LG and conventional gel in vitro. The stability of liposome gel was investigated by temperature,light and humidity experiments. Results： The optimal matrix prescription were Carbopol 0. 2 g,glycerol 3. 5 g and triethanolamine 0. 1 g. In vitro transdermal experiments showed that the cumulative penetration and permeation rate in 24 h of germacrone and tretinoin in ZTOC-LG were less than conventional gel but higher cumulative amounts in skin. Stability experiments showed that ZTOC-LG is sensitive to temperature and light but is insensitive to humidity. Conclusion： The preparation process of the liposome gel is simple and feasible,the qualityis controllable,and the cumulative amounts in the local skin can be improved by the liposome gel,thus achieving the effect of long action and slow release.
作者
陈积
赵小倩
马彦巧
李磊
谭丹枫
陶月英
陈泽慧
田应彪
CHEN Ji;ZHAO Xiao-qian;MA Yan-qiao;LI Lei;TAN Dan-feng;TAO Yue-ying;CHEN Ze-hui;TIAN Ying-biao(The Affiliated Hospital of Zunyi Medical College, Zunyi 563003, China;School of Pharmacy, Zunyi Medical College, Zunyi 563003, China;Department of Physiology, Zunyi Medical College, Zunyi 563003, China） F Ah~trnet] flhi~etlv~.Tn nnfJm]~ lh,~. nr~nnr~tinn nrnoPcc nf 7or]nnrv hlrm~rio n~] onmnn~lnd ]inncnnlo~ ~,~1)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2018年第7期830-838,共9页
Chinese Journal of New Drugs
基金
贵州省中医药管理局中西药
民族医药科学技术研究基金资助项目(QZYY-2014-034)
关键词
莪术油
维A酸
脂质体凝胶
体外透皮
稳定性
zedoary turmeric oil
tretinoin
liposome gel
in vitro percutaneous permeability
stability
