摘要
目的选择适宜比例的油、表面活性剂、助表面活性剂和水制备酮洛芬微乳制剂,以增加药物的溶解度和经皮渗透量。方法以伪三元相图为基础,依据微乳区域大小,初步筛选微乳处方,用改进的Franz扩散池研究酮洛芬微乳的透皮速率,进一步优化处方。结果油相、表面活性剂以及表面活性剂和助表面活性剂的质量比均对微乳的形成有一定的影响,酮洛芬微乳制剂处方为含药1.25%,油相(IPM)3%,混合表面活性剂(Labrasol/PlurolOleique)30%和水,其稳态渗透速率为(46.47±2.1)μg·cm-2·h-1。结论所制备的微乳具有很好的透皮速率,有望成为酮洛芬的新型经皮给药制剂。
Abstract
OBJECTIVE To prepare the microemulsion formulation containing ketoprofen was prepared by using appropriate proportion of oil, surfactant (S), cosurfactant (CoS) and water for increasing solubility and its in vitro transdermal delivery ability. METHODS According to the area of microemulsion basing on the pseudo-tertiary phase diagrams, the optimum formulation were screened initially. And the permeation flux of ketoprofen was determined in vitro using Franz diffusion cell to optimize the formulation deeply. RESULTS The results showed that oil, surfactant, the ratio of surfactant to cosurfactant had great effect on microemulsion. The optimum formulation was composed of 1.25% ketoprofen, 3% oil (IPM), 30% surfactant and cosurfactant (Labrasol/Plurol Oleique) and water. The permeation flux of ketoprofen was 46.47±2.1 μg·cm2·h-1. CONCLUSION The optimized microemulsion showed a good penetration, which may be a promising vehicle for the transdermal delivery of ketoprofen.
关键词
酮洛芬 /
微乳 /
经皮给药
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Key words
ketoprofen /
microemulsion /
transdermal delivery
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袁悦;李三鸣;王思玲;刘华.
酮洛芬微乳经皮给药制剂的研究[J]. 中国药学杂志, 2006, 41(21): 1647-1650
YUN Yue;LI Sn-ming;WNG Si-ling;LIU Hu.
Transdermal Delvery of Ketoprofen Microemulsion [J]. Chinese Pharmaceutical Journal, 2006, 41(21): 1647-1650
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参考文献
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脚注
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