吲哚美辛微乳的制备及经皮吸收研究

Preparation and Transdermal Absorption of Indomethacin Microemulsion

以油酸、Cremorphor RH60、Labrasol和水组成微乳系统,通过伪三元相图确定o/w微乳区并筛选出最佳微乳处方。考察5种吸收促进剂对吲哚美辛原药及微乳的促渗作用。结果表明,微乳中Cremorphor RH60与Labrasol的比例为1∶2时,o/w微乳区最大。月桂氮酮是吲哚美辛微乳的最佳透皮促进剂,用量为5%时渗透速率为(73.52±2.30)mgcm-2h-1,24h累积渗透量可达1700mg/cm2。

The system of microemulsion consisted of oleic acid, Cremorphor Rh60, Labrasol and water. Pseudoternarycomposition diagrams were drawn to confirm the area of o/w microemulsion, and to select the optimum formulation ofindomethacin microemulsion. The effects of five permeation enhancers on the penetration of indomethacin bulk drug andmicroemulsion were evaluated, respectively. The results showed that the area of o/w microemulsion reached a maximumat Cremorphor RH60-Labrasol (1∶2). The optimum permeation enhancer was azone, the penetration rate was (73.52±2.30)mgcm-2h-1 and the 24h cumulative amount reached 1700mg/cm2 when the microemulsion containing 5% azone.