Kweon Jang-Hoon, Chi Sang-Cheol, Park Eun-Seok
College of Pharmacy, Sungkyunkwan University, 300 Chonchon-dong, Changan-gu, Suwon, Kyonggi-do 440-746, Korea.
Arch Pharm Res. 2004 Mar;27(3):351-6. doi: 10.1007/BF02980072.
A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol:ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.
采用水包油(O/W)微乳体系研制了一种含双氯芬酸二乙胺(DDA)的透皮制剂。在所测试的油类中,月桂醇被选为微乳的油相,因为它对药物表现出良好的增溶能力和优异的皮肤渗透速率。构建伪三元相图以获得形成微乳所需的油、表面活性剂和助表面活性剂的浓度范围,并用离体大鼠皮肤评估这些添加剂对DDA皮肤渗透的影响。微乳的最佳配方由1.16%的DDA、5%的月桂醇、60%的水以及34.54%的Labrasol(表面活性剂)/乙醇(助表面活性剂)(1:2)组成。该配方在DDA经皮吸收方面的效率取决于水、月桂醇的含量以及Labrasol与乙醇的混合比例。得出的结论是,随着微乳中月桂醇和水含量的增加以及配方中Labrasol与乙醇混合比例的降低,DDA的经皮吸收增强。