Studies On Self-Emulsion-Base Etofesalamide Cream

Etofesalamide as a non-steroidal anti-inflammatory and anti-anaphylaxis drug was used in the treatment of chronic eczema and neurodermatitis which were generally treated by glucocorticoid topically. However, glucocorticoid could induce many side effects (eg: adermotrophia, pigment anomaly, angiotelectasis) while etofesalamide could avoid them .Definitely, the etofesalamide had widely clinical perspective in the area of treating chronic eczema and neurodermatitis.Self-Emulsion-Base are ready-to-use products which can spontaneously form superior, extremely stable o/w emulsions merely by heating in the presence of water.PEG-7 stearate (Tefose 63) is polyvalent o/w emulsifier which can be used to prepare elegant and very stable creams. The SPECTAZOLE (econazole nitrate cream),MONISTAT-3 (miconazole nitrate cream) and other antifungal had been authorized on the overseas market using Tefose 63 as emulsifing base.In this paper, some physicochemical properties of etofesalamide were determined . The study on solubility of etofesalamide in different mediums showed that etofesalamide was insoluble in water and Transcutol P had an excellent solubilizition to etofesalamide.The value of oil/water partition coefficient of etofesalamide demonstrated that etofesalamide was fit to be used topically.The effect of Transcutol P on the penetration of etofesalamide across rat skin and the drug residual amount in rat skin were studied by using modified Valia-Chien diffusion cell.It was shown that the concentration of etofesalamide in rat skin was increasing with the level of Transcutol P , but the drug accumulative penetration amount was not obviously changed.The formulation of etofesalamide cream with Tefose 63 as base was optimized by orthogonal design method and transdermal penetration experiment across rat skin in vitro.The drug release in vitro was studied by using modified Franz diffusion cell and synthesis membrane.The most suitable member and medium were 0.45 μm nylon membrane and 30 %PG/PBS7.4 solution respectively.The preparation process was optimized by orthogonal design...