自乳化基质乙氧苯柳胺乳膏的研制及透皮研究

Assessment of transdermal absorption for etofesalamide self-emulsion-base cream

目的:制各自乳化基质乙氧苯柳胺乳膏并对其体外透皮吸收行为进行考察。方法:采用Tefose 63为自乳化基质制备乙氧苯柳胺乳膏并考察其稳定性,采用改进的Franz扩散池,以大鼠离体腹部皮肤为透皮模型,用HPLC法测定药物在透皮接收液中的浓度及皮肤中药物滞留量。结果:自乳化基质乳膏具有较好的稳定性,在皮肤中的渗透系数及药物滞留量明显大于市售软膏,离体条件下,自乳化基质乳膏8 h渗透系数是市售软膏的1．56倍,皮肤中药物滞留量是市售软膏的2．31倍。结论:自乳化基质乙氧苯柳胺乳膏能促进药物渗透到皮肤并增加药物在皮肤中的滞留量,有望成为新型经皮给药制剂。

Objective：To assess the transdermal behaviors of etofesalamide self-emulsion-base （ESEB） cream in vitro newly prepared. Methods：Etofesalamide formed a cream when mixed with Tefose 63, a self-emulsion-base. The stability of the ESEB cream was studied. The transdermal features of the ESEB cream were assessed in vitro in a modified Franz diffusion cells by aids of a percutaneous permeation model made of rat abdominal skin. Etofesalamide concentrations in both receiving cell and residues on the skin were measured by HPLC. Results：The ESEB cream had a fine stability. The permeable coefficient of ESEB cream in vitro was the same as 1.56 times of corresponding marketing creams within 8 hours, and the residue amount on the skin was 2.31 times higher than marketing creams. Conclusion： The self-emulsion-base cream with better permeativity and retentivity has the potential to be a promising vehicle for transdermal drug delivery.