辅料羟丙基甲基纤维素-硬脂酸作为辣椒素透皮凝胶基质的研究

Study on HPMC-stearic acid as matrix for capsaicin transdermal gel

目的评价辅料羟丙基甲基纤维素-硬脂酸(HPMC-硬脂酸)作为辣椒素透皮凝胶基质的适用性,并对制剂处方进行优化。方法以HPMC-硬脂酸为基质制备了辣椒素透皮凝胶,通过正交设计试验,对基质处方进行优化,并考察其体外经皮渗透性能和稳定性。结果所制备的凝胶为白色半透明胶体,正交试验筛选出的优化处方组成为1%HPMC-硬脂酸、15%丙二醇、10%甘油,辣椒素12 h累积渗透量为275.45μg/cm2。结论以HPMC-硬脂酸为基质制备的辣椒素凝胶性质稳定,具有良好的适用性和经皮渗透性能,有望成为辣椒素的新型透皮给药制剂。

Objective To evaluate the applicability of hydroxypropyl methyl cellulose （HPMC）-stearic acid as matrix for capsaicin transdermal gel and to optimize the formula. Methods .HPMC-stearic acid was added as the matrix for the preparation of capsaicin transdermal gel, the formula was optimized by orthogonal design and its permeation ability in vitro and stability were investigated. Results The prepared gel was white translucent colloid. The best formula optimized by orthogonal test was 1% HPMC-stearic acid, 15% propylene glycol, and 10% glycerol, and the cumulative permeation quantity in vitro at 12 h was 275.45 μg/cm^2. Conclusion The capsaicin transdermal gel has good stability and percutaneous permeability, which may be a promising new dosage form for transdermal delivery of capsaicin.