睾酮凝胶剂的处方研究

目的:探讨睾酮凝胶剂的最佳处方.方法:以卡波姆940为基质设计不同的处方,探讨最佳制备方法,并在单室扩散池上测定睾酮通过小鼠腹部皮肤的透过量,研究不同的促吸收剂对经皮透过的影响.结果:1.0%卡波姆940,67%的乙醇为最佳基质;卡波姆940均匀撒入无水乙醇中,加热回流,使其溶胀完全再加中和剂形成凝胶;氮酮、肉豆蔻酸异丙酯、油酸等促渗剂均能显著提高睾酮凝胶的经皮透过速率,其中以肉豆蔻酸异丙酯的促渗透效果最好.结论:以1.0%卡波姆940,67%的乙醇和肉豆蔻酸异丙酯为基质的处方最佳.

Study on Formulation of Testosterone Gel

Objective: To explore the optimal formulation of testosterone gel taking Carbomer 940 as matrix. Method: Various formations whose skeleton was Carbomer 940 were designed to explore the optimum. The in-vitro permeation amount of the testosterone gel through belly skin of rat on Franz diffusion cell was determined. The effect of various skin permeation enhancers on the transdermal delivery was studied. Result: It was shown that 1% of Carbomer 940 and 67% of ethanol were the optimum matrix. Carbomer 940 was sprinkled into ethanol well-distributed and then refluxed. When Carbomer 940 was fully swelling, neutralizer was added to take Gel shape. Azone, isopropyl myristate, oleic acid and etc. all had enhancing effect on promoting the rate of permeation of testosterone gel. Isopropyl myristate was the best penetration enhancer in the all. Conclusion: 1 % of Carbomer 940,67% of ethanol and isopropyl myristate were the optimum matrix of testosterone gel.