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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。
Objective: To explore the best prescription of testosterone gel. METHODS: Different prescriptions were designed with carbomer 940 as the matrix, and the best preparation method was explored. The transdermal penetration of testosterone through the abdominal skin of mice was measured on a single-cell diffusion cell to study the effects of different absorbents on transdermal permeation . Results: 1.0% carbomer 940, 67% ethanol as the best matrix; Carbopol 940 evenly into anhydrous ethanol, heated to reflux, to swell completely plus neutralizer to form a gel; azone , Isopropyl myristate, oleic acid and other penetration enhancers can significantly increase the transdermal transmission rate of testosterone gel, of which isopropyl myristate promote the penetration of the best. CONCLUSIONS: Prescriptions with 1.0% carbomer 940, 67% ethanol and isopropyl myristate were the best.