魏晓红 梁文权 杭州 浙江医科大学药学系 中国现代应用药学 1999 0 16 2


    关键词：睾酮；经皮给药系统；聚丙烯酸酯；经皮渗透 期刊 zgxdyyyx 0 药剂 fur -->


    

摘要 目的： 寻找以聚丙烯酸酯为骨架的睾酮经皮给药系统的最佳处方。方法： 以聚丙烯酸酯为基质设计不同的处方，在单室扩散池上测定睾酮通过人皮肤的渗透速率，研究不同的促渗剂和睾酮用量对经皮渗透的影响；同时以测定残余量的方法测定贴片在体经皮渗透量。结果： 油酸、丙二醇、异丙醇、苯甲酸苄酯、月桂氮酮等促渗剂均能显著提高睾酮贴片的经皮渗透速率，其中以月桂氮酮加丙二醇的促渗作用最大；离体经皮渗透量随睾酮用量增大而增大；5cm² 贴片的在体经皮渗透量为0.25～0.35mg/d。结论： 按筛选所得处方制得50cm² 贴片可满足2～7mg/d的治疗量要求。

Study on the formulation of the transdermal delivery system of testosterone

    Wei Xiaohong(Wei XH),Liang Wenquan(Liang WQ)(Pharmacy Department of Zhejiang Medical University,HangZhou 310031)

ABSTRACT OBJECTIVE： To search after the optimum formulation of the TDS of testosterone.METHOD: Various formations whose skeleton was polyacrylic acid were designed.The in-vitro permeation rate of the patch through skin on franz diffusion cell was determined by HPLC.The effect of various skin permeation enhancers and the amount of testosterone on the release rate of the TDS were studied.The residual content of worn patches were also determined by HPLC.RESULTS: Organic small compounds and long unsaturated chain fat acids all have enhancing effect on the permeation of TDS of testosterone.The more the amount of testosterone was,the faster the release rate of the TDS was.Based on residual content analysis of worn patches,the estimated daily input rate of formulation was 2.5～3.5 mg/d per 50cm² .CONCLUSION: Based on residual content analysis of worn patches,the amount of tesosterone meeted the needs.

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