睾酮热熔压敏胶透皮贴剂的研制

Preparation of Testosterone Hot Melt Pressure Sensitive Adhesive Transdermal Patch

目的制备睾酮热熔压敏胶贴剂,并对其体外透皮性能进行研究。方法采用热塑性弹性体苯乙烯-异戊二烯-苯乙烯(SIS)热熔压敏胶基质制备睾酮透皮贴剂,采用Franz扩散池,以离体裸鼠皮肤为屏障进行体外透皮实验。通过药物累积透过量和稳态透皮速率筛选载药量和促渗剂,并将优化处方制备的贴剂与上市产品进行体外透裸鼠皮和猪皮实验的比较。结果睾酮热熔压敏胶贴剂最佳处方载药量2%,促渗剂肉豆蔻酸异丙酯(IPM)的用量为6%,体外透皮行为符合零级释放动力学;体外透裸鼠皮或猪皮实验,自制贴剂优于上市贴剂。结论 SIS热熔压敏胶在透皮给药系统中具有广阔的应用前景。

OBJECTIVE To prepare testosterone hot melt pressure sensitive adhesive （HMPSA） transdermal patch and investi- gate its percutaneous permeability in vitro. METHODS The matrix of thermoplastic elastomer styrene-isoprene-styrene（SIS）hot melt pressure sensitive adhesive was used for testosterone transdermal patch. The pereutaneous permeability through excised nude mice skin or porcine skin in vitro was conducted by Franz diffusion cells. Cumulative permeation quantity （Q） and steady state permeation rate （JB~） were evaluated to optimize drug loading capacity and enhancer. The optimal transdermal patches were compared with reference patches with regard to percutaneous behaviors using excised nude mice skin and porcine skin. RESULTS The optimal formulation contained 2% testosterone,6% trans dermal enhancer isopropyl myristate （IPM）. Its permeation behavior in vitro followed zero-order ki- netics. The permeation behavior of the optimal patches was better than the reference patches for excised nude mice skin and porcine skin. CONCLUSION SIS HMPSA has a broad application potential for transdermal drug delivery system.