Preparation and in vitro release characterization of hot-melt pressure sensitive adhesive transdermal patch of progesterone
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摘要: 目的 制备黄体酮热熔压敏胶透皮贴剂并考察其体外释药性能。 方法 采用苯乙烯-异戊二烯-苯乙烯热塑性弹性体热熔压敏胶为骨架材料,以大鼠离体皮肤为渗透屏障,采用改良Freeze扩散池,用HPLC法测定接收液浓度,筛选促渗剂的种类、浓度和涂布厚度,确定贴剂处方。 结果 促渗剂选择肉豆蔻酸异丙酯(IPM),含量为2%;选择涂布厚度为300 μm,得到累积渗透曲线为Q=6.172 1 t-5.457 7(r=0.998 8);24 h药物累积渗透量为144.17 μg/cm2;稳态渗透速率为(6.17±0.49) μg/(cm2·h)。 结论 制备的黄体酮热熔压敏胶透皮贴剂中的有效成分黄体酮体外经皮渗透良好,具有较好的临床应用前景。Abstract: Objective To prepare hot-melt pressure sensitive adhesive (HMPSA) transdermal patches of progesterone and investigate the release characterization in vitro. Methods SIS HMPSA was used as matrix material, modified Franz diffusion cell and excised female rat skin were used as model,the concentration of progesterone was determined by HPLC. The thickness of patch and penetration enhancers was screened out by permeation rate. Results 2% IPM was used to prepare progesterone HMPSA transdermal patch, thickness was 300 μm, the cumulative permeation curve was Q=6.172 1 t-5.457 7 (r=0.998 8). The cumulative releases of the patches in 24 h was 144.17 μg/cm2. The permeation rate was (6.17±0.49) μg/(cm2·h). Conclusion The progesterone HMPSA transdermal patch had good transdermal release in vitro, which would have good clinical application prospect.
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Key words:
- progesterone /
- HMPSA /
- percutaneous penetration /
- IPM
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