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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[1] 吴燕青,辛 虹.孕激素在激素替代疗法中的作用[J].国外医学计划生育分册,2003,23(1):37-40. [2] 黄建新,陈超慧.肌肉注射黄体酮局部不良反应的观察及护理[J].当代护士,2007,(1):66-67. [3] 靳 阳,李建民.黄体酮透皮吸收研究[J].南开大学学报,1997,30(4):21-25. [4] 马建芳,罗华菲,王 浩.睾酮热熔压敏胶透皮贴剂的研制[J]. 中国药学杂志,2012,47(21):1727-1731. [5] 俞振伟,应晓英,梁文权.热熔压敏胶中药物释放性能的研究[J].中国药学杂志,2009,44(24):1878-1882. [6] 王承潇,汤秀珍,沈平婊,等.热熔压敏胶应用于中药贴剂的研究进展[J].中草药,2010,41(3):496-499. [7] 龙利红,黄 群,侯淑贤,等.黄体酮缓释栓的制备及药动学[J].中国医院药学杂志,2006,26(2):156-160. [8] 张立雯.血浆和子宫中黄体酮和代谢物的测定及黄体酮膜的局部吸收研究[D].四川:四川大学,2004:6. [9] 孔雅慧.黄体酮硅橡胶阴道环(PVR)在家兔的药代动力学及药效学研究[D].上海:复旦大学,2006:7.
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