青藤碱压敏胶分散型贴剂的制备及体外经皮渗透性考察

目的制备青藤碱压敏胶分散型贴剂并考察其体外经皮渗透性。方法将青藤碱及各种渗透促进剂直接溶于压敏胶中制备压敏胶分散型贴剂;采用卧式双室扩散池,研究青藤碱贴剂的体外经皮渗透行为。结果由DURO-TAK87-4098型压敏胶制备的贴剂的稳态渗透速率显著高于由DURO-TAK 87-2677制备的贴剂。加入各种渗透促进剂后,促渗作用由大到小的排列顺序为(质量分数):15%肉豆蔻酸异丙酯>10%肉豆蔻酸异丙酯>10%氮酮>5%肉豆蔻酸异丙酯>10%油酸>10%N-甲基吡咯烷酮。联合应用促进剂后促渗作用由大到小的排列顺序为(质量分数):10%肉豆蔻酸异丙酯+5%薄荷醇>10%肉豆蔻酸异丙酯+5%氮酮>10%肉豆蔻酸异丙酯+10%薄荷醇>10%肉豆蔻酸异丙酯+10%氮酮,但与10%的豆蔻酸异丙酯或10%氮酮相比,没有协同作用。结论应用DURO-TAK87-4098型压敏胶制备的青藤碱压敏胶分散型贴剂有望制成长效抗炎镇痛贴剂,值得进一步深入研究。

Preparation of drug-in adhesive patches of sinomenine and its in vitro permeability through excised rat skin

Objective To prepare drug-in adhesive patches for sinomenine and evaluate its in vitro transdermal permeability. Methods Drug-in adhesive patches of sinomenine were prepared by dissolving sinomenine and different enhancers into the pressure sensitive adhesive. Permeation characteristics of sinomenine from patches were evaluated using 2-compartment horizontal diffusion cells. Results It was found 87-4098 existed a significant higher flux than 87-2677 on the penetration of sinomenine. The effect of permeation enhancement of different enhancers was in the following order: 15% (w) isopropyl myristate>10% isopropyl myristate>10% Azone>5% isopropyl myristate>10% oleic acid>10% N-methylpyrrolidone. When enhancers were used in combination, the rank order of enhancement effect for sinomenine was 10% (w) isopropyl myristate+5% menthol>10% isopropyl myristate+5% Azone>10% isopropyl myristate+10% menthol>10% isopropyl myristate+10% Azone, however, no synergistic effect was observed compared with 10% isopropyl myristate or Azone alone. Conclusions The drug-in adhesive patches of sinomenine have the potential to become an effective transdermal drug delivery system for curing arthritis deformans and is worthy of further investigation.