Balaguer-Fernández C, Femenía-Font A, Del Rio-Sancho S, Merino V, López-Castellano A
Departamento de Fisiología, Farmacología y Toxicología, Facultad de Ciencias Experimentales y de la Salud, Universidad CEU Cardenal Herrera, 46113 Moncada, Spain.
J Pharm Sci. 2008 Jun;97(6):2102-9. doi: 10.1002/jps.21129.
We have successfully obtained sumatriptan transdermal systems with different polymer compositions: methyl cellulose (MC), polyvinyl pyrrolidone (PVP) and a polyvinyl pyrrolidone (PVP)-polyvinyl alcohol (PVA) mixture. The systems contained 1,2-propylenglycol (MC) or sorbitol as a plasticizer (PVP and PVP-PVA), methacrylate copolymer as an adhesive agent, and an occlusive liner. Azone (5%, w/w) was incorporated into all the systems as a percutaneous enhancer. Transdermal systems are thin, transparent and non-adhesive when in a dry state. The permeation of sumatriptan succinate across pig ear skin was studied using the systems prepared. The formulation with MC polymer produced a statistically significant increment with respect to the PVP and PVP-PVA formulations (p < 0.05). Azone incorporation into the systems produced an increment in the sumatriptan flux values of all three transdermal systems with respect to those of the controls (p < 0.05). In addition, the application of iontophoresis to the wet methyl cellulose-Azone formulation produced a much higher increase of sumatriptan transdermal flux.
甲基纤维素（MC）、聚乙烯吡咯烷酮（PVP）以及聚乙烯吡咯烷酮（PVP）-聚乙烯醇（PVA）混合物。这些系统含有作为增塑剂的1,2 - 丙二醇（MC）或山梨醇（PVP和PVP - PVA）、作为黏合剂的甲基丙烯酸酯共聚物以及封闭性衬垫。所有系统均加入了氮酮（5%，w/w）作为经皮促进剂。透皮给药系统在干燥状态下呈薄片状、透明且无黏性。使用所制备的系统研究了琥珀酸舒马曲坦透过猪耳皮肤的渗透情况。与PVP和PVP - PVA配方相比，含MC聚合物的配方产生了具有统计学意义的增量（p < 0.05）。与对照相比，向系统中加入氮酮使所有三种透皮给药系统的舒马曲坦通量值均有所增加（p < 0.05）。此外，对湿的甲基纤维素 - 氮酮配方施加离子导入法可使舒马曲坦的透皮通量有更高的增加。
