Sumatriptan succinate transdermal delivery systems for the treatment of migraine.
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.
Balaguer-Fernández
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C
Departamento de Fisiología, Farmacología y Toxicología, Facultad de Ciencias Experimentales y de la Salud, Universidad CEU Cardenal Herrera, 46113 Moncada, Spain.
Femenía-Font
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A
Del Rio-Sancho
S
S
Merino
V
V
López-Castellano
A
A
D000279:Administration, Cutaneous; D000818:Animals; D001381:Azepines / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D015194:Diffusion Chambers, Culture; D004337:Drug Carriers; D004339:Drug Compounding; D007478:Iontophoresis; D007700:Kinetics; D008747:Methylcellulose / Q000737:chemistry; D008881:Migraine Disorders / Q000188:drug therapy*; D010539:Permeability; D010968:Plasticizers / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D019946:Propylene Glycol / Q000737:chemistry; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013012:Sorbitol / Q000737:chemistry; D018170:Sumatriptan / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods; D014014:Tissue Adhesives / Q000737:chemistry; D014662:Vasoconstrictor Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism
D001381:Azepines; D004337:Drug Carriers; D010968:Plasticizers; D011108:Polymers; D011109:Polymethacrylic Acids; D017366:Serotonin Receptor Agonists; D014014:Tissue Adhesives; D014662:Vasoconstrictor Agents; C035229:laurocapram; D013012:Sorbitol; D019946:Propylene Glycol; D018170:Sumatriptan; D011142:Polyvinyl Alcohol; D008747:Methylcellulose; D011205:Povidone