title: Duel-acting subcutaneous microemulsion formulation for improved migraine treatment with zolmitriptan and diclofenac: formulation and in vitro-in vivo characterization.
abstract: Subcutaneous triptan provides immediate analgesia in migraine and cluster headache but is limited by high pain recurrence due to rapid drug elimination. A dual-acting subcutaneous formulation providing immediate release of a triptan and slow but sustained release of a nonsteroidal anti-inflammatory drug may provide a longer duration of relief. A microemulsion-based technology has various advantages over other technically complex dosage forms. Oil-in-water microemulsions of zolmitriptan and diclofenac acid using Labrafac Lipophile, Tween 80, Capryol 90 and water were prepared. One formulation was characterised in vitro and found to have uniformly dispersed nanosized globules. The formulation provided differential release of zolmitriptan and diclofenac acid both in vitro as well as in vivo that may be potentially beneficial to migraine patients.
authors.affiliation: King's College London, Waterloo Campus, 150 Stamford Street, SE1 9NH, London, UK, dubeyr@drreddys.com.
authors.forename: R
authors.initials: R
authors.lastname: Dubey
authors.forename: Luigi G
authors.initials: LG
authors.lastname: Martini
authors.forename: Mark
authors.initials: M
authors.lastname: Christie
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000627:therapeutic use; D004008:Diclofenac / Q000627:therapeutic use*; D004655:Emulsions; D066298:In Vitro Techniques; D008297:Male; D046529:Microscopy, Electron, Transmission; D008881:Migraine Disorders / Q000188:drug therapy*; D023303:Oxazolidinones / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D058825:Serotonin 5-HT1 Receptor Agonists / Q000627:therapeutic use; D014363:Tryptamines / Q000627:therapeutic use*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D023303:Oxazolidinones; D058825:Serotonin 5-HT1 Receptor Agonists; D014363:Tryptamines; D004008:Diclofenac; C089750:zolmitriptan