A unique iontophoretic patch for optimal transdermal delivery of sumatriptan.
OBJECTIVE
Migraines affect approximately 10% of the adult population worldwide. The purpose of this study was to assess the pharmacokinetic and safety profile of a novel iontophoretic sumatriptan delivery system, NP101, which uses an electrical current to propel sumatriptan across intact skin and into underlying tissue. Four unique prototype iontophoretic sumatriptan patch conditions were compared to a 6 mg subcutaneous injection and an oral 50 mg tablet of sumatriptan succinate.


METHODS
This was a randomized, single-center, single-dose, six-period Phase I study.


RESULTS
Patches were well tolerated with fewer adverse events than the subcutaneous injection. Adverse events that were more prevalent for NP101 than other formulations included localized sensations and reactions at the patch site. A linear relationship was observed between total applied current and sumatriptan delivery. Patches delivering 6 and 12 mA per h yielded favorable sumatriptan systemic profiles, delivering drug at a rate that maintained plasma levels above the target level (> or = 10 ng/ml) for greater than 7 h.


CONCLUSIONS
This study met the initial objective to define the dose-current relationship in humans as well as delimiting specific current and current density targets for a well tolerated patch design that can deliver therapeutic drug levels for longer periods than currently possible.
Siegel
Steven J
SJ
Division of Neuropsychiatry, University of Pennsylvania, Translational Research Laboratories, 125 S. 31st St. Rm. 2223, Philadelphia, Pennsylvania 19104, USA. siegels@mail.med.upenn.edu
O'Neill
Carol
C
Dubé
Louise M
LM
Kaldeway
Peter
P
Morris
Russell
R
Jackson
David
D
Sebree
Terri
T
D000279:Administration, Cutaneous; D000284:Administration, Oral; D000328:Adult; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000009:adverse effects / Q000295:instrumentation*; D004867:Equipment Design; D005260:Female; D006801:Humans; D007279:Injections, Subcutaneous; D007478:Iontophoresis / Q000009:adverse effects / Q000295:instrumentation*; D008297:Male; D008875:Middle Aged; D008881:Migraine Disorders / Q000188:drug therapy*; D010865:Pilot Projects; D011087:Polycythemia Vera / Q000209:etiology; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D018170:Sumatriptan / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D013607:Tablets; D014662:Vasoconstrictor Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics
D017366:Serotonin Receptor Agonists; D013607:Tablets; D014662:Vasoconstrictor Agents; D018170:Sumatriptan