A Pharmacokinetic Study of an Ibuprofen Topical Patch in Healthy Male and Female Adult Volunteers.

Abstract

The pharmacokinetics of a novel locally applied ibuprofen topical patch was evaluated. Healthy subjects (n=28) were administered a 200-mg ibuprofen patch every 24hours for 5 days, and steady-state pharmacokinetics was determined. The amount of ibuprofen remaining in the patch following each patch removal was also assessed. The maximum steady-state drug concentration and area under the concentration curve from time 0 on day5 (t=0) to the 24-hours sample on day 6 were 514ng/mL (95% CI 439 to 603ng/mL) and 9.78kg·h/mL (95% CI 8.43 to 11.4kg·h/mL), respectively. Maximum ibuprofen concentration on day 5 occurred at 20 hours post-patch application. No evidence of drug accumulation was observed, and steady state was achieved between days 2 and 5. Ibuprofen levels attenuated rapidly to baseline within 24hours after treatment discontinuation. The amount of ibuprofen remaining in the patch was high (≥80%). Treatment-emergent adverse events were generally mild, with the most prevalent being headache (n=6; 21.4%). Only 4 TEAEs were considered related to the ibuprofen patch: paresthesia (n=1), headache (n=2), and pruritic rash (n=1). The study found that the systematic absorption of ibuprofen from a 200-mg patch was low and that the levels of ibuprofen leaving the patch over a 24-hour period are consistent with levels required for therapeutic relief as shown in other studies.