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 24 hours 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 day 5 (t = 0) to the 24-hours sample on day 6 were 514 ng/mL (95% CI 439 to 603 ng/mL) and 9.78 kg·h/mL (95% CI 8.43 to 11.4 kg·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 24 hours 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.

Topical Nonsteroid Anti-Inflamatory Drugs – indications, efficacy and safety

“…The systemic absorption of ibuprofen from a 200-mg patch is low and the levels of ibuprofen leaving the patch during a 24-hour exposure are consistent with the levels required for therapeutic relief. Pain relief with ibuprofen patch is achieved at doses much lower than those required for oral dosing (9). similar results were obtained for ketoprofen (3).…”

A hollow mesoporous carbon from metal-organic framework for robust adsorbability of ibuprofen drug in water

“…Chemically, this drug molecule, whose properties and structure are summarized in electronic supplementary material, table S1 and figure S1, is constructed from aromatic ring substituted with carboxylic acid (pK a value of 5) including 3 H-bonds (1 H-acceptor and 2 H-donors). In microorganisms, ibuprofen is rapidly metabolized in the form of hydroxyl- and carboxyl-ibuprofen [5]. Naturally, ibuprofen residues can derive from wastewater in the pharmaceutical industries, and partial excrement of medically treated humans and animals [6].…”

Topical NSAIDs for acute local pain relief: in vitro characterization of drug delivery profiles into and through human skin

“…A hypothesis based on this finding is that gels with an increased reliance on the formation of a concentration gradient within the upper skin layers upon dry down, as well as the drug remaining mobile in order to maintain the partition co-efficient (driving force) over time, could result in increased intra-patient variability. Pharmacokinetic data support this hypothesis, with a mean Cmax of 556 ng/mL (SD 249; 95% CI 439-603) for the ibuprofen medicated plaster [28], compared to 630 ng/mL (SD 520) for the ibuprofen gel [46] and 5.4 ng/mL (SD 4.6; range 2.2-29.4) for the diclofenac gel [47].…”

“…Most recently, an ibuprofen-medicated plaster [25] has been developed which has shown significant and clinically relevant reductions in local pain and tenderness when applied every 24 h in a double-blind, placebo-controlled clinical efficacy study [26,27]. NSAID plasters allow for continuous release of the drug under steady-state, with passive transport from a high concentration into the underlying tissues [28].…”