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Skin permeability and pharmacokinetics of diclofenac epolamine administered by dermal patch in Yorkshire-Landrace pigs

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      Abstract

      Purpose

      This study compared the pharmacokinetic profile, and systemic and local absorption of diclofenac, following dermal patch application and oral administration in Yorkshire-Landrace pigs.

      Patients and methods

      Twelve anesthetized, female, Yorkshire-Landrace pigs were randomized to receive either the dermal patch (FLECTOR ® patch, 10 × 14 cm; Alpharma Pharmaceuticals, a subsidiary of Pfizer Inc, New York, NY) or 50 mg oral diclofenac (Voltaren ®; Novartis, East Hanover, NJ). Tissue (skin area of 2 × 2 cm and underlying muscles approximately 2–3 cm in depth) and blood (10 mL) samples were collected at timed intervals up to 11.5 hours after initial patch application or oral administration. The concentrations of diclofenac in plasma, skin, and muscle samples were analyzed using validated ultra performance liquid chromatography tandem mass spectrometric methods.

      Results

      Peak systemic exposure of diclofenac was very low by dermal application compared with oral administration (maximum concentration [C max] values of 3.5 vs 9640 ng/mL, respectively). Absorption of diclofenac into underlying muscles beneath the dermal patch was sustained, and followed apparently zero-order kinetics, with the skin serving as a depot with elevated concentrations of diclofenac. Concentrations of diclofenac in muscles beneath the patch application site were similar to corresponding tissues after oral administration (C max values of 879 and 1160 ng/mL, respectively). In contrast to the wide tissue distribution of diclofenac after oral administration, dermal patch application resulted in high concentrations of diclofenac only on the treated skin and immediate tissue underneath the patch. Low concentrations of diclofenac were observed in the skin and muscles collected from untreated areas contralateral to the site of dermal patch application.

      Conclusion

      Dermal patch application resulted in low systemic absorption and high tissue penetration of diclofenac compared with oral administration.

      Related collections

      Author and article information

      Affiliations
      [1 ]Pfizer Inc, Groton, CT, USA
      [2 ]Tandem Labs, Durham, NC, USA
      [3 ]BioCryst Pharmaceuticals Inc, Durham, NC, USA
      [4 ]Alta Vetta Pharmaceutical Consulting LLC, Durham, NC, USA
      [5 ]Salix Pharmaceuticals Inc, Raleigh, NC, USA
      Author notes
      Correspondence: Susanna Tse, Pfizer Inc, Eastern Point Road, Groton, CT, USA, Tel +1 860 715 5942, Fax +1 860 715 6427, Email susanna.tse@ 123456pfizer.com
      Journal
      J Pain Res
      J Pain Res
      Journal of Pain Research
      Dove Medical Press
      1178-7090
      2012
      23 October 2012
      : 5
      : 401-408
      23166444 3500922 10.2147/JPR.S35450 jpr-5-401
      © 2012 Tse et al, publisher and licensee Dove Medical Press Ltd.

      This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.

      Categories
      Original Research

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