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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.

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          Author and article information

          Journal
          J Pain Res
          J Pain Res
          Journal of Pain Research
          Dove Medical Press
          1178-7090
          2012
          23 October 2012
          : 5
          : 401-408
          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
          Article
          jpr-5-401
          10.2147/JPR.S35450
          3500922
          23166444
          © 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

          Anesthesiology & Pain management

          nsaids, systemic absorption, tissue distribution, topical patch

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