Pharmacokinetics, safety and tolerability of a novel tocopheryl phosphate mixture/oxycodone transdermal patch system: a Phase I study

Pain Manag. 2017 Jul;7(4):243-253. doi: 10.2217/pmt-2016-0068. Epub 2017 Apr 19.

Abstract

Aim: To characterize the pharmacokinetic profile and evaluate the safety and tolerability of a transdermal oxycodone patch containing tocopheryl phosphate mixture (TPM).

Patients & methods: Eleven healthy subjects received a single application of three TPM/oxycodone patches applied to the torso for 72 h.

Results: Oxycodone was detected 8.0 ± 2.7-h postpatch administration, reaching a mean maximum plasma concentration of 3.41 ± 1.34 ng/ml at 49.3 ± 21.2 h. The safety profile was consistent with the application method and known side-effect profile of oxycodone and naltrexone. No treatment-limiting skin irritation was observed.

Conclusion: A 3-day application of the TPM/oxycodone patch demonstrated an acceptable safety profile and was well tolerated by healthy subjects, with limited dermal irritation following application.

Keywords: oxycodone; tocopheryl phosphate mixture (TPM); transdermal patch.

Publication types

  • Clinical Trial, Phase I

MeSH terms

  • Adult
  • Analgesics, Opioid* / administration & dosage
  • Analgesics, Opioid* / adverse effects
  • Analgesics, Opioid* / pharmacokinetics
  • Drug Combinations
  • Female
  • Healthy Volunteers
  • Humans
  • Male
  • Oxycodone* / administration & dosage
  • Oxycodone* / adverse effects
  • Oxycodone* / pharmacokinetics
  • Transdermal Patch* / adverse effects
  • alpha-Tocopherol / administration & dosage
  • alpha-Tocopherol / adverse effects
  • alpha-Tocopherol / analogs & derivatives*
  • alpha-Tocopherol / pharmacokinetics

Substances

  • Analgesics, Opioid
  • Drug Combinations
  • alpha-tocopherol phosphate
  • Oxycodone
  • alpha-Tocopherol