Pharmacokinetics, Safety and Tolerability of a Novel Tocopheryl Phosphate Mixture/Oxycodone Transdermal Patch System: A Phase I Study

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

Financial & competing interests disclosure

PD Gavin and AJ Smith are full-time employees of Phosphagenics Limited, Victoria, Australia. LS Simon and T Schlagheck report no conflicts. S Shakib received consulting fees from the IDT CMAX Drug Studies Unit, Adelaide, Australia, where the study was conducted. This study was funded by Phosphagenics Limited, Victoria, Australia. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Writing assistance was provided by G Williams, Health Writers S.L.U.

Ethical conduct of research

The study was approved by Bellberry Human Research Ethics Committee (Therapeutic Goods Administration [TGA] Clinical Trial Notification number 2013/0168) and performed and conducted in accordance with the standards of International Conference on Harmonization (Note for Guidance on Good Clinical Practice [CPMP/ICH/135/95] – annotated with TGA Comments) and the Declaration of Helsinki. All subjects were included after having given their informed consent.

Additional information

Funding

PD Gavin and AJ Smith are full-time employees of Phosphagenics Limited, Victoria, Australia. LS Simon and T Schlagheck report no conflicts. S Shakib received consulting fees from the IDT CMAX Drug Studies Unit, Adelaide, Australia, where the study was conducted. This study was funded by Phosphagenics Limited, Victoria, Australia. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. Writing assistance was provided by G Williams, Health Writers S.L.U.