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Absorption of different oral dosage forms of oxycodone in the elderly: a cross-over clinical trial in patients undergoing cystoscopy

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Abstract

Purpose

To characterize the pharmacokinetics (PK) of oxycodone following intravenous injection and administration of three oral dosage forms (solution, capsule, and controlled-release tablet) in elderly patients (age 76–89 years) undergoing cystoscopy.

Methods

This was an open, randomized study with two sequences and two visits in 15 elderly patients. The patients were given intravenous injection (over 10 min) of 5 mg of oxycodone hydrochloride trihydrate. Oxycodone hydrochloride (5 mg in all forms) was orally administered as a solution, a capsule, and a controlled-release tablet. Venous blood samples were collected up to 17 h after oxycodone administration. Population PK parameters were calculated with NONMEM VI 2.0. For intravenous injection we calculated clearance, volume of distribution at steady state, and the half-life of elimination, and for oral dosage forms also the absolute bioavailability.

Results

Clearance of the intravenous injections was 28.9 L/h; the volume of distribution at steady state and the half-life of elimination were 186 L and 5.2 h, respectively. The absolute bioavailability of oxycodone was 59 % from oral solutions, 64 % from capsules, and 55 % from controlled-release tablets.

Conclusions

Our results indicate that, in the elderly, the bioavailability of the three different oral dosage forms of oxycodone is fairly similar.

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Acknowledgments

The authors would like to thank V.-P. Ranta, PhD (pharm), A. Kuosmanen, BSc (pharm), H. Nordman, MD, and S. Savinainen, MD, for their help in conducting the study.

The authors have no conflicts of interest to report regarding the content of this manuscript. The study did not receive financial support from any external source.

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Correspondence to Hannu Kokki.

Additional information

Some of the study results were presented as an abstract at the Pain Congress, 7th Congress of the European Federation of IASP® Chapters (EFIC®) in Hamburg, Germany, September 2011.

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Kokki, M., Välitalo, P., Rasanen, I. et al. Absorption of different oral dosage forms of oxycodone in the elderly: a cross-over clinical trial in patients undergoing cystoscopy. Eur J Clin Pharmacol 68, 1357–1363 (2012). https://doi.org/10.1007/s00228-012-1267-9

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  • DOI: https://doi.org/10.1007/s00228-012-1267-9

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