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Table of Contents
Vol. 19, No. 1, 2006
Issue release date: December 2005
Section title: Original Paper
Skin Pharmacol Appl Skin Physiol 2006;19:17–21
(DOI:10.1159/000089139)

The Role of Menthol in Skin Penetration from Topical Formulations of Ibuprofen 5% in vivo

Brain K.R.a · Green D.M.a · Dykes P.J.b · Marks R.b · Bola T.S.c
aAn-eX Analytical Services Ltd, bDepartment of Medicine (Dermatology), UWCM/Cutest Systems Ltd, Cardiff, and cThe Mentholatum Company, Glasgow, UK

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: April 07, 2005
Accepted: June 29, 2005
Published online: December 07, 2005
Issue release date: December 2005

Number of Print Pages: 5
Number of Figures: 1
Number of Tables: 2

ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)

For additional information: http://www.karger.com/SPP

Abstract

In vivo plasma profiles from formulations containing 5% ibuprofen were compared after a single topical application in a randomised, double-blind, cross-over trial. IbuleveTM gel (Dermal Laboratories, UK) contained only ibuprofen whilst Deep ReliefTM gel (Mentholatum, UK) also contained 3% menthol. In contrast to results obtained when these products were compared under in vitro conditions, there was no statistically significant difference in vivo between delivery of ibuprofen. Estimated relative bioavailability fraction (Deep Relief gel/Ibuleve gel) from log-transformed AUC(0–24h) was 0.99 (95% CI: 0.94–1.04), estimated Cmax ratio was 0.96 (95% CI: 0.91–1.00) and estimated tmax ratio was 1.01 (95% CI: 0.81–1.20). Menthol produces local vasodilation, which reduces skin barrier function, and these data demonstrate that it is inappropriate to extrapolate from in vitro data where formulation components produce biologically-mediated enhancement of permeation which cannot be modelled ex vivo. In clinical use, these products deliver comparable amounts of ibuprofen, but only Deep Reliefgel provides the secondary immediate benefit of the direct analgesic action of menthol.

© 2006 S. Karger AG, Basel


Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: April 07, 2005
Accepted: June 29, 2005
Published online: December 07, 2005
Issue release date: December 2005

Number of Print Pages: 5
Number of Figures: 1
Number of Tables: 2

ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)

For additional information: http://www.karger.com/SPP


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