The Role of Menthol in Skin Penetration from Topical Formulations of Ibuprofen 5% in vivo
In vivo plasma profiles from formulations containing 5% ibuprofen were compared after a single topical application in a randomised, double-blind, cross-over trial. Ibuleve TM gel (Dermal Laboratories, UK) contained only ibuprofen whilst Deep Relief TM gel (Mentholatum, UK) also contained 3% menthol....
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| Veröffentlicht in: | Skin pharmacology and physiology 2006-01, Vol.19 (1), p.17-21 |
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| container_title | Skin pharmacology and physiology |
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| creator | Brain, K.R. Green, D.M. Dykes, P.J. Marks, R. Bola, T.S. |
| description | In vivo plasma profiles from formulations containing 5% ibuprofen were compared after a single topical application in a randomised, double-blind, cross-over trial. Ibuleve TM gel (Dermal Laboratories, UK) contained only ibuprofen whilst Deep Relief TM 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 C max ratio was 0.96 (95% CI: 0.91–1.00) and estimated t max 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. |
| doi_str_mv | 10.1159/000089139 |
| format | Article |
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Ibuleve TM gel (Dermal Laboratories, UK) contained only ibuprofen whilst Deep Relief TM 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 C max ratio was 0.96 (95% CI: 0.91–1.00) and estimated t max 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.</description><identifier>ISSN: 1660-5527</identifier><identifier>EISSN: 1660-5535</identifier><identifier>DOI: 10.1159/000089139</identifier><identifier>PMID: 16247245</identifier><language>eng</language><publisher>Basel, Switzerland: S. 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Karger AG Dec 2005</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c330t-e76e5b8a632dd11fc87a35e514b71491ea02d63a46a45043364ce776deee99633</citedby><cites>FETCH-LOGICAL-c330t-e76e5b8a632dd11fc87a35e514b71491ea02d63a46a45043364ce776deee99633</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,2423,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16247245$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Brain, K.R.</creatorcontrib><creatorcontrib>Green, D.M.</creatorcontrib><creatorcontrib>Dykes, P.J.</creatorcontrib><creatorcontrib>Marks, R.</creatorcontrib><creatorcontrib>Bola, T.S.</creatorcontrib><title>The Role of Menthol in Skin Penetration from Topical Formulations of Ibuprofen 5% in vivo</title><title>Skin pharmacology and physiology</title><addtitle>Skin Pharmacol Physiol</addtitle><description>In vivo plasma profiles from formulations containing 5% ibuprofen were compared after a single topical application in a randomised, double-blind, cross-over trial. Ibuleve TM gel (Dermal Laboratories, UK) contained only ibuprofen whilst Deep Relief TM 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 C max ratio was 0.96 (95% CI: 0.91–1.00) and estimated t max 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. 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Ibuleve TM gel (Dermal Laboratories, UK) contained only ibuprofen whilst Deep Relief TM 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 C max ratio was 0.96 (95% CI: 0.91–1.00) and estimated t max 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.</abstract><cop>Basel, Switzerland</cop><pub>S. Karger AG</pub><pmid>16247245</pmid><doi>10.1159/000089139</doi><tpages>5</tpages></addata></record> |
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| ispartof | Skin pharmacology and physiology, 2006-01, Vol.19 (1), p.17-21 |
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| source | Karger Journals; MEDLINE; Alma/SFX Local Collection |
| subjects | Administration, Cutaneous Adult Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Antipruritics - administration & dosage Antipruritics - pharmacology Cross-Over Studies Double-Blind Method Drug Combinations Female Humans Ibuprofen - administration & dosage Ibuprofen - pharmacokinetics Male Menthol - administration & dosage Menthol - pharmacology Middle Aged Original Paper Skin Absorption - drug effects |
| title | The Role of Menthol in Skin Penetration from Topical Formulations of Ibuprofen 5% in vivo |
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