Effects of l-Menthol and dl-Camphor on the Penetration and Hydrolysis of Methyl Salicylate in Hairless Mouse Skin.

Yano, Tadanori; Kanetake, Tohru; Saita, Masaru; Noda, Kanji

doi:10.1248/bpb1978.14.663

Cited by 30 publications

(15 citation statements)

References 16 publications

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“…Very little is known about the dermal absorption of these 3 compounds. One author has shown that the absorption of methyl salicylate could be increased in the presence of the other 2 compounds 17 …”

mentioning

confidence: 99%

Dermal Absorption of Camphor, Menthol, and Methyl Salicylate in Humans

Martin

Valdez

Boren

et al. 2004

The Journal of Clinical Pharma

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Camphor, menthol, and methyl salicylate occur in numerous over-the-counter products. Although extensively used, there have been no estimates of human exposure following administration via dermal application. Furthermore, there is little information about the pharmacokinetics of those compounds. The authors report the plasma concentrations of the intact compounds as a function of dose following dermal patch application. Three groups of 8 subjects (4 male, 4 female) applied a different number of commercial patches (2, 4, or 8) to the skin for 8 hours. Plasma samples were assayed using sensitive and selective gas-chromatographic methods. For the 8-patch group, the average maximum plasma concentrations (Cmax +/- SD) were 41.0 +/- 5.8 ng/mL, 31.9 +/- 8.8 ng/mL, and 29.5 +/- 10.5 ng/mL for camphor, menthol, and methyl salicylate, respectively. The corresponding values for the 4-patch group were 26.8 +/- 7.2 ng/mL, 19.0 +/- 5.4 ng/mL, and 16.8 +/- 6.8 ng/mL. The harmonic mean terminal half-lives were 5.6 +/- 1.3 hours, 4.7 +/- 1.6 hours, and 3.0 +/- 1.2 hours for camphor, menthol, and methyl salicylate, respectively. The 2-patch group had measurable but low plasma concentrations of each compound. Low-dose dermal application for an extended time results in low plasma concentrations of all 3 compounds. Four and 8 patches, when applied for 8 hours, gave measurable and nearly proportional plasma concentrations. Although unable to determine the absolute dermal bioavailability of these compounds, there appears to be relatively low systemic exposure to these potentially toxic compounds, even when an unrealistically large number of patches are applied for an unusually long time.

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confidence: 99%

Dermal Absorption of Camphor, Menthol, and Methyl Salicylate in Humans

Martin

Valdez

Boren

et al. 2004

The Journal of Clinical Pharma

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“…Дополнительные ком-поненты метилсалицилата, камфоры и левоментола в виде липофильных и амфифильных молекул проникают через кожу в подлежащие ткани и также оказывают местное бо-леутоляющее и противовоспалительное действие [18][19][20][21].…”

Section: The Efficacy and Safety Of Carmolis Gelunclassified

The Efficacy and Safety of Carmolis Gel in the Combination Therapy of Knee Osteoarthritis: Results of a Multicenter Clinical Trial

Denisov¹,

Зборовская²,

Заводовский³

et al. 2015

rsp

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“…Yano et al [28] reported that l-menthol inhibited the bioconversion of methyl salicylate in hairless mouse skin homogenate. Ethanol, commonly used as a chemical enhancer in transdermal therapeutic systems [29][30][31] , was an enzymatic inhibitor of bioconversion from estradiol to esterone [32] and from prednisolone farnesylate to prednisolone [33] in hairless mouse skin.…”

Section: Chemical Enhancement and Additivesmentioning

confidence: 99%

Skin Metabolism in Transdermal Therapeutic Systems

Hikima

Tojo²,

Maibach³

2005

Skin Pharmacol Physiol

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Skin has at least two barriers with protective functions: the stratum corneum physical barrier and a biochemical barrier in the epidermis and dermis. Numerous chemical and physical enhancers exist for transdermal therapeutic systems; some cause irritation, and possibly influence enzyme deactivation. Knowledge of enzymatic skin reactions is important for developing safe and efficacious transdermal systems for treatment not only of skin diseases but also for systemic application. This paper overviews the effects of (a) chemical enhancers and additives, (b) drug structure, and (c) physical enhancement on skin metabolism.

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Effects of l-Menthol and dl-Camphor on the Penetration and Hydrolysis of Methyl Salicylate in Hairless Mouse Skin.

Cited by 30 publications

References 16 publications

Dermal Absorption of Camphor, Menthol, and Methyl Salicylate in Humans

Dermal Absorption of Camphor, Menthol, and Methyl Salicylate in Humans

The Efficacy and Safety of Carmolis Gel in the Combination Therapy of Knee Osteoarthritis: Results of a Multicenter Clinical Trial

Skin Metabolism in Transdermal Therapeutic Systems

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