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Transdermal Permeation and Skin Retention of Diclofenac and Etofenamate/Flufenamic Acid From Over-the-Counter Pain Relief Products
M. Kopečná, A. Kováčik, P. Novák, M. Boncheva Bettex, K. Vávrová
Language English Country United States
Document type Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Anti-Inflammatory Agents, Non-Steroidal MeSH
- Administration, Cutaneous MeSH
- Pain MeSH
- Diclofenac * MeSH
- Gels MeSH
- Skin Absorption MeSH
- Flufenamic Acid * analogs & derivatives MeSH
- Humans MeSH
- Permeability MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
Topical pain relief products differ in the type of drug, concentration, and formulation. All these factors influence the drug transit through the skin barrier, and its eventual retention in the skin as a reservoir for subsequent release. In addition, the drug potency can be different, which is important for the product efficacy. We studied here ex vivo human skin permeation and retention of five over-the-counter NSAID gels containing 2.32% diclofenac (DIC) and 5-10% etofenamate (ETF). The potency of the permeated/retained drug amounts were compared using a composite parameter, the Index of Relative Topical Anti-inflammatory Activity (IRTAA), which is calculated as the product of the skin permeation/retention and the drug relative potency. The IRTAAs of the DIC gel were 94-667-fold higher and 72-208-fold higher for transdermal delivery and skin retention, respectively, than IRTAAs of the ETF gels. These superior IRTAAs indicate that DIC delivered by this topical formulation would achieve a higher bioactivity and would form a potent drug reservoir relevant for its subsequent long-lasting release.
GSK Consumer Healthcare S A Route de l'Etraz 2 Case Postale 1279 Nyon 1260 Switzerland
GSK Consumer Healthcare s r o Hvězdova 1734 2c 140 00 Praha 4 Czech Republic
References provided by Crossref.org
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