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Merck

Development of a novel triamcinolone acetonide-loaded spray solution for the treatment of stomatitis.

Die Pharmazie (2014-07-31)
Dong Wuk Kim, Yong-Il Kim, Fakhar Ud Din, Kwan Hyung Cho, Jong Oh Kim, Han-Gon Choi
RÉSUMÉ

To develop a novel triamcinolone acetonide (TAA)-loaded spray for the treatment of stomatitis, several spray solutions were prepared using various amounts of TAA, Eudragit L100 (Eudragit L) and PEG 400, and 100 ml ethanol. Their viscosity and spraying potential were investigated, with the result that the spraying threshold was 9.5 cP. The effect of PEG 400 on the properties of films formed after spraying was assessed. Its anti-inflammatory effect in mice was evaluated and compared to a commercial product. As the PEG 400 concentration increased, the film elongation and washability by the saliva solution increased, and tensile strength decreased. PEG 400 had little effect on mucoadhesive force and drug release. The TAA-loaded spray solution containing TAA, Eudragit L, PEG 400 and ethanol at the ratio of 1:6:3:100 (w/w/w/v) was easy to spray onto stomatitis lesions in the mouth via a spraying vessel incorporating a long straw. After spraying, the TAA-loaded spray formed a film with suitable elongation, tensile strength and washability that attached onto the mucosal membrane and released the drug. Moreover, it had excellent anti-inflammatory properties, similar to those of the commercial product. Thus, this novel TAA-loaded spray solution was easy to administer, had good film properties and excellent anti-inflammatory efficacy, and is therefore a potential candidate for the treatment of stomatitis.

MATÉRIAUX
Référence du produit
Marque
Description du produit

Sigma-Aldrich
Poly(methyl methacrylate-co-methacrylic acid), average Mw ~34,000 by GPC, average Mn ~15,000 by GPC
USP
Triamcinolone acetonide, United States Pharmacopeia (USP) Reference Standard
USP
Methacrylic acid copolymer type C, United States Pharmacopeia (USP) Reference Standard
USP
Methacrylic acid copolymer type B, United States Pharmacopeia (USP) Reference Standard
Supelco
Triamcinolone acetonide, analytical standard
Triamcinolone acetonide, European Pharmacopoeia (EP) Reference Standard
Triamcinolone acetonide for system suitability, European Pharmacopoeia (EP) Reference Standard