Metronidazole thermogel improves retention and decreases permeation through the skin

ABSTRACT Metronidazole (MTZ) is widely used as the standard antibiotic for the treatment of rosacea and, more recently, is being used off label in Brazilian hospitals for the treatment of wounds. Following oral administration, minimal amounts of active agent reaches the skin and side effects are strongly induced. Consequently, MTZ is currently being applied topically in order to improve the therapeutic efficacy with reduced side effects, with Rozex(r) (RZ) (an MTZ gelled formulation) being the only marketed product. This study examined whether the use of MTZ 0.75% from thermogel formulations could improve drug retention and reduce dermal exposure compared to that by Rozex(r). Following a 21 h permeation study, the highest total amount of MTZ permeated through the rat healthy and disturbed skin was seen with Rozex(r), but similar to all formulations regardless of the skin condition. On the other hand, the amount retained in the epidermis/dermis was larger for thermogel formulations; at least 4 fold that of Rozex(r), when the stratum corneum was present as a barrier. In conclusion, thermogel formulations can be favorable alternatives to Rozex(r) for the topical application of MTZ with improved efficacy and reduced side effects.

Análise e estudo viscosimétrico de diferentes géis de cetoprofeno 2.5% / Analysis and viscosimetric study of various 2.5% ketoprofen gels

O cetoprofeno é um fármaco pertencente à classe dos anti-inflamatórios não-esteroidais, inibe a síntese de prostaglandinas promovendo um potente efeito analgésico e anti-inflamatório. Para uso tópico, está disponível como medicamento de referência e diversos genéricos sob a forma gel 2,5%, além das preparações manipuladas em farmácias magistrais, adquiridas mediante receita médica. Este estudo objetivou avaliar a qualidade do cetoprofeno gel 2,5% manipulado em duas farmácias do Recife (PE) e, posteriormente, compará-lo ao medicamento de referência e a um genérico correspondente. Os resultados das análises mostraram que medicamentos referência e o genérico apresentaram, de forma geral, características semelhantes. As formulações magistrais também mostraram características próximas entre si, mas diferentes dos industrializados, indicando a necessidade de reformulação destas preparações magistrais avaliadas, como obediência à legislação vigente RDC 67/2007 da Agência Nacional de Vigilância Sanitária.

Ketoprofen is a non-steroidal anti-inflammatory drug that inhibits prostaglandin synthesis and promotes a strong analgesic and anti-inflammatory effect. For topical use, it is available as a reference drug as well as several generic preparations in gel at 2.5%, apart from preparations compounded in pharmacies and sold under medical prescription. The aim of this study was to assess the quality of 2.5% ketoprofen gels compounded in two pharmacies in Recife and then compare them with a reference drug and a corresponding generic drug. The results of the analysis show that the generic and reference drugs display, in general, similar characteristics. The compounded formulations also had similar characteristics, when compared to each other, but were different from the manufactured gels. These results indicate that these compounded preparations must be reformulated to comply with RDC 67/2007, the current regulation issued by the National Agency of Sanitary Surveillance (ANVISA).