Data di Pubblicazione:
2007
Citazione:
Ex vivo study of transdermal permeation of four diclofenac salts from different vehicles / P. Minghetti, F. Cilurzo, A. Casiraghi, L. Montanari, A. Fini. - In: JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0022-3549. - 96:4(2007), pp. 814-823.
Abstract:
The ex vivo permeation of diclofenac was studied using four different salts
(sodium, potassium, diethylamine, and epolamine) dissolved in four different solvents (water, propylene glycol (PG), Transcutol, and oleic acid (OA)) as donor phases through a human skin membrane. The four salts show different solubility values and different behavior in the four solvents, which are also permeation enhancers and this fact further is connected to the permeation results. The same order of magnitude of fluxes through the membrane as those previously reported for acidic diclofenac released from buffer solutions of pH >7 were found, taking into account differences originated by different membranes and other parameters tested in the experiments. Saturation concentration for the four salts in different solvents, necessary to calculate permeation coefficients, was
critically evaluated; a short discussion made it possible to explain that corrections in the solubility values must be considered, related to the complex behavior in solution of these salts. Statistical processing of the experimental data suggests that differences between the four salts in promoting absorption of the drug is unproven; while differences are
evident between the solvents, water is the most effective enhancing vehicle. Aqueous
formulations containing diclofenac salt with an organic base appear to be the best
combination to promote permeation in topical applications
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Counterions; Diclofenac salts; Permeability coefficient; Permeation enhancer vehicles; Solubility; Transdermal permeation
Elenco autori:
P. Minghetti, F. Cilurzo, A. Casiraghi, L. Montanari, A. Fini
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