生物等效性和生物利用度杂志

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Galantamine Delivery on Buccal Mucosa: Permeation Enhancement and Design of Matrix Tablets

V. De Caro, G. Giandalia, M.G. Siragusa, G. Campisi and L.I. Giannola

The most important feature in transbuccal drug delivery is the low drug passage through the buccal mucosa. In our previous work we demonstrated the aptitude of Galantamine to penetrate the buccal tissue. The collected data suggested that Galantamine passively crosses the membrane, but the calculated Js and Kp values showed that the drug amount that crosses the membrane wasn’t sufficient to assure blood therapeutic level. So, in this study, ex vivo permeation tests, using porcine buccal mucosa, were performed in presence of physical or chemical enhancers. No significant differences in penetration rate were observed using chemical enhancers as sodium dehydrocholate, EDTA disodium salt and trisodium citrate dihydrate; while, Js and Kp were extensively affected by application of electric fields. Tablets, designed for Galantamine administration on buccal mucosa, were prepared by direct compression of drug loaded Eudragit® RS 100 matrices. When the tablets were coated with lipophilic material, Galantamine is slowly discharged from buccal tablets, following the Higuchian kinetic. Buccal tablets containing Galantamine may represent a potential alternative dosage form in Alzheimer management.