title: Use of Permeapad® for prediction of buccal absorption: A comparison to in vitro, ex vivo and in vivo method.
abstract: The present work explores the usefulness of Permeapad® for prediction of buccal absorption. Permeability studies with the model drug metoprolol were carried out using the Permeapad® barrier at pH values 7.4; 8.5; 9.0, and 9.5. It was confirmed that Permeapad® can withstand these conditions, and as expected, a clear increase in permeability was found with increasing pH. The permeation results across Permeapad® were compared to published in vitro, ex vivo and in vivo studies for the same formulations. Results showed that the permeability of metoprolol using the Permeapad® barrier correlated very well to both in vitro and ex vivo studies, (r(2)=0.98 and 0.97), respectively. Furthermore, excellent in vitro in vivo correlation IVIVC (r(2)=0.98) was obtained when comparing apparent permeability coefficient to the absolute bioavailability of metoprolol administered buccally to mini-pigs. Results indicate that Permeapad® can be used to mimic the buccal absorption of metoprolol as a faster and less laborious method as compared to any of the other mentioned methods.
authors: University of Southern Denmark, Campusvej 55, DK-5230 Odense, Denmark.
authors: Hanady Ajine
authors: HA
authors: Bibi
authors: Biologics and Pharmaceutical Science, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark.
authors: René
authors: R
authors: Holm
authors: University of Southern Denmark, Campusvej 55, DK-5230 Odense, Denmark. Electronic address: annette.bauer@sdu.dk.
authors: Annette
authors: A
authors: Bauer-Brandl
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008790:Metoprolol / Q000008:administration & dosage / Q000493:pharmacokinetics; D009061:Mouth Mucosa / Q000378:metabolism; D065568:Oral Mucosal Absorption; D010539:Permeability; D013552:Swine; D013556:Swine, Miniature
chemical_list: D008790:Metoprolol
keywords: Buccal absorption; IVIVC; In vitro; Metoprolol; Permeability; Permeapad®; pH