Use of Permeapad® for prediction of buccal absorption: A comparison to in vitro, ex vivo and in vivo method

Eur J Pharm Sci. 2016 Oct 10:93:399-404. doi: 10.1016/j.ejps.2016.08.041. Epub 2016 Aug 24.

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.

Keywords: Buccal absorption; IVIVC; In vitro; Metoprolol; Permeability; Permeapad®; pH.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Drug Delivery Systems*
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Metoprolol / administration & dosage
  • Metoprolol / pharmacokinetics
  • Mouth Mucosa / metabolism
  • Oral Mucosal Absorption*
  • Permeability
  • Swine
  • Swine, Miniature

Substances

  • Metoprolol