title: A comparative ex vivo drug permeation study of beta-blockers through porcine buccal mucosa.
abstract: Apparent permeability coefficients (kp) of a series of beta-blockers: acebutolol, atenolol, labetalol, metoprolol, oxprenolol and propranolol, through porcine buccal mucosa were determined. The aim of the study was to determine the permeation parameters (apparent permeability coefficient, kp; flux, J; and lag time, TL) as a measure of the intrinsic permeability of porcine buccal mucosa to these drugs, in order to predict the efficacy of their possible administration through human buccal mucosa. A positive linear correlation was observed between the apparent permeability coefficient, kpand the partition coefficient, P. Oxprenolol and propranolol are the drugs that presented the highest values of kp: 0.3231×10(2) cm/h and 0.5666×10(2) cm/h, respectively. Multiple linear regression (MLR) using least square estimation was performed on the data set with logkpas dependent variable and the descriptors as predictor variables. The potential systemic capacity after a buccal administration was predicted by estimating the plasma concentrations at steady-stated (Css). Considering the entire process of permeation ex vivo, propranolol and oxprenolol would seem to be the best candidates for administration through the buccal mucosa.
authors.affiliation: Pharmacy Pharmaceutical Technology Department, Biopharmaceutical Pharmacokinetics Unit, Faculty of Pharmacy, Av. Joan XXIII, s/n, Barcelona 08028, Spain.
authors.forename: Sonia
authors.initials: S
authors.lastname: Amores
authors.affiliation: Pharmacy Pharmaceutical Technology Department, Biopharmaceutical Pharmacokinetics Unit, Faculty of Pharmacy, Av. Joan XXIII, s/n, Barcelona 08028, Spain. Electronic address: jaclauroba@ub.edu.
authors.forename: Jacinto
authors.initials: J
authors.lastname: Lauroba
authors.affiliation: Pharmacy Pharmaceutical Technology Department, Biopharmaceutical Pharmacokinetics Unit, Faculty of Pharmacy, Av. Joan XXIII, s/n, Barcelona 08028, Spain.
authors.forename: Ana
authors.initials: A
authors.lastname: Calpena
authors.affiliation: Pharmacy Pharmaceutical Technology Department, Biopharmaceutical Pharmacokinetics Unit, Faculty of Pharmacy, Av. Joan XXIII, s/n, Barcelona 08028, Spain.
authors.forename: Helena
authors.initials: H
authors.lastname: Colom
authors.affiliation: Animal Facility at Bellvitge-University of Barcelona, Spain.
authors.forename: Alvaro
authors.initials: A
authors.lastname: Gimeno
authors.affiliation: Pharmacy Pharmaceutical Technology Department, Biopharmaceutical Pharmacokinetics Unit, Faculty of Pharmacy, Av. Joan XXIII, s/n, Barcelona 08028, Spain.
authors.forename: José
authors.initials: J
authors.lastname: Domenech
mesh_terms: D000278:Administration, Buccal; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D001692:Biological Transport; D006801:Humans; D066298:In Vitro Techniques; D016018:Least-Squares Analysis; D016014:Linear Models; D008954:Models, Biological; D015394:Molecular Structure; D009061:Mouth Mucosa / Q000378:metabolism*; D010096:Oxprenolol / Q000378:metabolism; D010539:Permeability; D011433:Propranolol / Q000378:metabolism; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D000319:Adrenergic beta-Antagonists; D010096:Oxprenolol; D011433:Propranolol
keywords: Beta-blockers; Buccal permeation; Ex vivo drug permeation; Porcine buccal mucosa