A comparative ex vivo drug permeation study of beta-blockers through porcine buccal mucosa

作者：Amores Sonia; Lauroba Jacinto^*; Calpena Ana; Colom Helena; Gimeno Alvaro; Domenech Jose

来源：International Journal of Pharmaceutics, 2014, 468(1-2): 50-54.

DOI：10.1016/j.ijpharm.2014.03.050

• Buccal permeation
• Beta-blockers
• Porcine buccal mucosa
• Ex vivo drug permeation

Apparent permeability coefficients (k(p)) 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, k(p); flux, J; and lag time, T-L) 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, k(p)and the partition coefficient, P. Oxprenolol and propranolol are the drugs that presented the highest values of k(p): 0.3231 x 10(2) cm/h and 0.5666 x 10(2) cm/h, respectively. Multiple linear regression (MLR) using least square estimation was performed on the data set with log k(p)as 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 (C-ss). Considering the entire process of permeation ex vivo, propranolol and oxprenolol would seem to be the best candidates for administration through the buccal mucosa.

• 出版日期2014-7-1