<abstract xmlns="http://www.w3.org/1999/xhtml"><p>Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 3<sup>3</sup> factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and <italic>in vitro</italic> release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.</p></abstract>

Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.

Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, <italic>in vitro</italic> release, and mucoadhesive strength

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics,  release, and mucoadhesive strength

Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These...

Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Publié en ligne: 26 juin 2019

Pages: 381 - 398

Accepté: 30 nov. 2018

DOI: https://doi.org/10.2478/acph-2019-0022

Mots clés
azelnidipine, liquisol, core-in-cup, buccoadhesive tablets, tablet micromeritics, release

© 2019 Amira A. Rashad et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Publié en ligne: 26 juin 2019

Pages: 381 - 398

Accepté: 30 nov. 2018

DOI: https://doi.org/10.2478/acph-2019-0022

Mots clésazelnidipine, liquisol, core-in-cup, buccoadhesive tablets, tablet micromeritics, release

© 2019 Amira A. Rashad et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
azelnidipine, liquisol, core-in-cup, buccoadhesive tablets, tablet micromeritics, release