Acta Pharm. 69 (2019) 381-398

Original research paper

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

AMIRA A. RASHAD, SARA NAGEEB EL-HELALY, RANDA T. ABD EL REHIM and OMAIMA N. EL-GAZAYERLY

sara.elhelaly@pharma.cu.edu.eg

¹ Mepaco-Medifood Pharmaceutical Company, El Sharkia, Egypt

² Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt

Accepted November 30, 2018

Published online December 14, 2018

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 buccoadhesive 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 showed 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.

Keywords: azelnidipine, liquisol, core-in-cup, buccoadhesive tablets, tablet micromeritics, in vitro release