Study of the influence of alkalizing components on matrix pellets prepared by extrusion/spheronization

Abstract

The aim of this study was to investigate the effects of alkalizing components and the nature of the wetting liquid on the properties of matrix pellets prepared by extrusion and spheronization. Atenolol was used as an active pharmaceutical ingredient, ethylcellulose as a matrix former, microcrystalline cellulose as a filler and disodium phosphate anhydrous and trisodium phosphate dodecahydrate as alkalizing materials. Water and a water-ethanol mixture served as granulation liquids. Pellet formation was evaluated via mechanical, dissolution and morphological studies. In order to enhance the dissolution of Atenolol from the pellets, alkalizing components were used and the influence of these components on the pH was tested. Investigations of the breaking hardness, the morphology and the dissolution revealed that the pellets containing trisodium phosphate dodecahydrate and prepared with a higher amount of water as binding liquid displayed the best physico-chemical parameters and uniform dissolution. In in vitro experiments, the dissolution release complied with the texture of the pellets and the effect of pH. The pellets have suitable shape and very good hardness for the coating process and are appropriate for subsequent in vivo experiments.

Delayed release matrix pellet preparation containing an alkalizing pore-former agent

“…In order to obtain a very good mass for this process, it is necessary to use MCC and the matrix former together. Ethylcellulose (EC) has frequently been used as a coating material for tablets and pellets (Wallace, 1990;Iyer et al, 1993;Ye et al, 2007) and as a binder in the preparation of microcapsules and microspheres, but it is also used as a monolithic matrix former for formulations in which modified drug release is ensured by diffusion (Corti et al, 2008;Huang et al, 2006;Fan et al, 2001). Several commercially available polymers are suitable for the coating of pharmaceutical dosage forms (McGinity, 1997), and some can be used to control the drug release kinetics.…”

Development and characterization of matrix pellets prepared by extrusion / sheronization of atenolol

“…Preparation of a multiparticulate matrix system with an alkalizing component is a reasonable way to ensure an appropriately alkaline micromilieu (Hamedelniel et al, 2010a). Trisodium phosphate dodecahydrate was incorporated as alkalizing and pore-former substance; our previous work had revealed that a matrix-former polymer is required to control the parallel release of At and the alkalizing component utilized (Hamedelniel et al, 2010b) and to ensure that the dosage form reaches the intestine in intact form. Thus, it is necessary to prepare a delayed-release product.…”