Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging – Effect of solubility of additives on HPMC matrix tablets
Artikel i vetenskaplig tidskrift, 2009

Extensive studies of extended release tablets based on hydrophilic polymers have illuminated several aspects linked to their functionality. However, in some respects key factors affecting the mechanisms of release are yet unexplored. In the present study, a novel NMR-microimaging method has been used to study the influence of the solubility of additives in extended release hydroxypropyl methylcellulose (HPMC) matrix tablets. During the course of the tablet dissolution the movement of the swelling and erosion fronts were studied simultaneously to the release of both polymer and additives. Moreover, the focused beam reflectance measurement (FBRM) technology was for the first time assessed for both release and dissolution rate studies of poorly soluble particles. The studied formulations comprised solely HPMC, 40% HPMC and 60% mannitol (Cs = 240 mg/ml) and 40% HPMC and 60% dicalcium phosphate (DCP) (Cs = 0.05 mg/ml). The dissolution rate of the tablets was highest for the HPMC/mannitol formulation, followed by HPMC/DCP and plain HPMC tablet. A contrasting order was found regarding the degree and kinetics of swelling. The results were interpreted in light of how the mass transport in the gel layer is influenced by the solubility of additives. A mechanistic model, considering osmotic pressure gradient and the effective diffusion of the dissolution medium in the gel is proposed.

Författare

Farhad Tajarobi

Chalmers, Kemi- och bioteknik, Farmaceutisk teknologi

SuMo Biomaterials

Susanna Abrahmsén-Alami

AstraZeneca Sweden

A. Carlsson

AstraZeneca Sweden

Anette Larsson

SuMo Biomaterials

Chalmers, Kemi- och bioteknik, Farmaceutisk teknologi

European Journal of Pharmaceutical Sciences

0928-0987 (ISSN)

Vol. 37 89-97

Ämneskategorier

Farmaceutisk vetenskap

DOI

10.1016/j.ejps.2009.01.008