Buoyant sustained release granules based on chitosan.

Abstract

Attempts to develop sustained release intragastric 'floating' granules based on chitosan are described, using chitosan of different degrees of deacetylation (chitosan H and L), in granular form or in laminated preparations. The granules were made from chitosan H (chitosan H granules), from a 1:1 mixture of chitosan H and L (1:1 mixture granules), from a 1:2 mixture of chitosan H and L (1:2 mixture granules), or from chitosan L (chitosan L granules). They were prepared by a method involving deacidification, had internal cavities, were immediately buoyant in both acidic and neutral fluids, and gave sustained release of prednisolone (used as a model drug). The laminated preparations, composed of a chitosan granule layer and a chitosan L membrane, were also immediately buoyant in the same fluids, and also provided sustained release of the model drug. The release properties were controlled by regulating the chitosan L content of the granules, or the chitosan L membrane thickness of the laminate. In an absorption study using beagle dogs, sustained drug absorption from these preparations was obtained.