Preparation and in-vitro evaluation of alginate beads of flurbiprofen

The purpose of this study was to prep. and evaluate alginate gel beads as an oral controlled release system of flurbiprofen (FLUP)​.  FLUP is one of the potent nonsteroidal antiinflammatory drugs (NSAIDs) which has deleterious side effects on the GIT such as irritation, ulceration and hemorrhage.  The release of FLUP from alginate beads was strongly affected by pH of the dissoln. medium and drug : polymer ratio.  In all cases the drug release front alginate beads showed nearly zero-​order mechanism.  The release rate of drug was more rapidly in alk. medium (pH 7.4) than that at pH 5.8.  The swelling property of dried alginate beads was of interest.  The beads remained unchanged in acidic medium (pH 1.2 and 5.8) but swelled rather rapidly in pH 7.4 phosphate buffer to a size greater than their original size before being dried.  Such a pH-​sensitive swelling properties could be advantageous for orally administered drug vehicles, esp. when an acid-​sensitive drug or drug that has adverse-​effects on the GIT is incorporated in the beads.  The effect of the intact drug as well as FLUP alginate beads on the ulcerogenic activity of the drug in the stomach of rabbit was carried out.  It was obsd. that, the ulcerogenic activity of the intact drug disappeared and the mucosal surface did not show hemorrhage or inflammation when the drug is loaded with alginate beads.