Cross-linked high amylose starch derivatives as matrices for controlled release of high drug loadings

Selection of hydrogels as excipients in controlled drug release systems depends on the characteristics of the gel and of the drug. Three types of derivatives were synthesized from cross-linked high amylose starch (HASCL-6) by substitution of hydroxylic groups with cationic (carboxymethyl: CM), anionic (aminoethyl: AE) and acetate (Ac) groups. These new polymeric excipients are able to control the release over 20 h from monolithic tablets loaded with 20 to 60% drug. Three drugs were used as model tracer: acetaminophen (uncharged), acetylsalicylic acid (having an acidic group) and metformin (having a basic group). It was found that the release of ionic drugs from CM-HASCL-6 and AE-HASCL-6 matrices can be partially controlled by ionic interaction between pendant groups of polymer and drugs. The substitution degree of HASCL-6 derivatives can also be varied to modulate the drug's release time. These derivatives represent a novel generation of pharmaceutical excipients, recommended for high loading dosage formulations. (C) 2001 Elsevier Science B.V. All rights. reserved.