Synthesis of hydroxypropyl methacrylate/polysaccharide graft copolymers as matrices for controlled release tablets.
Hydrophilic matrices are an interesting option when developing drug delivery systems. With this aim, hydroxypropyl methacrylate was grafted onto hydroxypropyl starch and hydroxypropyl cellulose substrates by following the Ce(IV) redox initiation method. Different amounts of ethyleneglycol' dimethacrylate, 7 and 34 mol%, as the crosslinking monomer, were also added. The drying of grafted products was carried out by lyophilization, obtaining white powders. Reaction yields (percent grafting, grafting efficiency, etc.) and some physical characteristics of the powders (particle size, moisture uptake, density, morphology, etc.) were determined. These parameters indicate how useful these products may be as potential matrices for direct compressed tablets. In this light, the powder flowability and the binding properties of each copolymer were determined. The graft copolymers can be considered of great interest as direct compression excipients. Due to their different chemical structure and composition, they showed differences in viscoelastic properties that revealed an interesting range of possibilities for use in drug delivery formulations. Tablets formulated with conventional excipients were also tested. Dissolution tests of various tablets were carried out. In 12 hr, 60-80% of the model drugs was released.
Goñi
I
I
Dpto. Ciencia y Tecnología de Polímeros, Facultad de Química, Universidad del País Vasco, Apartado 1072, San Sebastián, Spain.
Ferrero
M C
MC
Jiménez-Castellanos
R M
RM
Gurruchaga
M
M
D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D019245:Compressive Strength; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry; D020100:Hydrogels; D008689:Methacrylates / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000138:chemical synthesis*; D011134:Polysaccharides / Q000737:chemistry*; D011208:Powders; D012212:Rheology; D012995:Solubility; D013213:Starch / Q000031:analogs & derivatives / Q000737:chemistry; D013607:Tablets; D013806:Theophylline / Q000737:chemistry; D014867:Water
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D020100:Hydrogels; D008689:Methacrylates; D011108:Polymers; D011134:Polysaccharides; D011208:Powders; D013607:Tablets; D014867:Water; D002482:Cellulose; D013213:Starch; C008079:hydroxypropylcellulose; D013806:Theophylline; C032802:hydroxypropyl methacrylate