Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: Physicochemical and technological characterisation

• Published in: European journal of pharmaceutics and biopharmaceutics 2009-05, Vol.72 (1), p.138-147
• Main Authors: Marinich, J.A., Ferrero, C., Jiménez-Castellanos, M.R.
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Chemistry, Pharmaceutical - methods; Compression properties; Drying process; Ethyl methacrylate; Excipients - chemistry; General pharmacology; Graft copolymers; Heckel analysis; Medical sciences; Methylmethacrylates - chemistry; Microscopy, Electron, Scanning; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymers - chemistry; Porosity; Powders; Spectrophotometry - methods; Spectrophotometry, Infrared - methods; Spectroscopy characterisation; Starch; Tablets; Technology, Pharmaceutical - methods; Temperature; Waxy maize starch; X-Rays; Zea mays
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2008.12.008

Nowadays, graft copolymers are being used as an interesting option when developing a direct compression excipient for controlled release matrix tablets. New graft copolymers of ethyl methacrylate (EMA) on waxy maize starch (MS) and hydroxypropylstarch (MHS) were synthesised by free radical polymerization and alternatively dried in a vacuum oven (OD) or freeze-dried (FD). This paper evaluates the performance of these new macromolecules and discusses the effect of the carbohydrate nature and drying process on their physicochemical and technological properties. Grafting of EMA on the carbohydrate backbone was confirmed by IR and NMR spectroscopy, and the grafting yields revealed that graft copolymers present mainly a hydrophobic character. The graft copolymerization also leads to more amorphous materials with larger particle size and lower apparent density and water content than carbohydrates (MS, MHS). All the products show a lack of flow, except MHSEMA derivatives. MSEMA copolymers underwent much plastic flow and less elastic recovery than MHSEMA copolymers. Concerning the effect of drying method, FD derivatives were characterised by higher plastic deformation and less elasticity than OD derivatives. Tablets obtained from graft copolymers showed higher crushing strength and disintegration time than tablets obtained from raw starches. This behaviour suggests that these copolymers could be used as excipients in matrix tablets obtained by direct compression and with a potential use in controlled release.