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Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: physicochemical and technological characterisation.
Eur J Pharm Biopharm. 2009 May; 72(1):138-47.EJ

Abstract

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.

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Authors+Show Affiliations

Marinich JA
Departamento Farmacia y Tecnología Farmacéutica, Universidad de Sevilla, Sevilla, Spain.
Ferrero C
No affiliation info available
Jiménez-Castellanos MR
No affiliation info available

MeSH

Chemistry, PharmaceuticalExcipientsMethylmethacrylatesMicroscopy, Electron, ScanningParticle SizePolymersPorosityPowdersSpectrophotometrySpectrophotometry, InfraredStarchTabletsTechnology, PharmaceuticalTemperatureX-RaysZea mays

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19146956

Citation

Marinich, J A., et al. "Graft Copolymers of Ethyl Methacrylate On Waxy Maize Starch Derivatives as Novel Excipients for Matrix Tablets: Physicochemical and Technological Characterisation." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 72, no. 1, 2009, pp. 138-47.
Marinich JA, Ferrero C, Jiménez-Castellanos MR. Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: physicochemical and technological characterisation. Eur J Pharm Biopharm. 2009;72(1):138-47.
Marinich, J. A., Ferrero, C., & Jiménez-Castellanos, M. R. (2009). Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: physicochemical and technological characterisation. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 72(1), 138-47. https://doi.org/10.1016/j.ejpb.2008.12.008
Marinich JA, Ferrero C, Jiménez-Castellanos MR. Graft Copolymers of Ethyl Methacrylate On Waxy Maize Starch Derivatives as Novel Excipients for Matrix Tablets: Physicochemical and Technological Characterisation. Eur J Pharm Biopharm. 2009;72(1):138-47. PubMed PMID: 19146956.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: physicochemical and technological characterisation. AU - Marinich,J A, AU - Ferrero,C, AU - Jiménez-Castellanos,M R, Y1 - 2008/12/25/ PY - 2008/05/25/received PY - 2008/07/29/revised PY - 2008/12/15/accepted PY - 2009/1/17/entrez PY - 2009/1/17/pubmed PY - 2009/9/22/medline SP - 138 EP - 47 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 72 IS - 1 N2 - 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. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/19146956/Graft_copolymers_of_ethyl_methacrylate_on_waxy_maize_starch_derivatives_as_novel_excipients_for_matrix_tablets:_physicochemical_and_technological_characterisation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(08)00484-0 DB - PRIME DP - Unbound Medicine ER -