Synthesis of hydroxypropyl methacrylate/polysaccharide graft copolymers as matrices for controlled release tablets

被引:21
作者
Goñi, I
Ferrero, MC
Jiménez-Castellanos, RM
Gurruchaga, M
机构
[1] Univ Basque Country, Dept Ciencia & Tecnol Polimeros, San Sebastian, Spain
[2] Univ Seville, Fac Farm, Dept Farm & Tecnol Farmaceut, E-41012 Seville, Spain
关键词
controlled release; direct compression; graft copolymers; poly(hydroxypropyl methacrylate); polysaccharide;
D O I
10.1081/DDC-120014577
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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, here 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 here determined. The graft copolymers cart 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 carious tablets were carried out. In 12 hr, 60-80% of the model drugs was released.
引用
收藏
页码:1101 / 1115
页数:15
相关论文
共 25 条
[1]  
[Anonymous], 1985, J CONTROL RELEASE
[2]   PREPARATION OF A NOVEL TYPE OF CONTROLLED-RELEASE CARRIER AND EVALUATION OF DRUG RELEASE FROM THE MATRIX TABLET AND ITS PHYSICAL-PROPERTIES [J].
AOKI, S ;
OHWAKI, T ;
UESUGI, K ;
TATSUISHI, K ;
OZAWA, H ;
KAYANO, M .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1992, 85 (1-3) :29-38
[3]  
BOLHUIS GK, 1973, PHARM WEEKBLAD, V108, P469
[4]   RHEOLOGICAL BEHAVIOR OF HYDROPHILIC POLYMERS AND DRUG RELEASE FROM ERODIBLE MATRICES [J].
BONFERONI, MC ;
CARAMELLA, C ;
SANGALLI, ME ;
CONTE, U ;
HERNANDEZ, RM ;
PEDRAZ, JL .
JOURNAL OF CONTROLLED RELEASE, 1992, 18 (03) :205-212
[5]   GRAFT-COPOLYMERIZATION OF DIFFERENT MIXTURES OF ACRYLIC-MONOMERS ON AMYLOPECTIN - SWELLING BEHAVIOR [J].
CASTELLANO, I ;
PASCUAL, B ;
VAZQUEZ, B ;
GONI, I ;
GURRUCHAGA, M .
JOURNAL OF APPLIED POLYMER SCIENCE, 1994, 54 (05) :577-584
[6]   Contribution to the study of new graft copolymer matrices for drug delivery systems. Technological study [J].
Castellano, I ;
Goni, I ;
Gurruchaga, M ;
Velasco, MV ;
Munoz, A ;
JimenezCastellanos, MR .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 146 (01) :71-79
[7]   The influence of drying method on the physical properties of some graft copolymers for drug delivery systems [J].
Castellano, I ;
Gurruchaga, M ;
Goni, I .
CARBOHYDRATE POLYMERS, 1997, 34 (1-2) :83-89
[8]   Synthetic PMMA-grafted polysaccharides as hydrophilic matrix for controlled-release forms [J].
Castellano, I ;
Goñi, I ;
Ferrero, M ;
Muñoz, A ;
Jiménez-Castellanos, R ;
Gurruchaga, M .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1999, 25 (12) :1249-1257
[9]  
DOELKER E, 1987, HYDROGELS MED PHARM, V2, P115
[10]  
Dumitriu S, 1996, POLYSACCHARIDES MED, P705