Cross-linked high amylose starch resistant to amylase as a matrix for the slow release of biologically active compounds
OwnerVincent Lenaerts, Francois Chouinard +2inventors
InventorsVincent Lenaerts, Francois Chouinard, Mircea Alexandru Mateescu, Pompilia Ispas-Szabo
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Abstract
The present invention is concerned with a solid slow release oral pharmaceutical dosage unit resistant to amylase which comprises a solid dosage unit made up of an admixture of a therapeutic dosage of an orally effective pharmaceutical product, an optional polysaccharide or polyol, and cross-linked high amylose starch, wherein the cross-linking of the high amylose starch has been carried out with a covalent or non-covalent cross-linking agent with from about 0.1 g to about 30 g of cross-linking agent per 100 g of high amylose starch.
Claims34
A solid controlled release oral pharmaceutical dosage unit in the form of a tablet comprising a blend of 0.01-80% by weight of the tablet of a dry powder of a pharmaceutical product, and 20-99.99% by weight of the tablet of a dry powder of high amylose starch, wherein said high amylose starch comprises a mixture of from about 10-60% by weight of amylopectin and from about 40-90% amylose, wherein said high amylose starch has been covalently cross-linked with a covalent cross-linking agent wherein the cross-linking has been carried out with from about 0.1 g to about 30 grams of cross-linking agent per 100 g of said high amylose starch, wherein said dosage unit is resistant to degradation by amylase.
A method for imparting sustained release to a pharmaceutical product, comprising the steps of:
- (a) providing the pharmaceutical product in dry powder form;
- and
- (b) blending the pharmaceutical product with a powder comprising a high amylose starch, wherein said high amylose starch comprises a mixture of from about 10-60% amylopectin and 40-90% amylose, wherein said high amylose starch has been covalently cross-linked with a cross-linking agent wherein the cross-linking has been carried out with from about 0.1 g to about 30 g of cross-linking agent per 100 g of said high amylose starch;
- and
- (c) compressing the blend to form a tablet.
A solid controlled release pharmaceutical dosage unit in the form of a tablet comprising:
- (a) a pharmaceutical product;
- (b) high amylose starch, wherein said high amylose starch comprises 10-60% by weight amylopectin and 40-90% by weight amylose;
- and
- (c) a polysaccharide or a polyol;
- wherein said high amylose starch and said polysaccharide or said polyol have been covalently co-cross-linked with a covalent cross-linking agent wherein the cross-linking has been carried out with from about 0.1 g to about 30 g of cross-linking agent per 100 g of high amylose starch.
A method for imparting sustained release to a pharmaceutical product, comprising the steps of:
- (a) providing the pharmaceutical product in dry powder form;
- (b) blending the pharmaceutical product with a powder comprising a high amylose starch, wherein said high amylose starch comprises 10-60% by weight amylopectin and 40-90% by weight amylose, wherein said high amylose starch has been covalently co-cross-linked with a polysaccharide or polyol and a cross-linking agent wherein the cross-linking has been carried out with from about 0.1 g to about 30 g of cross-linking agent per 100 g of said high amylose starch;
- and
- (c) compressing the blend to form a tablet.
A method for imparting sustained release to a pharmaceutical product, comprising the steps of:
- (a) providing the pharmaceutical product in dry powder form;
- (b) blending the pharmaceutical product with a powder comprising a high amylose starch, wherein said high amylose starch comprises 10-60% by weight amylopectin and 40-90% by weight amylose, wherein said high amylose starch has been covalently cross-linked using a covalent cross-linking agent wherein the cross-linking has been carried out with from about 0.1 g to about 30 g of cross-linking agent per 100 g of said high amylose starch;
- (c) blending the powder of step (b) with a polysaccharide or polyol;
- and
- (d) compressing the blend to form a tablet.
Dependencies are inferred from the claim text.