Tablets containing cross-linked high amylose starch having functional groups as a matrix for the slow release of pharmaceutical agents

摘要

A solid controlled release oral pharmaceutical dosage unit in the form of a tablet comprises a) a blend of 0.01-80% by weight of the tablet of a dry powder of a pharmaceutical product, and b) 20-99.99% by weight of the tablet of a dry powder of high amylose starch wherein the dosage unit is resistant to degradation by amylase. The high amylose starch comprises a mixture of from 10-60% by weight of amylopectin and from 40-90% amylose. The high amylose starch has been covalently cross-linked with a covalent cross-linking agent wherein the cross-linking has been carried out with from 0.1 g to 30 grams of cross- linking agent per 100 g of the high amylose starch A solid controlled release pharmaceutical dosage unit in the form of a tablet comprises: a) a pharmaceutical product; b) high amylose starch, wherein the high amylose starch comprises 10-60% by weight amylopectin and 40-90% by weight amylose; and c) a polysaccharide or a polyol. The high amylose starch and the polysaccharide or the polyol are covalently co-cross-linked with a covalent cross- linking agent and the cross-linking is carried out with from 0.1 g to 30 g of cross-linking agent per 100 g of high amylose starch. The cross-linked high amylose starch having functional groups is prepared by: a) reacting high amylose starch with a cross-linking agent cross-linked a concentration of 0.1 g to 40 g of cross- linking agent per 100 g of high amylose starch to afford cross-linked amylose; and b) reacting the cross-linked high amylose starch with a functional group-attaching reagent at a concentration of 75 g to 250 g of functional group-attaching reagent per 100 g of cross-linked amylose to afford the cross-linked amylose having functional groups. The functional group attaching reagent is monochloroacetic acid and chloroethylamine hydrochloride.