CONTROLLED RELEASE FROM COPOLYMERS OF ACRYLIC OR METHACRYLIC ACID/L-DOPA, ACRYLIC OR METHACRYLIC ACID/L-.ALPHA.-METHYL DOPA, ACRYLIC OR METHACRYLIC ACID/CARBIDOPA AND THEIR COMBINATIONS

摘要

The invention relates to site directed drug delivery systems providing a controlled release of L-dopa, carbidopa, L-.alpha.-methyldopa and/or their combinations which eliminates or at least reduces the deleterious side effec ts of these drugs. Biologically active copolymers having directional characteristics to the digestive mucous tissue comprise L-dopa, carbidopa or L- .alpha.-methyldopa chemically combined with biologically acceptable poly(acrylic acid) or poly(methacrylic acid). The copolymers are obtained by a process comprising the steps of: (a) reacting L-dopa, carbidopa or L-.alpha. - methyldopa with a chlorination agent; (b) bringing into reaction the product of step (a) and poly(acrylic acid) or poly(methacrylic acid) in the presence of a suitable catalyst; (c) washing the copolymer obtained in step (b) with a suitable organic solvent and drying it until constant weight. Controlled release antihypertensive pharmaceuticals comprise at least one biologically active copolymer selected from the group consisting of poly(acrylic acid/L- .alpha.-methyldopa), poly(methacrylic acid/L-$G(a)-methyldopa), poly(acrylic acid/carbidopa), poly(methacrylic acid/carbidopa) or combinations thereof an d a pharmaceutically acceptable vehicle. Controlled release pharmaceuticals comprising at least one biologically active copolymer selected from the grou p consisting of poly(acrylic acid/L-dopa), poly(methacrylic acid/L-dopa), poly(acrylic acid/carbidopa), poly(methacrylic acid/carbidopa) or combinatio ns thereof and a pharmaceutically acceptable vehicle are used in the therapeuti c treatment of Parkinson syndrome.