# US 5,102,666 A · Calcium polycarbophil controlled release composition and method > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,102,666 A - Document ID: US5102666A - Status: Granted - Kind: A - Application number: 07/580,854 - Filed: 1990-09-11 - Granted: 1992-04-07 - Earliest claimed: 1990-09-11 - Assignees: Oramed Ltd. - Inventors: Ramesh N. Acharya - Web page: https://patentgrep.com/patent/US5102666A ## CPC - A61K 8/733: {Alginic acid; Salts thereof} - A61K 8/8147: {Homopolymers or copolymers of acids; Metal or ammonium salts thereof, e.g. crotonic acid, (meth)acrylic acid; Compositions of derivatives of such polymers} - A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin} - A61Q 11/00: Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses - A61Q 19/00: Preparations for care of the skin - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS ## Abstract Controlled release compositions comprising calcium polycarbophil and an active agent selected from the group consisting of medicinal agents, breath fresheners, and flavors, and a method of controlled release of such an active agent. ## Claims ### Claim 1 A polymeric controlled release composition comprising a reaction complex formed by the interaction of (1) a calcium polycarbophil component which is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer, said polymer containing (1) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of unpolymerized repeating unit and cross-linking agent, respectively, with (2) water, in the presence of an active agent selected from the group consisting of medicinal agents, breath fresheners, and flavors, wherein the amount of calcium polycarbophil present is from about 0.1 to about 99 percent, the amount of active agent present is from about 0.0001 to about 65 percent, by weight, based upon of the composition, and the amount of water present is from about 5 to about 200 percent, based upon the weight of calcium polycarbophil, said interaction being at a pH from about 3 to about 10, and the calcium polycarbophil being originally present, prior to said interaction, in the form of the calcium salt, having a calcium content from about 5 to about 25 percent, based on the weight of the polycarbophil. ### Claim 2 (depends on 1) The composition according to claim 1 wherein said active agent is a medicament. ### Claim 3 (depends on 2) The composition according to claim 2 wherein said polymeric composition also comprises a hydrophilic colloid. ### Claim 4 (depends on 3) The composition according to claim 3 wherein the said polymeric composition also comprises simple or complex carbohydrates or polyols. ### Claim 5 (depends on 3) The composition according to claim 3 wherein said polymeric composition also comprises one or more cosolvents selected from the group consisting of glycerol, propylene glycol and polyethylene glycol. ### Claim 6 (depends on 3) The composition according to claim 3 which is formed by combining a two component system comprising as one component a polymer phase containing calcium polycarbophil and as the second component a liquid phase containing water or optionally other solvents and the complex is formed at the time of use. ### Claim 7 (depends on 3) The composition according to claim 3 which is formed, in situ by combining a polymer phase dispersed in a nonpolar solvent with water from body fluid, when administered parenterally. ### Claim 8 (depends on 3) The composition according to claim 3 wherein at least about 90 percent of said polymer repeating units contain at least one carboxyl functionality. ### Claim 9 (depends on 3) The composition according to claim 3 wherein at least about 95 percent of said polymer repeating units contain at least one carboxyl functionality. ### Claim 10 (depends on 9) The method according to claim 9 wherein said composition comprises an intimate mixture of said reaction complex and said active agent. ### Claim 11 (depends on 3) The composition according to claim 3 wherein said polymer contains about 0.1 to about 1 percent by weight of polymerized cross-linking agent. ### Claim 12 (depends on 3) The composition according to claim 3 wherein said carboxyl functionality is provided by polymerized acrylic acid. ### Claim 13 (depends on 3) The composition according to claim 3 wherein the ratio by weight of said reaction complex to said active agent is from about 200,000:1 to about 1:100. ### Claim 14 A method of controlled release treatment comprising the steps of: (a) providing a polymeric complex and a therapeutically effective amount of an active agent contained within said complex, said polymeric complex comprising a reaction complex formed by the reaction of (1) a water-swellable, but water-insoluble, fibrous cross-linked carboxy-functional polymer, said polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality and (b) about 0.05 to about 1.5 percent cross linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of the unpolymerized repeating unit and cross-linking agent, respectively, or a salt thereof, with (2) water, said interaction being performed in the presence of an active agent, selected from the group consisting of medicinal agents, wherein the amount of calcium polycarbophil present is from about 0.1 to about 99 percent, the amount of active agent present is from about 0.0001 to about 65 percent, by weight, based upon the weight of the composition, and the amount of water present is from about 5 to about 200 percent, based upon the weight of calcium polycarbophil, said interaction being at a pH from about 3 to about 10, and the calcium polycarbophil being originally present, prior to said interaction, in the form of the calcium salt, having a calcium content from about 5 to about 25 percent, based on the weight of the polycarbophil; and (b) contacting an area of skin or mucous membrane to be treated with said composition for a period of time that is sufficient to allow a therapeutically effective amount of said active agent to be released from the complex.