# US 8,541,393 B2 · Antimicrobial locking solutions comprising taurinamide derivatives and biologically acceptable salts and acids, with the addition of small concentrations of heparin > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,541,393 B2 - Document ID: US8541393B2 - Status: Granted - Kind: B2 - Application number: 13/199,605 - Filed: 2011-09-02 - Published: 2012-08-16 - Granted: 2013-09-24 - Earliest claimed: 2004-11-02 - Assignees: ND Partners, LLC - Applicants: Frank R. Prosl - Inventors: Frank R. Prosl - Web page: https://patentgrep.com/patent/US8541393B2 ## CPC - A61L 29/16: Biologically active materials, e.g. therapeutic substances {(A61L29/048 takes precedence)} - A01N 25/02: containing liquids as carriers, diluents or solvents - A01N 43/88: six-membered rings with three ring hetero atoms - A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63) - A61K 31/185: Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327) - A61K 31/727: Heparin; Heparan - A61L 29/00: Materials for catheters, {medical tubing, cannulae, or endoscopes} or for coating catheters (shape or structure of catheters A61M25/00) - A61L 29/043: {Polysaccharides} - A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors - A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics - A61P 31/04: Antibacterial agents - A61L 2300/204: with nitrogen-containing functional groups, e.g. aminoxides, nitriles, guanidines - A61L 2300/406: Antibiotics - A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K) - A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention relates to inhibiting or preventing infection and protecting against patency complications after a blood catheter has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising (A) at least one taurinamide derivative, (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof; and (C) heparin at a low concentration. ## Claims ### Claim 1 A locking solution composition for treating and reducing infection and flow reduction in blood catheters comprising a solution of: a. at least one taurinamide derivative; b. a biologically acceptable acid and a biologically acceptable salt of said acid in a combination that brings the pH of the combination into a range that enhances antimicrobial activity of the taurinamide derivative; and c. heparin in a concentration of 50 to 2500 units per ml, wherein the heparin concentration is sufficient to prevent reactions of the taurinamide derivative with stagnant blood but low enough that expulsion and/or spillage of the solution into a patient's bloodstream carries a low risk of patient hemorrhage. ### Claim 2 (depends on 1) The composition of claim 1 wherein the biologically acceptable acid is chosen from the group consisting of citric acid and lactic acid and the biologically acceptable salt is chosen from the group consisting of citrate and lactate. ### Claim 3 (depends on 1) The composition of claim 1 wherein the taurinamide derivative is taurolidine, the biologically acceptable acid is citric acid, the biologically acceptable salt is citrate, and the pH range is 5.2 to 6.5. ### Claim 4 (depends on 1) The composition of claim 1 wherein the concentration of heparin is in the range of 50 to 1750 units per ml. ### Claim 5 (depends on 1) The composition of claim 1 wherein the concentration of heparin is in the range of 50 to 500 units per ml. ### Claim 6 (depends on 1) The composition of claim 1 wherein the concentration of heparin is in the range 50 to 150 units per ml. ### Claim 7 A method of enhancing the antimicrobial activity and resistance to flow reduction produced by a catheter locking solution comprising taurolidine in combination with citrate and citric acid by maintaining the pH in the range of 5.2 to 6.5 and of protecting a catheter against taurolidine reaction with blood therein by adding heparin in a concentration of 50 to 2500 units per ml, wherein the heparin concentration is sufficient to prevent reactions of the taurolidine with stagnant blood but low enough that expulsion and/or spillage of the solution into a patient's bloodstream carries a low risk of patient hemorrhage. ### Claim 8 (depends on 7) The method of claim 7 in which the concentration of heparin is in the range of 50 units per ml to 1750 units per ml. ### Claim 9 (depends on 7) The method of claim 7 in which the concentration of heparin is in the range of 50 units per ml to 500 units per ml. ### Claim 10 (depends on 7) The method of claim 7 in which the concentration of heparin is in the range of 50 units per ml to 150 units per ml. ### Claim 11 A composition for treating and reducing infection and patency loss in hemodialysis catheters comprising a locking solution comprising: a. at least one taurinamide derivative; and b. heparin in a concentration of 50 to 2500 units per ml, wherein the heparin concentration is sufficient to prevent reactions of the taurinamide derivative with stagnant blood but low enough that expulsion and/or spillage of the solution into a patient's bloodstream carries a low risk of patient hemorrhage. ### Claim 12 (depends on 11) The composition of claim 11 wherein the taurinamide derivative is taurolidine. ### Claim 13 (depends on 11) The composition of claim 11 wherein the concentration of heparin is in the range of 50 to 1750 units per ml. ### Claim 14 (depends on 11) The composition of claim 11 wherein the concentration of heparin is in the range of 50 to 500 units per ml. ### Claim 15 (depends on 11) The composition of claim 11 wherein the concentration of heparin is in the range 50 to 150 units per ml. ### Claim 16 A locking solution composition for treating and reducing infection and flow reduction in catheters comprising a solution of: a. at least one taurinamide derivative; b. a biologically acceptable acid in sufficient concentration to bring the pH of the composition into a range that enhances antimicrobial activity of the taurinamide derivative; and c. heparin in a concentration of 50 to 2500 units per ml, wherein the heparin concentration is sufficient to prevent reactions of the taurinamide derivative but low enough that expulsion and/or spillage of the solution into a patient's bloodstream carries a low risk of patient hemorrhage. ### Claim 17 (depends on 16) The composition of claim 16 wherein the taurinamide derivative is taurolidine. ### Claim 18 (depends on 16) The composition of claim 16 wherein the concentration of heparin is in the range of 50 to 1750 units per ml. ### Claim 19 (depends on 16) The composition of claim 16 wherein the concentration of heparin is in the range 50 to 500 units per ml. ### Claim 20 (depends on 16) The composition of claim 16 wherein the concentration of heparin is in the range 50 to 150 units per ml.