# US 8,569,480 B2 · Hydroxyethylstarch > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,569,480 B2 - Document ID: US8569480B2 - Status: Granted - Kind: B2 - Application number: 12/850,394 - Filed: 2010-08-04 - Published: 2010-11-25 - Granted: 2013-10-29 - Earliest claimed: 2004-03-01 - Assignees: B. Braun Melsungen AG - Applicants: Michael Boll; Andreas Fisch; Donat R. Spahn - Inventors: Michael Boll; Andreas Fisch; Donat R. Spahn - Web page: https://patentgrep.com/patent/US8569480B2 ## CPC - A61K 31/718: Starch or degraded starch, e.g. amylose, amylopectin - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 9/0026: {Blood substitute; Oxygen transporting formulations; Plasma extender} - A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin - A61P 7/06: Antianaemics - A61P 7/08: Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock (artificial tears A61P27/04) - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 41/00: Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution - C08B 31/12: having alkyl or cycloalkyl radicals substituted by heteroatoms, {e.g. hydroxyalkyl or carboxyalkyl starch} - C08L 3/08: Ethers - 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 - C08B: POLYSACCHARIDES; DERIVATIVES THEREOF (polysaccharides containing less than six saccharide radicals attached to each other by glycosidic linkages C07H; fermentation or enzyme-using processes C12P19/00; sugar industry C13; production of cellulose D21) - C08L: COMPOSITIONS OF MACROMOLECULAR COMPOUNDS (compositions based on polymerisable monomers C08F, C08G; artificial filaments or fibres D01F; textile treating compositions D06) ## Abstract Described are a hydroxyethylstarch, a process for the preparation thereof, a pharmaceutical formulation containing such a hydroxyethylstarch, and the use of the pharmaceutical formulation for the preparation of a volume replacement, a plasma replacement or a plasma volume expander, as well as the use of the pharmaceutical formulation for maintaining normovolemia and/or for improving the macro- and microcirculation and/or for improving the nutritive oxygen supply and/or for stabilizing hemodynamics and/or for improving the volume efficiency and/or for reducing the plasma viscosity and/or for increasing anemia tolerance and/or for hemodilution, especially for therapeutic hemodilution in disturbed blood supply and arterial, especially peripheral arterial, occlusive diseases. ## Claims ### Claim 1 A hydroxyethylstarch having an average molecular weight, Mw, of from above 600,000 to 1,500,000, characterized by having a molar substitution MS of from 0.25 to 0.5 and a C2/C6 ratio of from 2 to below 8, wherein the hydroxyethylstarch is at least sterile filtered or heat sterilized for use as a volume replacement or plasma expander. ### Claim 2 (depends on 1) The hydroxyethylstarch according to claim 1, wherein the molar substitution MS is from 0.35 to 0.5. ### Claim 3 (depends on 1) The hydroxyethylstarch according to claim 1, wherein the C2/C6 ratio is from 2 to 7. ### Claim 4 (depends on 1) The hydroxyethylstarch according to claim 1, wherein the hydroxyethylstarch is obtainable from a waxy maize starch. ### Claim 5 (depends on 2) The hydroxyethylstarch according to claim 2, wherein the C2/C6 ratio is from 2 to 7. ### Claim 6 A process for preparing a hydroxyethylstarch for use as a volume replacement or plasma expander comprising the steps: (i) reacting water-suspended starch with ethylene oxide; and (ii) partially hydrolyzing a starch derivative with acid until a desired range of average molecular weight of the hydroxyethylstarch is reached; and wherein the hydroxyethylstarch comprises an average molecular weight, Mw, of from above 600,000 to 1,500,000, characterized by having a molar substitution MS of from 0.25 to 0.5 and a C2/C6 ratio of from 2 to below 8. ### Claim 7 (depends on 6) The process according to claim 6, wherein an alkalizing agent is added to said water-suspended starch. ### Claim 8 (depends on 6) The process according to claim 6, further comprising the step of sterilization. ### Claim 9 (depends on 6) The process according to claim 6, wherein the suspended starch is corn starch. ### Claim 10 (depends on 6) The process according to claim 6, further comprising the step of ultrafiltration. ### Claim 11 A method of treating a patient in need of maintaining normovolemia, improving macro- and microcirculation, improving nutritive oxygen supply, stabilizing hemodynamics, improving volume efficiency, reducing plasma viscosity, increasing anemia tolerance, requiring hemodilution, or a combination thereof, the method comprising: providing a pharmaceutical formulation comprising a hydroxyethylstarch, the hydroxyethylstarch having an average molecular weight, Mw, of at least 500,000 characterized by having a molar substitution MS of from 0.25 to 0.5 and a C2/C6 ratio of from 2 to below 8, wherein the hydroxyethyl starch is at least one of sterile filtered and heat sterilized; and administering the pharmaceutical formulation to the patient. ### Claim 12 (depends on 11) The method of claim 11, wherein the hemodilution involves therapeutic hemodilution in disturbed blood supply and arterial diseases. ### Claim 13 (depends on 11) The method of claim 11, wherein the pharmaceutical formulation is in the form of at least one of an aqueous solution and a colloidal aqueous solution. ### Claim 14 (depends on 11) The method of claim 11, wherein the hydroxyethylstarch is in a concentration of up to 20%. ### Claim 15 (depends on 11) The method of claim 11, wherein the pharmaceutical formulation further includes plasma-adapted electrolytes. ### Claim 16 (depends on 11) The method of claim 11, wherein the pharmaceutical formulation is in the form of at least one of a buffered solution and a solution with metabolizable anions. ### Claim 17 (depends on 11) The method of claim 11, wherein the pharmaceutical formulation is in the form of a hypertonic solution.