# US 5,700,459 A · Pharmacological composition containing polyelectrolyte complexes in microparticulate form and at least one active agent > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,700,459 A - Document ID: US5700459A - Status: Granted - Kind: A - Application number: 08/341,164 - Filed: 1994-11-16 - Granted: 1997-12-23 - Earliest claimed: 1990-04-25 - Assignees: Hoechst Aktiengesellschaft - Inventors: Volker Krone; Michael Magerstadt; Axel Walch; Albrecht Groner; Dieter Hoffmann - Web page: https://patentgrep.com/patent/US5700459A ## CPC - G09B 23/286: {for scanning or photography techniques, e.g. X-rays, ultrasonics} - A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers} - A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)} - A61K 49/223: {Microbubbles, hollow microspheres, free gas bubbles, gas microspheres} - A61P 35/00: Antineoplastic agents - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - G09B: EDUCATIONAL OR DEMONSTRATION APPLIANCES; APPLIANCES FOR TEACHING, OR COMMUNICATING WITH, THE BLIND, DEAF OR MUTE; MODELS; PLANETARIA; GLOBES; MAPS; DIAGRAMS (devices for psychotechnics or for testing reaction times A61B5/16; games, sports, amusements A63; projectors, projector screens G03B) - 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 invention relates to a pharmacological composition comprising a polyelectrolyte complex, in particular a polyacid with an average particle size of less than 15 .mu.m and an active agent, among which are active peptides, proteins, enzymes, enzyme inhibitors, antigens, cytostatics, antiinflamatory agents, antibiotics and vaccines. The said composition ensures that the active agent is converted in a non-deleterious manner into a form which can be administered. In addition, the biodistribution, bioavailability and absorption of the pharmaceutical are beneficially affected. ## Claims ### Claim 1 A pharmaceutical composition consisting essentially of: a) a polyelectrolyte complex in microparticulate form, wherein said polyelectrolyte complex has an average particle size of less than 15 .mu.m and is comprised of a polybase and a polyacid, wherein at least one of said polyacid and said polybase is a polymer, and wherein when said polyacid is a polymer, the polymer is selected from the group consisting of xylan polysulfates, dextran sulfates, poly(amino acids), polysaccharide polysulfates, inulin sulfates, hydroxyethylstarch sulfates, polysaccharide polysulfonates, polysaccharide polyphosphates, polyphosphates, and derivatives of said polymer, and wherein when said polybase is a polymer, the polymer is selected from the group consisting of poly-L-lysine, poly-.alpha.,.beta.-(2-dimethylaminoethyl)-D,L-aspartamide, chitosan, lysine octadecyl ester, aminated dextrans, aminated cyclodextrins, aminated cellulose ethers, aminated pectins, and derivatives of said polymer; and b) a pharmaceutically effective amount of at least one active agent selected from the group consisting of an enzyme inhibitor, an antigen, a cytostatic, an antiinflammatory agent, an antibiotic, a vaccine and an ultrasonic contrast agent. ### Claim 2 (depends on 1) A pharmaceutical composition as claimed in claim 1, wherein at least one of said polyacid and said polybase contains said active agent. ### Claim 3 (depends on 1) A pharmaceutical composition as claimed in claim 1, wherein the microparticles further contain one or more auxiliaries. ### Claim 4 (depends on 1) A pharmaceutical composition as in claim 1, wherein the active agent is an ultrasonic contrast agent. ### Claim 5 (depends on 1) A pharmaceutical composition as claimed in claim 1, wherein the polyelectrolyte complex has an average particle size of .ltoreq.5 .mu.m. ### Claim 6 (depends on 1) The method of treating a patient in need of a vaccine which comprises administering a pharmaceutical composition as claimed in claim 1 as a vaccine. ### Claim 7 (depends on 1) The method of diagnosing a patient using a diagnostic aid comprising a pharmaceutical composition as claimed in claim 1. ### Claim 8 (depends on 1) The method of treating a patient comprising administrations of a pharmaceutical composition as claimed in claim 1 as a therapeutic agent. ### Claim 9 (depends on 1) The method of treating a patient in need of diagnosis with an ultrasonic diagnostic aid comprising administration of a pharmaceutical composition as claimed in claim 1. ### Claim 10 (depends on 6) The method of treating a patient comprising parenteral administration of a pharmaceutical composition as claimed in claim 6. ### Claim 11 (depends on 1) A pharmaceutical composition as claimed in claim 1, wherein the active agent is an active peptide. ### Claim 12 (depends on 1) A pharmaceutical composition as claimed in claim 1, wherein the active agent is a protein. ### Claim 13 (depends on 1) A pharmaceutical composition as claimed in claim 1, wherein the active agent is an enzyme.