# US 2013/0156934 A1 · Microcapsules by coacervation containing a pharmaceutical incorporated in the coating polymer > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2013/0156934 A1 - Document ID: US20130156934A1 - Status: Published application - Kind: A1 - Application number: 13/681,727 - Filed: 2012-11-20 - Published: 2013-06-20 - Earliest claimed: 2003-05-30 - Assignees: Aptalis Pharma Limited - Inventors: Roberto Golzi; Luigi Boltri; Christian Stollberg - Web page: https://patentgrep.com/patent/US20130156934A1 ## CPC - A61J 3/005: {Coating of tablets or the like (coating of sweetmeats or confectionery A23G3/20; coating of granules in general B01J2/006)} - A61K 9/1676: {having a drug-free core with discrete complete coating layer containing drug (adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921)} - B01J 13/06: by phase separation - B01J 13/08: Simple coacervation, i.e. addition of highly hydrophilic material {(combined with spraying B01J13/043; combined with mechanical division B01J13/04)} - B01J 13/206: {Hardening; drying} - A61K 9/5078: {with drug-free core} - A61J: CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE - 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) - B01J: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS ## Abstract Microcapsules containing an active ingredient, constituted by a core coated with a polymer membrane, characterized in that the active ingredient is incorporated in the polymer coating layer, and in that said layer is applied using microencapsulation techniques (coacervation by means of phase separation). The microcapsules; thus produced have excellent properties of taste masking and prolonged release of the active ingredients. ## Claims ### Claim 1 A method of preparing microcapsules containing at least one active ingredient comprising: providing cores having a dimension ranging from 50 to 1200 μm; and applying a polymeric membrane comprising at least one active ingredient and, optionally, at least one membrane additive to said core; wherein said applying is by coacervation by phase separation of a suspension of said active ingredient and, optionally, of said membrane additive in a solution of a water-soluble or a water-insoluble coating polymer. ### Claim 2 (depends on 1) The method as claimed in claim 1 comprising the following steps: (a) forming a solution of the membrane polymer in an aqueous or in an organic solvent; (b) suspending the cores, the particles of active ingredient and, optionally, at least one membrane additive in the solution obtained in step (a); (c) causing coacervation of the membrane polymer in the suspension obtained in (b) by phase separation, thereby forming the polymeric membrane on the core; (d) optionally, treating the microcapsules formed in step (c) to a hardening of the membrane; and (e) recovering the microcapsules thereby obtained in step (c) or step (d). ### Claim 3 (depends on 2) The method as claimed in claim 2 wherein step a) and b) are carried out as a single step. ### Claim 4 (depends on 2) The method as claimed in claim 2, wherein the membrane polymer is a water insoluble polymer, the solution of said polymer is in an organic solvent and said active ingredient is water-soluble. ### Claim 5 (depends on 4) The method as claimed in claim 4 wherein said polymer is ethylcellulose. ### Claim 6 (depends on 4) The method as claimed in claim 4 wherein the solvent used in step a) is cyclohexane. ### Claim 7 (depends on 4) The method as claimed in claim 4 wherein the membrane additive is added in step (b), and is selected from the group consisting of lactose, mannitol, polyvinylpyrrolidone, hydroxypropylmethylcellulose, methylcellulose, hydroxypropylcellulose, swelling agents, sodium carboxymethylamide, croscarmellose, crospovidone, pregelatinized starch, pH modifiers, and combinations thereof. ### Claim 8 (depends on 4) The method as claimed in claim 4, wherein in step (c) phase separation takes place by variation in temperature. ### Claim 9 (depends on 2) The method as claimed in claim 2, wherein the membrane polymer is a water soluble polymer, the solution of said polymer is in an aqueous solvent, and said active ingredient is water-insoluble. ### Claim 10 (depends on 9) The method as claimed in claim 9, wherein said polymer is selected from the group consisting of gelatine, cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate and derivates thereof. ### Claim 11 (depends on 9) The method as claimed in claim 9, wherein the solvent used in step (a) is water at a pH between 1 and 9. ### Claim 12 (depends on 11) The method as claimed in claim 11, wherein the pH is between 4 and 7. ### Claim 13 (depends on 9) The method as claimed in claim 9, wherein the membrane additive is added in step (b), and is selected from the group consisting of dibasic calcium phosphate, calcium sulfate, barium sulfate, calcium carbonate, magnesium carbonate, silicates, and combinations thereof. ### Claim 14 (depends on 9) The method as claimed in claim 9, wherein in step (c) phase separation takes place by pH variation, variation in temperature or insolubilisation of the polymer by adding phase-separation inducing agents. ### Claim at position 15 15-30. (canceled)