# US 2014/0193509 A1 · Carrier pellets, method for production thereof and use thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0193509 A1 - Document ID: US20140193509A1 - Status: Published application - Kind: A1 - Application number: 14/209,056 - Filed: 2014-03-13 - Published: 2014-07-10 - Earliest claimed: 2008-01-17 - Assignees: ADD Advanced Drug Delivery Technologies Ltd.; Ipc Process-Center GmbH & Co. KG - Applicants: ADD Advanced Drug Delivery Technologies Ltd.; Ipc Process-Center GmbH & Co. KG - Inventors: Antje Weigt; Wolfgang Kempe; Burkhard Schlütermann - Web page: https://patentgrep.com/patent/US20140193509A1 ## CPC - A61K 9/1617: {Organic compounds, e.g. phospholipids, fats} - A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)} - A61K 9/1682: {Processes} - A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient} - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - 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) ## Abstract The invention relates to a method for the production of carrier pellets for pharmaceutical active substances. Likewise, the invention relates to such carrier pellets and also to pharmaceutical formulations containing these. The carrier pellets according to the invention are used for transporting and releasing pharmaceutical active substances, in particular in the human body. ## Claims ### Claim 1 A method for the production of carrier pellets for a pharmaceutically active substance, the method comprising: a) producing a liquid formulation by dissolving, dispersing, or a combination of dissolving and dispersing at least one physiologically well-tolerated pH regulator in at least one solvent or emulsifier; b) introducing the liquid formulation into a fluidized-bed or spouted-bed unit using at least one nozzle; c) forming essentially spherical carrier pellets by spray granulation in the unit wherein the solvent is evaporated by a drying gas flow; and d) discharging the carrier pellets from the unit. ### Claim 2 (depends on 1) The method according to claim 1; wherein the at least one pH regulator has a regulating effect in physiological surroundings such that the pH value is lowered or increased and the bioavailability of the pharmaceutically active substance is made possible or increased. ### Claim 3 (depends on 1) The method according to claim 1; wherein the at least one pH regulator comprises at least one organic acid selected from the group consisting of ascorbic acid, a C1-C18 monocarboxylic acid, a C1-C18 dicarboxylic acid, a C1-C18 tricarboxylic acid and mixtures thereof. ### Claim 4 (depends on 3) The method according to claim 3; wherein the at least one organic acid is selected from the group consisting of citric acid, succinic acid, malic acid, fumaric acid, tartaric acid, sorbic acid, adipinic acid, salts thereof, and mixtures thereof. ### Claim 5 (depends on 1) The method according to claim 1; wherein the at least one pH regulator comprises an acidic or basic salt. ### Claim 6 (depends on 1) The method according to claim 1; wherein the pH regulator comprises a buffer system comprising an organic acid and salt of the organic acid or an organic base and salt of the organic base, wherein the buffer system stabilizes the pH. ### Claim 7 (depends on 6) The method according to claim 6; wherein the buffer system comprises at least one combination selected from the group consisting of: citric acid and a citrate; and tartaric acid and a tartrate. ### Claim 8 (depends on 1) The method according to claim 1; wherein the pH regulator acts in physiological surroundings as pH-increasing, pH-lowering, or pH-stabilising. ### Claim 9 (depends on 1) The method according to claim 1; wherein the pH regulator comprises at least one organic base selected from the group consisting of a purine base, a pyrimidine base, and a mixture thereof. ### Claim 10 (depends on 9) The method according to claim 9; wherein the purine base is selected from the group consisting of adenine, guanine, hypoxanthine, xanthine, and mixtures thereof. ### Claim 11 (depends on 9) The method according to claim 9; wherein the pyrimidine base is selected from the group consisting of cytosine, uracil, thymine, and mixtures thereof. ### Claim 12 (depends on 1) The method according to claim 1; wherein the pH regulator comprises at least one basic inorganic salt selected from the group consisting of NaHCO3, K2CO3, Na2CO3, KHCO3, Ca(OH)2, CaO, phosphates, and mixtures thereof. ### Claim 13 (depends on 1) The method according to claim 1; wherein the liquid formulation further comprises at least one physiologically well-tolerated binder. ### Claim 14 (depends on 13) The method according to claim 13; wherein the at least one binder is selected from the group consisting of methyl celluloses, hydroxymethyl celluloses, hydroxypropylmethyl celluloses, alginates, pectins, polyvinylpyrrolidones, xanthanes, hydrocolloids, and mixtures thereof. ### Claim 15 (depends on 1) The method according to claim 1; wherein the at least one solvent or emulsifier is water or an organic solvent selected from the group consisting of ethyl alcohol, isopropanol, n-propanol, and mixtures thereof. ### Claim 16 (depends on 13) The method according to claim 13; wherein the quantity ratio of pH regulator to binder in the liquid formulation is in the range of 50:50 to 99:1. ### Claim 17 (depends on 13) The method according to claim 13; wherein the liquid formulation contains: 30 to 80% by weight of the at least one pH regulator; 0.5 to 5% by weight of the at least one binder; and 15 to 69.5% by weight of the at least one solvent. ### Claim 18 (depends on 1) The method according to claim 1; wherein the temperature in the unit is in the range of 5 to 100° C. ### Claim 19 (depends on 1) The method according to claim 1; wherein the drying gas flow has, at the entrance into the unit, a temperature in the range of 5 to 120°. ### Claim 20 (depends on 1) The method according to claim 1; wherein the drying gas is air, nitrogen, or inert gas. ### Claim 21 (depends on 1) The method according to claim 1; wherein the spray granulation is effected in a fluidized-bed unit into which the drying gas is supplied via a sieve plate and the liquid formulation is introduced by the at least one nozzle disposed above the sieve plate. ### Claim 22 (depends on 1) The method according to claim 1; wherein the spray granulation is effected in a spouted-bed unit into which the drying gas is supplied via longitudinal gaps disposed in the lower half of the unit and the liquid formulation is introduced by the at least one nozzle disposed between the longitudinal gaps. ### Claim 23 (depends on 22) The method according to claim 22; wherein the introduction of the liquid formulation is effected through the nozzle from below to above. ### Claim 24 A carrier pellet for carrying a pharmaceutically active substance, the carrier pellet comprising at least one physiologically well-tolerated pH regulator, wherein the carrier pellets are produced by the method comprising: a) producing a liquid formulation by dissolving, dispersing, or a combination of dissolving and dispersing at least one physiologically well-tolerated pH regulator in at least one solvent or emulsifier; b) introducing the liquid formulation into a fluidized-bed or spouted-bed unit using at least one nozzle; c) forming essentially spherical carrier pellets by spray granulation in the unit wherein the solvent is evaporated by a drying gas flow; and d) discharging the carrier pellets from the unit. ### Claim 25 (depends on 24) The carrier pellet according to claim 24; wherein the carrier pellet has a diameter in the range of 50 μm to 1.5 mm. ### Claim 26 (depends on 24) The carrier pellet according to claim 24; wherein the carrier pellet is essentially spherical. ### Claim 27 (depends on 26) The carrier pellet according to claim 26; wherein the carrier pellet has a sphericity of 0.8 to 1.0. ### Claim 28 (depends on 24) The carrier pellet according to claim 24; wherein the carrier pellet has a width-length ratio of 0.8 to 1.0. ### Claim 29 (depends on 24) The carrier pellet according to claim 24; wherein the carrier pellet is a dense carrier pellet. ### Claim 30 (depends on 24) A combination of carrier pellets comprising: at least two of the carrier pellets according claim 24; wherein at least two of the carrier pellets in the combination have essentially the same size. ### Claim 31 (depends on 24) A pharmaceutical formulation comprising: one or more carrier pellets according to claim 24; and at least one pharmaceutically active substance. ### Claim 32 (depends on 31) A method of releasing a pharmaceutically active substance, the method comprising: introducing one or more pharmaceutical formulations according to claim 31 into physiological surroundings, wherein the one or more carrier pellets releases the pharmaceutically active substance into the physiological surroundings.