# US 11,992,559 B2 · Microsphere formulations comprising lurasidone and methods for making and using the same > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,992,559 B2 - Document ID: US11992559B2 - Status: Granted - Kind: B2 - Application number: 17/679,385 - Filed: 2022-02-24 - Published: 2022-08-25 - Granted: 2024-05-28 - Earliest claimed: 2021-02-24 - Assignees: Oakwood Laboratories, LLC - Applicants: Oakwood Laboratories, LLC - Inventors: Colin Spencer; Griffin Beyer; Tracy Richey; Mark Smith; Nicholas DeLucia - Web page: https://patentgrep.com/patent/US11992559B2 ## CPC - A61K 9/50: Microcapsules {having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals (A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167)} - 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 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)} - A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)} - A61K 9/5089: {Processes} - A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin - A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) - 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 Extended-release microsphere formulations comprising lurasidone are provided. In one aspect, the microsphere formulations are characterized in that the lurasidone is released in vivo in humans over a period of about 30 days. Methods for making and using the formulations are also provided. ## Claims ### Claim 1 A microsphere formulation, comprising: polymer microspheres, each polymer microsphere comprising: an active pharmaceutical ingredient consisting of lurasidone or a pharmaceutically acceptable salt thereof; and a biodegradable polymer wherein the biodegradable polymer comprises an acid terminated poly(D,L-lactide-co-glycolide) with lactide:glycolide ratio of about 75 to about 25, and wherein the biodegradable polymer has an inherent viscosity of about 0.14 dL/g to about 0.56 dL/g, wherein each polymer microsphere comprises a drug load of lurasidone of greater than or equal to 55% by weight of the polymer microsphere, and wherein the polymer microspheres have a particle size of less than or equal to 25 μm (D50). ### Claim 2 (depends on 1) The microsphere formulation of claim 1, wherein the pharmaceutically acceptable salt of lurasidone is lurasidone HCl. ### Claim 3 (depends on 1) The microsphere formulation of claim 1, wherein each polymer microsphere has a lurasidone drug load of from 55% to about 70% by weight of the polymer microsphere; and wherein the polymer microspheres have a particle size of from about 9 μm to 25 μm (D50). ### Claim 4 (depends on 3) The microsphere formulation of claim 3, wherein the polymer microspheres have been irradiated. ### Claim 5 (depends on 1) A pharmaceutical composition comprising the microsphere formulation of claim 1. ### Claim 6 (depends on 1) The microsphere formulation of claim 1, characterized in that about 75% to 100% of the lurasidone is released over a period of about 30 days of injection into a subject, but not more than about 20% of the lurasidone has been released within about 24 hours of injection into the subject. ### Claim 7 (depends on 3) The microsphere formulation of claim 3, wherein the polymer microspheres have a particle size of between about 14 μm (D50) and 25 μm (D50). ### Claim 8 (depends on 3) The microsphere formulation of claim 3, wherein: the biodegradable polymer comprises an acid terminated poly(D,L-lactide-co-glycolide) with lactide:glycolide of about 75: about 25, and wherein the biodegradable polymer has an inherent viscosity of from about 0.14 dL/g to about 0.21 dL/g. ### Claim 9 (depends on 3) The microsphere formulation of claim 3, wherein: the biodegradable polymer comprises an acid terminated poly(D,L-lactide-co-glycolide) with lactide:glycolide of about 75: about 25, and wherein the biodegradable polymer has an inherent viscosity of from about 0.14 dL/g to about 0.29 dL/g. ### Claim 10 (depends on 3) The microsphere formulation of claim 3, wherein the polymer microspheres have a particle size of from about 14 μm (D50) to about 20 μm (D50). ### Claim 11 (depends on 3) A pharmaceutical composition comprising the microsphere formulation of claim 3. ### Claim 12 (depends on 3) The microsphere formulation of claim 3, characterized in that about 75% to 100% of the lurasidone is released over a period of about 30 days of injection into a subject, but not more than about 20% of the lurasidone has been released within about 24 hours of injection into the subject. ### Claim 13 A microsphere formulation, comprising: polymer microspheres, each polymer microsphere comprising: an active pharmaceutical ingredient consisting of lurasidone HCl; and a biodegradable polymer comprising an acid terminated poly(D,L-lactide-co-glycolide) (“PLGA”) with lactide:glycolide of about 75: about 25 and an inherent viscosity of from about 0.14 dL/g to about 0.56 dL/g, wherein each polymer microsphere has a lurasidone drug load of from 55% to about 70% by weight of the polymer microsphere; wherein the polymer microspheres have a particle size of about 14 μm (D50) to about 25 μm (D50); and wherein the microsphere formulation is characterized in that about 75% to 100% of the lurasidone is released over a period of about 30 days of injection into a subject, but not more than about 20% of the lurasidone has been released within about 24 hours of injection into the subject. ### Claim 14 (depends on 13) A pharmaceutical composition comprising the microsphere formulation of claim 13. ### Claim 15 (depends on 13) The microsphere formulation of claim 13, wherein the inherent viscosity of the PLGA is from about 0.14 dL/g to about 0.29 dL/g. ### Claim 16 (depends on 13) The microsphere formulation of claim 13, wherein the inherent viscosity of the PLGA is from about 0.14 dL/g to about 0.21 dL/g.