# US 11,439,647 B2 · Dosing regimens associated with extended release paliperidone injectable formulations > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,439,647 B2 - Document ID: US11439647B2 - Status: Granted - Kind: B2 - Application number: 17/314,245 - Filed: 2021-05-07 - Published: 2022-06-02 - Granted: 2022-09-13 - Earliest claimed: 2020-11-30 - Assignees: Janssen Pharmaceutica NV - Applicants: Janssen Pharmaceutica NV - Inventors: Ruth Milz; Frank Wiegand; Panna Sanga; John Louie - Web page: https://patentgrep.com/patent/US11439647B2 ## CPC - A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)} - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - 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 9/10: Dispersions; Emulsions - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin - A61P 3/04: Anorexiants; Antiobesity agents - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 25/24: Antidepressants - 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 present invention provides a method of treating patients with long acting injectable paliperidone palmitate formulations. ## Claims ### Claim 1 A method of stabilizing or decreasing body weight of a patient who has been treated with a paliperidone palmitate extended-release injectable suspension at either one-month intervals (PP1M) or three-month intervals (PP3M), comprising administering a last dose of the PP1M or the PP3M and then administering an initial dose of a paliperidone palmitate extended-release injectable suspension having a six month dosing interval (PP6M), wherein the patient has a body mass index (BMI) of 25 to less than 30 at the time of the initial dose of the PP6M. ### Claim 2 (depends on 1) The method of claim 1, wherein the patient has been treated with the PP1M for at least four months. ### Claim 3 (depends on 1) The method of claim 1, wherein the patient has been treated with the PP3M for at least one 3-month interval. ### Claim 4 (depends on 2) The method of claim 2, wherein the initial dose of the PP6M is administered 1 month ±7 days after the last dose of the PP1M is administered. ### Claim 5 (depends on 4) The method of claim 4, wherein: when the last dose of the PP1M comprises 156 mg of paliperidone palmitate, the initial dose of the PP6M comprises 1092 mg of paliperidone palmitate. ### Claim 6 (depends on 4) The method of claim 4, wherein: when the last dose of the PP1M comprises 234 mg of paliperidone palmitate, the initial dose of the PP6M comprises 1560 mg of paliperidone palmitate. ### Claim 7 (depends on 3) The method of claim 3, wherein the initial dose of the PP6M is administered 3 months after the last dose of the PP3M is administered. ### Claim 8 (depends on 7) The method of claim 7, wherein: when the last dose of the PP3M comprises 546 mg of paliperidone palmitate, the initial dose of the PP6M comprises 1092 mg of paliperidone palmitate. ### Claim 9 (depends on 7) The method of claim 7, wherein: when the last dose of the PP3M comprises 819 mg of paliperidone palmitate, the initial dose of the PP6M comprises 1560 mg of paliperidone palmitate. ### Claim 10 (depends on 9) The method of claim 9, wherein the patient's body weight is assessed at the time of the initial dose of the PP6M. ### Claim 11 (depends on 9) The method of claim 9, wherein the PP3M and PP6M each comprise: 280 mg/mL to 350 mg/mL of the paliperidone palmitate; 8 mg/mL to 12 mg/mL of a wetting agent; one or more buffering agents; 65 mg/mL to 85 mg/mL of a suspending agent; and water q.s. ad 100%. ### Claim 12 (depends on 11) The method of claim 11, wherein the PP3M or PP6M is from pH 6.0 to pH 8.0. ### Claim 13 (depends on 11) The method of claim 11, wherein the one or more buffering agents comprise citric acid monohydrate, sodium dihydrogen phosphate monohydrate, disodium hydrogen phosphate anhydrous, or sodium hydroxide. ### Claim 14 (depends on 11) The method of claim 11, wherein the PP3M and PP6M each comprise: 312 mg/mL of paliperidone palmitate; 10 mg/mL of polysorbate 20; and 75 mg/mL of polyethylene glycol 4000. ### Claim 15 (depends on 4) The method of claim 4, wherein the PP1M comprises: 140 mg/mL to 180 mg/ml of the paliperidone palmitate; 8 mg/mL to 16 mg/ml of a wetting agent; one or more buffering agents; 20 mg/mL to 40 mg/ml of a suspending agent; and water q.s. ad 100%. ### Claim 16 (depends on 15) The method of claim 15, wherein the PP1M is from pH 6.0 to pH 8.0. ### Claim 17 (depends on 15) The method of claim 15, wherein the one or more buffering agents comprise citric acid monohydrate, sodium dihydrogen phosphate monohydrate, disodium hydrogen phosphate anhydrous, or sodium hydroxide. ### Claim 18 (depends on 15) The method of claim 15, wherein the PP1M comprises: 156 mg/mL of paliperidone palmitate; 12 mg/mL of polysorbate 20; and 30 mg/mL of polyethylene glycol 4000. ### Claim 19 (depends on 15) The method of claim 15, wherein the PP6M comprises: 280 mg/mL to 350 mg/mL of the paliperidone palmitate; 8 mg/mL to 12 mg/mL of a wetting agent; one or more buffering agents; 65 mg/mL to 85 mg/mL of a suspending agent; and water q.s. ad 100%. ### Claim 20 (depends on 19) The method of claim 19, wherein the PP6M is from pH 6.0 to pH 8.0. ### Claim 21 (depends on 19) The method of claim 19, wherein the one or more buffering agents comprise citric acid monohydrate, sodium dihydrogen phosphate monohydrate, disodium hydrogen phosphate anhydrous, or sodium hydroxide. ### Claim 22 (depends on 19) The method of claim 19, wherein the PP6M comprises: 312 mg/mL of paliperidone palmitate; 10 mg/mL of polysorbate 20; and 75 mg/mL of polyethylene glycol 4000. ### Claim 23 (depends on 9) The method of claim 9, wherein the PP3M and PP6M each comprise 280 mg/mL to 350 mg/mL of paliperidone palmitate. ### Claim 24 (depends on 9) The method of claim 9, wherein the PP3M and PP6M each comprise 312 mg/mL of paliperidone palmitate.