# US 11,304,951 B1 · 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 11,304,951 B1 - Document ID: US11304951B1 - Status: Granted - Kind: B1 - Application number: 17/314,330 - Filed: 2021-05-07 - Granted: 2022-04-19 - Earliest claimed: 2020-11-30 - Assignees: Janssen Pharmaceutica NV - Applicants: Janssen Pharmaceutica NV - Inventors: Srihari Gopal; Raja Venkatasubramanian; Huybrecht T'Jollyn - Web page: https://patentgrep.com/patent/US11304951B1 ## CPC - 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 9/0024: {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 9/10: Dispersions; Emulsions - A61K 47/02: Inorganic compounds - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - 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 - 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) - 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 for administering paliperidone palmitate to a patient in need thereof who has been administered a first dose of a first paliperidone palmitate extended-release injectable suspension (first suspension), the method comprising: administering in a deltoid muscle of the patient a re-initiation loading dose of a second paliperidone palmitate extended-release injectable suspension (second suspension) at a time that is more than six months and three weeks after administration of said first dose of the first suspension but less than eight months after administration of said first dose of the first suspension; and administering in a deltoid or gluteal muscle of the patient a maintenance dose of the first suspension at a time that is one month ±7 days after administering the re-initiation loading dose of the second suspension; wherein there is no intervening dose of paliperidone palmitate between the first dose of the first suspension and the re-initiation loading dose of the second suspension, and no intervening dose of paliperidone palmitate between the re-initiation loading dose of the second suspension and the maintenance dose of the first suspension; wherein the first suspension is a six-month extended release injectable suspension (PP6M), and the second suspension is a one-month extended release injectable suspension (PP1M). ### Claim 2 (depends on 1) The method of claim 1, wherein the first dose of the first suspension comprises about 1092 mg of paliperidone palmitate; the re-initiation loading dose of the second suspension comprises about 156 mg of paliperidone palmitate; and the maintenance dose of the first suspension comprises about 1092 mg of paliperidone palmitate. ### Claim 3 (depends on 1) The method of claim 1, wherein the first dose of the first suspension comprises about 1560 mg of paliperidone palmitate; the re-initiation loading dose of the second suspension comprises about 234 mg of paliperidone palmitate; and the maintenance dose of the first suspension comprises about 1560 mg of paliperidone palmitate. ### Claim 4 (depends on 1) The method of claim 1, wherein the first dose of the first suspension and the maintenance dose of the first suspension are administered in a gluteal muscle. ### Claim 5 (depends on 1) The method of claim 1, wherein the patient is in need of treatment for psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, or bipolar disorder. ### Claim 6 (depends on 5) The method of claim 5, wherein the patient is in need of treatment for schizophrenia. ### Claim 7 (depends on 1) The method of claim 1, wherein the first suspension comprises: about 280 mg/mL to about 350 mg/mL of the paliperidone palmitate; about 8 mg/mL to about 12 mg/mL of a wetting agent; one or more buffering agents; about 65 mg/mL to about 85 mg/mL of a suspending agent; and water q.s. ad 100%. ### Claim 8 (depends on 7) The method of claim 7, wherein the first suspension is from about pH 6.0 to about pH 8.0. ### Claim 9 (depends on 7) The method of claim 7, wherein the one or more buffering agents comprise citric acid monohydrate, sodium dihydrogen phosphate monohydrate, disodium hydrogen phosphate anhydrous, or sodium hydroxide. ### Claim 10 (depends on 7) The method of claim 7, wherein the first suspension comprises: about 312 mg/mL of paliperidone palmitate; about 10 mg/mL of polysorbate 20; and about 75 mg/mL of polyethylene glycol 4000. ### Claim 11 (depends on 7) The method of claim 7, wherein the second suspension comprises: about 140 mg/mL to about 180 mg/ml of the paliperidone palmitate; about 8 mg/mL to about 16 mg/ml of a wetting agent; one or more buffering agents; about 20 mg/mL to about 40 mg/ml of a suspending agent; and water q.s. ad 100%. ### Claim 12 (depends on 11) The method of claim 11, wherein the second suspension is from about pH 6.0 to about 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 second suspension comprises: about 156 mg/mL of paliperidone palmitate; about 12 mg/mL of polysorbate 20; and about 30 mg/mL of polyethylene glycol 4000. ### Claim 15 (depends on 2) The method of claim 2, wherein the patient is in need of treatment for psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, or bipolar disorder. ### Claim 16 (depends on 15) The method of claim 15, wherein the patient is in need of treatment for schizophrenia. ### Claim 17 (depends on 16) The method of claim 16, wherein the first dose of the first suspension and the maintenance dose of the first suspension are administered in a gluteal muscle. ### Claim 18 (depends on 17) The method of claim 17, wherein the first suspension comprises about 280 mg/mL to about 350 mg/mL of paliperidone palmitate, and the second suspension comprises about 140 mg/mL to about 180 mg/ml of paliperidone palmitate. ### Claim 19 (depends on 17) The method of claim 17, wherein the first suspension comprises: about 280 mg/mL to about 350 mg/mL of paliperidone palmitate; about 8 mg/mL to about 12 mg/mL of a wetting agent; one or more buffering agents; about 65 mg/mL to about 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 second suspension comprises: about 140 mg/mL to about 180 mg/ml of paliperidone palmitate; about 8 mg/mL to about 16 mg/ml of a wetting agent; one or more buffering agents; about 20 mg/mL to about 40 mg/ml of a suspending agent; and water q.s. ad 100%. ### Claim 21 (depends on 3) The method of claim 3, wherein the patient is in need of treatment for psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, or bipolar disorder. ### Claim 22 (depends on 21) The method of claim 21, wherein the patient is in need of treatment for schizophrenia. ### Claim 23 (depends on 22) The method of claim 22, wherein the first dose of the first suspension and the maintenance dose of the first suspension are administered in a gluteal muscle. ### Claim 24 (depends on 23) The method of claim 23, wherein the first suspension comprises about 280 mg/mL to about 350 mg/mL of paliperidone palmitate, and the second suspension comprises about 140 mg/mL to about 180 mg/ml of paliperidone palmitate. ### Claim 25 (depends on 23) The method of claim 23, wherein the first suspension comprises: about 280 mg/mL to about 350 mg/mL of paliperidone palmitate; about 8 mg/mL to about 12 mg/mL of a wetting agent; one or more buffering agents; about 65 mg/mL to about 85 mg/mL of a suspending agent; and water q.s. ad 100%. ### Claim 26 (depends on 25) The method of claim 25, wherein the second suspension comprises: about 140 mg/mL to about 180 mg/ml of paliperidone palmitate; about 8 mg/mL to about 16 mg/ml of a wetting agent; one or more buffering agents; about 20 mg/mL to about 40 mg/ml of a suspending agent; and water q.s. ad 100%.