# US 11,298,352 B2 · Bupropion as a modulator of drug activity > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,298,352 B2 - Document ID: US11298352B2 - Status: Granted - Kind: B2 - Application number: 17/201,820 - Filed: 2021-03-15 - Published: 2021-07-22 - Granted: 2022-04-12 - Earliest claimed: 2013-11-05 - Assignees: Antecip Bioventures II LLC - Applicants: Antecip Bioventures II LLC - Inventors: Herriot Tabuteau - Web page: https://patentgrep.com/patent/US11298352B2 ## CPC - A61K 31/485: Morphinan derivatives, e.g. morphine, codeine - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} - A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} - A61K 31/15: Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) {; Imines (C—N=C)} - A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone - A61K 31/381: having five-membered rings - A61P 25/04: Centrally acting analgesics, e.g. opioids - 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 Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan. ## Claims ### Claim 1 A method of increasing dextromethorphan plasma levels, comprising co-administering bupropion and dextromethorphan once a day or twice a day for at least 8 consecutive days to a human being who is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan; wherein about 90 mg to about 220 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion is co-administered with dextromethorphan hydrobromide, or the free base form or another salt form of dextromethorphan, once or twice a day; and wherein the bupropion and the dextromethorphan are the only therapeutically active agents to be co-administered and co-administering the bupropion and the dextromethorphan results in an AUC0-24 of dextromethorphan on the eighth day that is at least about 20 times the AUC0-24 of dextromethorphan that would result from administering the same daily dose of the dextromethorphan without the bupropion for eight consecutive days. ### Claim 2 (depends on 1) The method of claim 1, wherein co-administering the bupropion and the dextromethorphan results in an AUC0-24 of dextromethorphan on the eighth day that is about 20 times to about 80 times the AUC0-24 that would result from administering the same daily dose of the dextromethorphan without the bupropion for eight consecutive days. ### Claim 3 (depends on 2) The method of claim 2, wherein about 90 mg to about 150 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion, is co-administered with about 40 mg to about 60 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan, once a day or twice a day. ### Claim 4 (depends on 3) The method of claim 3, wherein the AUC0-24 of dextromethorphan on the eighth day is about 1,900 ng·hr/mL. ### Claim 5 (depends on 3) The method of claim 3, wherein the AUC0-24 of dextromethorphan on the eighth day is about 1300 ng·hr/mL to 2,975 ng·hr/mL. ### Claim 6 (depends on 5) The method of claim 5, wherein about 105 mg of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion, is co-administered with about 42 mg to about 48 mg of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan, once a day or twice a day. ### Claim 7 (depends on 5) The method of claim 5, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of depression. ### Claim 8 (depends on 5) The method of claim 5, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of nicotine addiction. ### Claim 9 (depends on 5) The method of claim 5, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of agitation associated with Alzheimer's disease. ### Claim 10 (depends on 5) The method of claim 5, wherein the Cmax of dextromethorphan on the eighth day is about 69 ng/mL to about 154 ng/ml. ### Claim 11 (depends on 10) The method of claim 10, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of depression. ### Claim 12 (depends on 10) The method of claim 10, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of nicotine addiction. ### Claim 13 (depends on 10) The method of claim 10, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of agitation associated with Alzheimer's disease. ### Claim 14 (depends on 10) The method of claim 10, wherein AUC0-12 of bupropion on the eighth day is at least 600 ng·hr/mL. ### Claim 15 (depends on 14) The method of claim 14, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of depression. ### Claim 16 (depends on 14) The method of claim 14, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of nicotine addiction. ### Claim 17 (depends on 14) The method of claim 14, wherein the bupropion and the dextromethorphan are co-administered to the human being for the treatment of agitation associated with Alzheimer's disease. ### Claim 18 (depends on 14) The method of claim 14, wherein the bupropion and the dextromethorphan are co-administered once a day or twice a day for at least 14 consecutive days. ### Claim 19 (depends on 14) The method of claim 14, wherein the bupropion and the dextromethorphan are co-administered once a day or twice a day for at least 30 consecutive days. ### Claim 20 (depends on 14) The method of claim 14, wherein the human being is converted to poor metabolizer status on the eighth day after co-administering the bupropion and the dextromethorphan.