# US 11,439,636 B1 · 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 11,439,636 B1 - Document ID: US11439636B1 - Status: Granted - Kind: B1 - Application number: 17/405,429 - Filed: 2021-08-18 - Granted: 2022-09-13 - Earliest claimed: 2013-11-05 - Assignees: Antecip Bioventures II LLC - Applicants: Antecip Bioventures II LLC - Inventors: Herriot Tabuteau - Web page: https://patentgrep.com/patent/US11439636B1 ## 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 - 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 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 in a human being, comprising orally administering, once a day or twice a day, a dosage form comprising bupropion and dextromethorphan to the human being, wherein the human being is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the dosage form contains about 75 mg to about 150 mg of the bupropion and about 45 mg of the dextromethorphan and bupropion and dextromethorphan are the only therapeutically active agents to be administered, wherein the dosage form is orally administered for at least eight consecutive days, and wherein on the eighth day that the dosage form is orally administered, the human being has a Cmin of dextromethorphan that is at least about 40 ng/mL. ### Claim 2 (depends on 1) The method of claim 1, wherein the dosage form contains about 45 mg of the dextromethorphan and about 100 mg to about 140 mg of the bupropion. ### Claim 3 (depends on 1) The method of claim 1, wherein on the eighth day that the dosage form is orally administered, the human being has a Cmin of dextromethorphan that is at least about 15 times the Cmin that would be achieved by orally administering the same amount of the dextromethorphan without bupropion for eight consecutive days. ### Claim 4 (depends on 1) The method of claim 1, wherein on the eighth day that the dosage form is orally administered, the human being has an AUC0-12 of dextromethorphan that is at least about 700 ng·hr/mL. ### Claim 5 (depends on 1) The method of claim 1, wherein on the eighth day that the dosage form is orally administered, the human being has an AUC0-12 of dextromethorphan that is about 750 ng·hr/mL. ### Claim 6 (depends on 1) The method of claim 1, wherein on the eighth day that the dosage form is orally administered, the human being has a Cmax of dextromethorphan that is at least about 70 ng/mL. ### Claim 7 A method of increasing dextromethorphan plasma levels in a human being, comprising orally administering, once a day or twice a day, a dosage form comprising bupropion and dextromethorphan to the human being, wherein the human being is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the dosage form contains about 75 mg to about 150 mg of the bupropion and about 45 mg of the dextromethorphan and bupropion and dextromethorphan are the only therapeutically active agents to be administered, wherein the dosage form is orally administered for at least eight consecutive days, and wherein on the eighth day that the dosage form is orally administered, the human being has a Cmin of dextromethorphan that is about 45 ng/mL. ### Claim 8 (depends on 7) The method of claim 7, wherein on the eighth day that the dosage form is orally administered, the human being has a Cmin of dextromethorphan that is at least about 15 times the Cmin that would be achieved by orally administering the same amount of the dextromethorphan without bupropion for eight consecutive days. ### Claim 9 (depends on 7) The method of claim 7, wherein the bupropion and the dextromethorphan are in separate domains, layers, or phases within the dosage form. ### Claim 10 (depends on 9) The method of claim 9, wherein the domains, the layers, or the phases containing the bupropion provide sustained release of bupropion and the domains, the layers, or the phases containing the dextromethorphan provide immediate release of dextromethorphan. ### Claim 11 (depends on 7) The method of claim 7, wherein the human being is at risk of experiencing an adverse event as a result of being treated with dextromethorphan. ### Claim 12 (depends on 7) The method of claim 7, wherein the human being is at risk of experiencing an adverse event as a result of being treated with bupropion. ### Claim 13 (depends on 7) The method of claim 7, wherein the dosage form is orally administered for at least 30 consecutive days. ### Claim 14 (depends on 7) The method of claim 7, wherein on the eighth day that the dosage form is orally administered, the human being is converted to a poor metabolizer of dextromethorphan. ### Claim 15 (depends on 7) The method of claim 7, wherein the human being is at least 18 years of age. ### Claim 16 A method of increasing dextromethorphan plasma levels in a human being, comprising orally administering, once a day or twice a day, a dosage form comprising bupropion and dextromethorphan to the human being, wherein the human being is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the dosage form contains about 75 mg to about 150 mg of the bupropion and about 45 mg of the dextromethorphan and bupropion and dextromethorphan are the only therapeutically active agents to be administered, wherein the dosage form is orally administered for at least eight consecutive days, and wherein on the eighth day that the dosage form is orally administered, the human being has a Cmin of dextromethorphan that is about 40 ng/mL to 119.3 ng/mL. ### Claim 17 (depends on 16) The method of claim 16, wherein the dosage form contains about 45 mg of the dextromethorphan and about 100 mg to about 140 mg of the bupropion. ### Claim 18 (depends on 16) The method of claim 16, wherein on the eighth day that the dosage form is orally administered, the human being has a Cmin of dextromethorphan that is at least about 15 times the Cmin that would be achieved by orally administering the same amount of the dextromethorphan without bupropion for eight consecutive days. ### Claim 19 (depends on 16) The method of claim 16, wherein the dosage form provides sustained release of bupropion and immediate release of dextromethorphan. ### Claim 20 (depends on 16) The method of claim 16, wherein the dextromethorphan or the bupropion is deuterium-modified. ### Claim 21 (depends on 1) The method of claim 1, wherein the human being is at risk of experiencing an adverse event as a result of being treated with bupropion. ### Claim 22 (depends on 16) The method of claim 16, wherein the human being is at risk of experiencing an adverse event as a result of being treated with bupropion.