# US 11,433,035 B2 · Dosage forms and methods for enantiomerically enriched or pure bupropion > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,433,035 B2 - Document ID: US11433035B2 - Status: Granted - Kind: B2 - Application number: 16/907,691 - Filed: 2020-06-22 - Published: 2020-10-08 - Granted: 2022-09-06 - Earliest claimed: 2018-09-20 - Assignees: Axsome Therapeutics, Inc. - Applicants: Axsome Therapeutics, Inc. - Inventors: Herriot Tabuteau - Web page: https://patentgrep.com/patent/US11433035B2 ## CPC - A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)} - A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} - A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} - 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 This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation. ## Claims ### Claim 1 A method of treating attention deficit/hyperactivity disorder (AD/HD) comprising orally administering an (S)-bupropion that is at least 95% enantiomerically pure to a human being in need thereof, wherein the (S)-bupropion is not deuterium-enriched, wherein about 20 mg to about 100 mg of the (S)-bupropion is orally administered once daily and is therapeutically effective for treating AD/HD, wherein the (S)-bupropion that is at least 95% enantiomerically pure is orally administered in a dosage form that is free of any active pharmaceutical ingredients other than the (S)-bupropion that is at least 95% enantiomerically pure and the accompanying 5% or less (R)-bupropion. ### Claim 2 (depends on 1) The method of claim 1, wherein the human being has an age of about 18 years or less. ### Claim 3 (depends on 1) The method of claim 1, wherein the dosage form contains a binder. ### Claim 4 (depends on 1) The method of claim 1, wherein the dosage form contains an excipient. ### Claim 5 (depends on 1) The method of claim 1, wherein the dosage form contains a disintegrating agent. ### Claim 6 (depends on 1) The method of claim 1, wherein the dosage form contains a lubricant. ### Claim 7 (depends on 1) The method of claim 1, wherein the method achieves a Cmax of (S)-bupropion in the human being that is at least about 60 ng/mL. ### Claim 8 (depends on 1) The method of claim 1, wherein the method is effective in achieving a Cmax of (S)-bupropion that is at least 5-fold greater than the Cmax of (R)-bupropion that results from orally administering the same amount of (R)-bupropion to the human being. ### Claim 9 (depends on 1) The method of claim 1, wherein the method achieves a Cmax of (R,R)-hydroxybupropion that is at least about 500 ng/mL in the human being. ### Claim 10 (depends on 1) The method of claim 1, wherein the method is effective in achieving a Cmin of (R,R)-hydroxybupropion that is at least 3-fold greater than the Cmin of (R,R)-hydroxybupropion that results from orally administering the same amount of (R)-bupropion to the human being. ### Claim 11 (depends on 1) The method of claim 1, wherein orally administering the (S)-bupropion results in (R,R)-hydroxybupropion that is at least 97% of the total amount of hydroxybupropion present in the plasma of the human being. ### Claim 12 (depends on 1) The method of claim 1, wherein the (S)-bupropion is orally administered for at least 8 consecutive days. ### Claim 13 (depends on 1) The method of claim 1, wherein the (S)-bupropion is orally administered for at least 14 consecutive days. ### Claim 14 (depends on 1) The method of claim 1, wherein the (S)-bupropion is orally administered for at least 21 consecutive days. ### Claim 15 (depends on 1) The method of claim 1, wherein the dosage form provides sustained release of (S)-bupropion. ### Claim 16 (depends on 1) The method of claim 1, wherein the method achieves a Cmax of (R,R)-hydroxybupropion in the human being that is at least about 600 ng/mL. ### Claim 17 (depends on 1) The method of claim 1, wherein the dosage form is in a form of tablet, capsule, or syrup. ### Claim 18 (depends on 1) The method of claim 1, wherein the dosage form is orally administered to the human being under fasting conditions. ### Claim 19 (depends on 1) The method of claim 1, wherein the (S)-bupropion is at least 97% enantiomerically pure. ### Claim 20 (depends on 1) The method of claim 1, wherein the (S)-bupropion is at least 99% enantiomerically pure. ### Claim 21 (depends on 1) The method of claim 1, wherein the (S)-bupropion is in a salt form. ### Claim 22 (depends on 1) The method of claim 1, wherein the (S)-bupropion is in the free base form.