# US 11,439,600 B2 · Abuse deterrent oral solid dosage form > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,439,600 B2 - Document ID: US11439600B2 - Status: Granted - Kind: B2 - Application number: 16/625,271 - Filed: 2018-06-22 - Published: 2020-07-16 - Granted: 2022-09-13 - Earliest claimed: 2017-06-23 - Assignees: Sun Pharma Advanced Research Company Ltd. - Applicants: Sun Pharma Advanced Research Company Limited - Inventors: Nitin Dharmadhikari; Yashoraj Zala; Abhishek Jain; Bramhanand Hanamannavar; Umesh Pai - Web page: https://patentgrep.com/patent/US11439600B2 ## CPC - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 31/485: Morphinan derivatives, e.g. morphine, codeine - A61K 9/2009: {Inorganic compounds} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} - A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol - 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 An abuse deterrent oral solid dosage form comprising: an inner portion comprising a drug susceptible to abuse and a pH dependent polymer soluble in acidic medium an outer portion, wherein the portion is devoid of drug susceptible to abuse and comprises an immediate release form of alkalizer and a sustained release form of alkalizer, the sustained release form of alkalizer comprising an alkalizer and a rate controlling excipient. ## Claims ### Claim 1 An abuse deterrent oral solid dosage form comprising: an inner portion comprising a drug susceptible to abuse, a first immediate release form of one or more alkalizers and a pH dependent polymer soluble in acidic medium, and an outer portion, wherein the outer portion is devoid of drug susceptible to abuse and comprises a mixture of: a second immediate release form of one or more alkalizers; and a sustained release form of an alkalizer, the sustained release form comprising an alkalizer and a rate controlling excipient. ### Claim 2 (depends on 1) The abuse deterrent oral solid dosage form as claimed in claim 1, wherein the alkalizer of the sustained release form is released gradually in a sustained manner over a period of about 2 hours in 0.01 N hydrochloric acid. ### Claim 3 (depends on 1) The abuse deterrent oral solid dosage form of claim 1, wherein the one or more alkalizers in the second immediate release form is sodium carbonate, sodium bicarbonate, magnesium oxide or any mixture thereof, and the alkalizer in the sustained release form is magnesium oxide. ### Claim 4 (depends on 1) The abuse deterrent oral solid dosage form of claim 1, wherein the pH dependent polymer soluble in acidic medium is methyl methacrylate and diethylaminoethyl methacrylate copolymer. ### Claim 5 (depends on 1) The abuse deterrent oral solid dosage form of claim 1, wherein the amount of the alkalizer in the immediate release forms is in the range of about 0.2 to 2.8 millimoles and the amount of the alkalizer in the sustained release form is in the range of about 1.4 to 6 millimoles. ### Claim 6 (depends on 1) The abuse deterrent oral solid dosage form of claim 1, wherein the weight ratio of (i) the total amount of alkalizers and (ii) the pH dependent polymer soluble in acidic medium is the range of 2.0 to 3.0. ### Claim 7 (depends on 1) The abuse deterrent oral solid pharmaceutical composition of claim 1, wherein the rate controlling excipient is selected from ethyl cellulose, cellulose acetate, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, carboxymethyl cellulose, hydroxyethyl methylcellulose, hydroxypropyl cellulose, fatty acids, lower alcohol fatty acid ester, glycerol fatty acid esters, acetylated glycerol fatty acid esters, lactic acid derivatives of mono/diglycerides, sorbitan fatty acid esters, reaction mixtures of polyols and fatty acids, glycerides, vegetable oils, hydrogenated vegetable oils, sterols, and mixtures thereof. ### Claim 8 (depends on 1) The abuse deterrent oral solid pharmaceutical composition of claim 1, wherein the rate controlling excipient is selected from ethyl cellulose, cellulose acetate, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, carboxymethyl cellulose, hydroxyethyl methylcellulose, and hydroxypropyl cellulose. ### Claim 9 (depends on 1) The abuse deterrent oral solid pharmaceutical composition of claim 1, wherein the rate controlling excipient is ethyl cellulose. ### Claim 10 (depends on 1) The abuse deterrent oral solid pharmaceutical composition of claim 1, wherein the sustained release form is in the form of an admixture, granules, extrudates or coated particles. ### Claim 11 (depends on 1) The abuse deterrent oral solid dosage form of claim 1, wherein the amount of the alkalizer in the immediate release form is in the range of about 0.2 to 2.8 millimoles and the amount of the alkalizer in the sustained release form is in the range of about 1.4 to 4.2 millimoles and the total amount of alkalizer is in the range of about 3.75 to 6 millimoles per unit abuse deterrent oral solid dosage form. ### Claim 12 (depends on 1) The abuse deterrent oral solid dosage form of claim 1, wherein the total amount of alkalizer is in the range of about 3.75 to 6 millimoles per unit abuse deterrent oral solid dosage form. ### Claim 13 (depends on 1) A method of treating a patient having hyperacidity with a drug susceptible to abuse, the method comprising administering an abuse deterrent oral solid dosage form according to claim 1 to the patient. ### Claim 14 (depends on 13) The method of claim 13, wherein the abuse deterrent oral solid dosage form is administered to the patient in the fed state. ### Claim 15 (depends on 1) A method of treating a patient having acid rebound effect with a drug susceptible to abuse, the method comprising administering an abuse deterrent oral solid dosage form according to claim 1 to the patient. ### Claim 16 (depends on 15) The method of claim 15, wherein the abuse deterrent oral solid dosage form is administered to the patient in the fed state.