# US 2021/0275546 A1 · High drug load solid oral dosage forms of dexamethasone > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2021/0275546 A1 - Document ID: US20210275546A1 - Status: Published application - Kind: A1 - Application number: 17/319,487 - Filed: 2021-05-13 - Published: 2021-09-09 - Earliest claimed: 2020-05-14 - Assignees: Jubilant Pharma Holdings Inc. - Applicants: Jubilant Pharma Holdings Inc. - Inventors: Indranil Nandi - Web page: https://patentgrep.com/patent/US20210275546A1 ## CPC - A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/2009: {Inorganic compounds} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 9/4841: {Filling excipients; Inactive ingredients} - 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 The present invention relates to high drug load solid oral pharmaceutical compositions comprising dexamethasone or its pharmaceutically acceptable salts or solvates thereof. The present invention also relates to a process for preparing high drug load solid oral pharmaceutical compositions comprising dexamethasone or its pharmaceutically acceptable salts or solvates thereof. The preferred drug load in the compositions of the present invention is from about 26% to 50% by weight based on the total weight of the composition. The prepared compositions of dexamethasone as per the present invention exhibit desirable technical attributes. ## Claims ### Claim 1 A high drug load solid oral pharmaceutical composition comprising: i) about 26% to about 50% by weight of dexamethasone or its pharmaceutically acceptable salts or solvates thereof; ii) from 0 to about 70% by weight of one or more diluents; iii) from 0 to about 30% by weight of one or more binders; iv) from 0 to about 20% by weight of one or more disintegrants; and v) from 0.1% to about 5% by weight of one or more lubricants. ### Claim 2 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, further comprises one or more pharmaceutically acceptable excipients selected from glidant and surfactant. ### Claim 3 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the composition is substantially free of any starch excipient. ### Claim 4 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the composition is free of any dry binder in an intra-granular part of the composition. ### Claim 5 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the composition is free of any binder. ### Claim 6 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the composition comprises dexamethasone or its pharmaceutically acceptable salts or solvates thereof in an amount of about 27.5% or more. ### Claim 7 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the diluent comprises one or more of lactose, mannitol, microcrystalline cellulose, silicified microcrystalline cellulose, starch, pregelatinized starch, and dicalcium phosphate. ### Claim 8 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the binder comprises one or more of hydroxypropyl methylcellulose, povidone, starch, and microcrystalline cellulose. ### Claim 9 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the disintegrant comprises one or more of pregelatinized starch, sodium starch glycolate, crospovidone, croscarmellose sodium, and microcrystalline cellulose. ### Claim 10 (depends on 2) The high drug load solid oral pharmaceutical composition according to claim 2, wherein the glidant comprises one or more of talc, magnesium silicate, colloidal silicon dioxide, amorphous silicon dioxide, and calcium silicate. ### Claim 11 (depends on 2) The high drug load solid oral pharmaceutical composition according to claim 2, wherein the surfactant comprises one or more of sodium lauryl sulphate, polysorbate, and poloxamers. ### Claim 12 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, prepared by wet or dry granulation process. ### Claim 13 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, prepared by the direct compression process. ### Claim 14 (depends on 1) The high drug load solid oral pharmaceutical composition according to claim 1, wherein the composition is in the form of a tablet. ### Claim 15 A high drug load immediate-release tablet composition comprising: i) about 26% to about 35% by weight of dexamethasone or its pharmaceutically acceptable salts or solvates thereof; ii) from about 50% to about 70% by weight of one or more diluents; iii) from about 0.01% to about 10% by weight of one or more disintegrants; and iv) from about 0.1% to about 5% by weight of one or more lubricants; wherein the composition is free of a binder. ### Claim 16 A high drug load immediate-release tablet composition comprising: i) about 26% to about 35% by weight of dexamethasone or its pharmaceutically acceptable salts or solvates thereof; ii) from about 50% to about 70% by weight of one or more diluents; iii) from about 0.01% to about 10% by weight of one or more binders; and iv) from about 0.1% to about 5% by weight of one or more lubricants; wherein the composition is free of a disintegrant. ### Claim 17 (depends on 15) The high drug load immediate-release tablet composition according to claim 15, wherein the composition comprises 20 mg of dexamethasone. ### Claim 18 (depends on 15) The high drug load immediate-release tablet composition according to claim 15, wherein the composition further comprises from about 0.01% to about 5% by weight of one or more glidants. ### Claim 19 (depends on 15) The high drug load immediate-release tablet composition according to claim 15, wherein the composition further comprises from about 0.01% to about 5% by weight of one or more surfactants. ### Claim 20 (depends on 15) The high drug load immediate-release tablet composition according to claim 15, wherein the composition releases more than 70% of drug within 45 minutes in 500 ml of 0.1N Hydrochloric acid, using USP II apparatus (Paddle) at a temperature of 37±0.5° C. and a rotation speed of 50 revolutions per minute.