# US 8,541,025 B2 · Co-crystals and pharmaceutical formulations comprising the same > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,541,025 B2 - Document ID: US8541025B2 - Status: Granted - Kind: B2 - Application number: 13/034,039 - Filed: 2011-02-24 - Published: 2011-09-29 - Granted: 2013-09-24 - Earliest claimed: 2008-09-03 - Assignees: Vertex Pharmaceuticals Incorporated - Applicants: Eleni Dokou; Rahela Gasparac; Dragutin Knezic; Billie J. Kline; Valdas Jurkauskas - Inventors: Eleni Dokou; Rahela Gasparac; Dragutin Knezic; Billie J. Kline; Valdas Jurkauskas - Web page: https://patentgrep.com/patent/US8541025B2 ## CPC - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 31/497: containing further heterocyclic rings - A61K 31/658: {o-phenolic cannabinoids, e.g. cannabidiol, cannabigerolic acid, cannabichromene or tetrahydrocannabinol} - A61P 31/14: for RNA viruses - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - 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 An immediate release formulation of an active ingredient. ## Claims ### Claim 1 A pharmaceutical composition comprising: an active ingredient, and one or more excipients present in an amount about at least 1% of the total weight of the formulation, wherein the active ingredient comprises a co-crystal, the co-crystal comprising VX-950 and a co-former of 4-hydroxybenzoic acid, wherein the co-crystal is present in amount about at least 68% of the total weight of the formulation. ### Claim 2 (depends on 1) The formulation of claim 1, wherein the molar ratio of the active ingredient with respect to the co-former ranges from about 5:1 to about 1:5. ### Claim 3 (depends on 2) The formulation of claim 2, wherein the molar ratio of VX-950 with respect to the co-former is about 1:1. ### Claim 4 (depends on 1) The formulation of claim 1, wherein the one or more excipients is selected from the group consisting of a filler, a surfactant, a glidant, a lubricant and a disintegrant. ### Claim 5 (depends on 1) The formulation of claim 1, wherein the one or more excipients comprises one or more fillers. ### Claim 6 (depends on 5) The formulation of claim 5, wherein the one or more fillers is selected from one or more from the group consisting of the following: mannitol, lactose, sucrose, dextrose, maltodextrin, sorbitol, xylitol, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, methylcellulose, ethylcellulose, hydroxyethylcellulose, methylhydroxyethylcellulose, talc, starch, pregelatinized starch, dibasic calcium phosphate, calcium sulfate and calcium carbonate. ### Claim 7 (depends on 6) The formulation of claim 6, wherein the one or more fillers is microcrystalline cellulose, lactose or a combination thereof. ### Claim 8 (depends on 6) The formulation of claim 6, wherein the one or more fillers are microcrystalline cellulose, and lactose. ### Claim 9 (depends on 1) The formulation of claim 1, wherein the one or more excipients comprises one or more disintegrants. ### Claim 10 (depends on 9) The formulation of claim 9, wherein the one or more disintegrants is selected from one or more from the group consisting of the following: croscarmellose sodium, sodium alginate, calcium alginate, alginic acid, starch, pregelatinized starch, sodium starch glycolate, crospovidone, cellulose and its derivatives, carboxymethylcellulose calcium, carboxymethylcellulose sodium, soy polysaccharide, guar gum, an ion exchange resin, an effervescent system based on food acids and an alkaline carbonate component, and sodium bicarbonate. ### Claim 11 (depends on 10) The formulation of claim 10, wherein the one or more disintegrants is croscarmellose sodium. ### Claim 12 (depends on 1) The formulation of claim 1, wherein the one or more excipients comprises one or more surfactants. ### Claim 13 (depends on 1) The formulation of claim 1, wherein the one or more surfactants is selected from one or more from the group consisting of the following: sodium lauryl sulfate, docusate sodium, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene 20 stearyl ethers, polyoxyethylene alkyl ethers, polyoxyethylene castor oil derivatives, pegylated hydrogenated castor oils, sorbitan esters of fatty acids, Vitamin E or tocol derivatives, vitamin E TPGS, tocopheryl esters, lecithin, phospholipids and their derivatives, poloxamers, stearic acid, oleic acid, oleic alcohol, cetyl alcohol, mono and diglycerides, propylene glycol esters of fatty acids, glycerol esters of fatty acids, ethylene glycol palmitostearate, polyoxylglycerides, propylene glycol monocaprylate, propylene glycol monolaurate and polyglyceryl oleate. ### Claim 14 (depends on 13) The formulation of claim 13, wherein the one or more surfactants is sodium lauryl sulfate. ### Claim 15 (depends on 1) The formulation of claim 1, wherein the one or more excipients includes one or more glidants. ### Claim 16 (depends on 15) The formulation of claim 15, wherein the one or more glidants is selected from one or more from the group consisting of the following: talc, colloidal silica, magnesium oxide, magnesium silicate, leucine and starch. ### Claim 17 (depends on 16) The formulation of claim 16, wherein the one or more glidants is colloidal silica. ### Claim 18 (depends on 1) The formulation of claim 1, wherein the one or more excipients includes one or more lubricants. ### Claim 19 (depends on 18) The formulation of claim 18, wherein the one or more lubricants is selected from one or more from the group consisting of the following: talc, fatty acid, stearic acid, magnesium stearate, calcium stearate, sodium stearate, glyceryl monostearate, sodium lauryl sulfate, sodium stearyl fumarate, hydrogenated oils, fatty alcohol, fatty acid ester, glyceryl behenate, mineral oil, vegetable oil, leucine, sodium benzoate, or a combination thereof. ### Claim 20 (depends on 19) The formulation of claim 19, wherein the one or more lubricants is sodium stearyl fumarate. ### Claim 21 (depends on 1) The formulation of claim 1 comprising: about 68 wt. % of the co-crystal, about 12 wt. % of a first filler; about 12 wt. % of a second filler; about 3 wt. % of a disintegrant; about 2 wt. % of a surfactant; about 1 wt. % of a glidant; and about 3 wt. % of a lubricant. ### Claim 22 (depends on 1) The formulation of claim 1, wherein the one or more excipients comprises microcrystalline cellulose, lactose, croscarmellose sodium, sodium lauryl sulfate, colloidal silica and sodium stearyl fumarate. ### Claim 23 (depends on 1) The formulation of claim 1 comprising: about 68 wt. % of the co-crystal, about 12 wt. % of microcrystalline sodium; about 12 wt. % lactose; about 3 wt. % of croscarmellose sodium; about 2 wt. % of sodium lauryl sulfate; about 1 wt. % of colloidal silica; and about 3 wt. % of sodium stearyl fumarate. ### Claim 24 (depends on 1) The formulation of claim 1, wherein the formulation is in a form of a capsule, tablet, pill, powder, granule, aqueous suspension or solution. ### Claim 25 (depends on 24) The formulation of claim 24, wherein the formulation is in a form of a capsule. ### Claim 26 (depends on 24) The formulation of claim 24, wherein the formulation is in a form of a tablet. ### Claim 27 (depends on 26) The formulation of claim 26, wherein the tablet is coated. ### Claim 28 (depends on 1) The formulation of claim 1, wherein the formulation is an immediate release formulation.