Formulations for c-Met kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9238571-B2
Application number	US-201013498600-A
Country	US
Kind code	B2
Filing date	Sep 21, 2010
Priority date	Sep 30, 2009
Publication date	Jan 19, 2016
Grant date	Jan 19, 2016

Abstract

The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.

First claim

What is claimed is:

1. A pharmaceutical composition comprising from 30% to 35% by weight of 1-[3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2- ylmethyl)methanesulfonamide or a pharmaceutically acceptable salt thereof, 40% to 45% by weight of an acidulant, 20% to 25% by weight of a diluent, 1.0% to 5.0% by weight of a disintegrant and from 0.5% to 2.0% by weight of a lubricant, wherein the weight ratio of 1-[3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide to acidulant is selected from within a range of 0.3 to 5.0.

2. The pharmaceutical composition of claim 1 wherein the acidulent is selected from the group consisting of acetic, adipic, benzenesulphonic, benzoic, caprylic, cinnamic, citric, ethanedisulphonic, tartaric, ascorbic, maleic, glutamic, lactic, oxalic, L-Aspartic, 2-hydroxyethanesulfonic, pamoic, malonic, gentisic, salicylic, fumaric, glucoheptoic, gluconic, glucuronic, hippuric, lactobionic, laurylsulfuric, malic, malonic, mandelic, methanesulphonic, propionic, stearic, toluenesulphonic, undecylenic, camphorsulfonic and oleic acid.

3. The pharmaceutical composition of claim 1 wherein the diluent is selected from the group consisting of microcrystalline cellulose, lactose, mannitol, calcium phosphate, calcium carbonate, magnesium carbonate, sucrose, glucose, sorbitol, calcium sulfate, powdered cellulose, silicified microcrystalline cellulose, cellulose acetate, compressible sugar, dextrates, dextrin, dextrose, ethylcelluose, fructose, glyceryl palmitostearate, kaolin, lactitol, magnesium carbonate, magnesium oxide, maltodextrin, maltose, medium-chain triglycerides, polydextrose, polymethacrylates, simethicone, sodium alginate, sodium chloride, tragacanth, trehalose, xylitol and starch.

4. The pharmaceutical composition of claim 1 wherein the disintegrant is selected from the group consisting of croscarmellose sodium, starch, crospovidone, sodium starch glycolate, calcium carbonate, sodium carbonate, magnesium carbonate, alginic acid, tribasic calcium phosphate, calcium carboxymethylcellulose, sodium carboxymethylcellulose, powdered cellulose, chitosan, colloidal silicon dioxide, guar gum, hydroxypropyl cellulose, magnesium aluminium silicate, methylcellulose, povidone, and sodium alginate.

5. The pharmaceutical composition of claim 1 wherein the lubricant is selected from the group consisting of magnesium stearate, stearic acid, sodium stearyl fumerate, talc, calcium stearate, glycerin monostearate, glyceryl behenate, glyceryl palmitostearate, magnesium lauyl sulfate, medium chain triglycerides, poloxamer, sodium benzoate, sodium chloride, sodium lauryl sulfate and zinc stearate.

6. The pharmaceutical composition of claim 1 wherein the acidulant is citric acid, the diluent is microcrystalline cellulose, the disintegrant is croscarmellose sodium and the lubricant is magnesium stearate.

7. A method of improving the absorption of a c-Met kinase inhibitor by administering to a patient the pharmaceutical composition of claim 1 .

Assignees

• Ward Robert
• Merck Sharp & Dohme

Inventors

• Ward Robert

Classifications

• A61K31/444

  containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone · CPC title

• B66C23/76

  and movable to take account of variations of load or of variations of length of jib · CPC title

• A61K9/1617

  Organic compounds, e.g. phospholipids, fats · CPC title

• A61K9/1694

  resulting in granules or microspheres of the matrix type containing more than 5% of excipient · CPC title

• B66C23/44 Primary

  Jib-cranes adapted for attachment to standard vehicles, e.g. agricultural tractors · CPC title