FIELD: medicine; pharmaceutics.
SUBSTANCE: group of inventions relates to a pharmaceutical composition containing a compound of Formula 1, a compound of Formula 2 or a combination thereof, for use in treating cancer, wherein the composition is in the form of a tablet or capsule:
Formula 1
,
Formula 2
,
where R1 is -CH2CH2CH2N(CH3)2, and where the tablet or capsule further contains at least one binder, at least one diluent and at least one lubricant, where said binder is selected from polyvinylpyrrolidone, hydroxypropylmethylcellulose or hydroxypropylcellulose, said diluent is selected from microcrystalline cellulose, lactose or mannitol, and said lubricant is selected from talc, magnesium stearate, sodium stearyl fumarate or glyceryl behenate, and also relates to a method of producing a pharmaceutical composition containing a compound of Formula 1, said method comprising steps of: 1) forming a solution of a free base from an alkylcarbamoylnaphthalenyloxyoctenoylhydroxyamide of Formula 1 in a first organic solvent, 2) adding phosphoric acid to the free base solution to form a compound of Formula 1, 3) preparing a compound of Formula 1 with at least one binder, at least one diluent and at least one lubricant, where said binder is selected from polyvinylpyrrolidone, hydroxypropylmethylcellulose or hydroxypropylcellulose, said diluent is selected from microcrystalline cellulose, lactose or mannitol, and said lubricant is selected from talc, magnesium stearate, sodium stearyl fumarate or glyceryl behenate, to obtain a composition, and 4) preparing a pharmaceutical composition in the form of a tablet or capsule by preparing a tablet from said composition using a granulation method, or by granulating said composition of step 3) and filling it into a capsule.
EFFECT: group of inventions provides excellent stability and low hygroscopicity of the compound of Formula 1 and the compound of Formula 2.
7 cl, 8 dwg, 16 tbl
