DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation
DCFirst Claim
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1. A method of treating type 2 diabetes mellitus comprising orally administering to a patient in need thereof a pharmaceutical composition comprising:
- (a) 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in a dosage of 2.5 mg or 5 mg,(b) metformin hydrochloride,(c) one or more pharmaceutical excipients, and(d) a basic amino acid having an intramolecular amino group and alkaline characteristics, which basic amino acid is present in an amount sufficient to suppress degradation of said 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine,wherein the pharmaceutical composition is a tablet comprising a film-coat; and
wherein the pharmaceutical composition comprises the following amounts;
0.1-0.5% of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, 47-85% of metformin hydrochloride, and 0.07-2.2% of the basic amino acid, wherein each of the foregoing percentage amounts are based on the weight of total coated tablet mass.
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Abstract
The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and a partner drug, processes for the preparation thereof, and their use to treat certain diseases.
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Citations
20 Claims
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1. A method of treating type 2 diabetes mellitus comprising orally administering to a patient in need thereof a pharmaceutical composition comprising:
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(a) 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in a dosage of 2.5 mg or 5 mg, (b) metformin hydrochloride, (c) one or more pharmaceutical excipients, and (d) a basic amino acid having an intramolecular amino group and alkaline characteristics, which basic amino acid is present in an amount sufficient to suppress degradation of said 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, wherein the pharmaceutical composition is a tablet comprising a film-coat; and wherein the pharmaceutical composition comprises the following amounts;
0.1-0.5% of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, 47-85% of metformin hydrochloride, and 0.07-2.2% of the basic amino acid, wherein each of the foregoing percentage amounts are based on the weight of total coated tablet mass. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
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12. A method of treating type 2 diabetes mellitus comprising orally administering to a patient in need thereof a solid pharmaceutical composition which is a mono-layer tablet comprising:
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1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in a dosage of 2.5 mg, metformin hydrochloride, L-arginine in an amount sufficient to suppress degradation of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and one or more fillers and one or more binders, wherein the percentage of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is about 0.2%-0.4%, by weight of total tablet core and, wherein the DPP-4 inhibitor and L-arginine are comprised in a weight ratio of from about 1;
10 to about 10;
1. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19)
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20. A method of achieving glycemic control in a type 2 diabetes patient comprising orally administering to the patient a pharmaceutical composition comprising:
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(a) 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in a dosage of 2.5 mg or 5 mg, (b) metformin hydrochloride, (c) one or more pharmaceutical excipients, and (d) a basic amino acid having an intramolecular amino group and alkaline characteristics, which basic amino acid is present in an amount sufficient to suppress degradation of said 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, wherein the pharmaceutical composition is a tablet comprising a film-coat; and wherein the pharmaceutical composition comprises the following amounts;
0.1-0.5% of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, 47-85% of metformin hydrochloride, and 0.07-2.2% of the basic amino acid, wherein each of the foregoing percentage amounts are based on the weight of total coated tablet mass.
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Specification