TABLETS CONTAINING A 1-(beta-D-GLUCOPYRANOSYL)-3-(PHENYLTHIENYLMETHYL)BENZENE COMPOUND
The present invention is directed to a tablet containing a 1-(β-D-glucopyranosyl)-3-(phenylthienylmethyl)benzene compound in high drug loading, in particular, containing the compound ranging from 30 to 95% by weight of tablet and pharmaceutically acceptable additives.
1 . A tablet comprising a compound of formula (A):
or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of from about 30 to 95% by weight of tablet.
2 . The tablet according to claim 1 , wherein a pharmaceutically acceptable salt of compound (A) is hemihydrate of compound (A).
3 . The tablet according to claim 1 , wherein the pharmaceutically acceptable additives comprises a bulking agent (a filler), a binder, a disintegrant, and a lubricant.
4 . The tablet of claim 3 , wherein a) compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of from 30 to 95% by weight of tablet; b) the bulking agent (the filler) is present in an amount within the range of from about 0 to 70% by weight of tablet; c) the binder is present in an amount within the range of from about 1 to 25% by weight of tablet; d) the disintegrant is present in an amount within the range of from about 1 to 25% by weight of tablet; and e) the lubricant is present in an amount within the range of from about 0.25 to 20% by weight of tablet.
5 . The tablet of claim 3 , wherein a) compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of from 50 to 90% by weight of tablet; b) the bulking agent or filler is present in an amount within the range of from about 5 to 15% by weight of tablet; c) the binder is present in an amount within the range of from about 1 to 5% by weight of tablet; d) the disintegrant is present in an amount within the range of from about 1. to 5% by weight of tablet; and e) the lubricant is present in an amount within the range of from about 1 to 10% by weight of tablet.
6 . The tablet according to claim 1 , wherein compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of 65% to 90% by weight of the tablet.
7 . The tablet of claim 3 , wherein compound (A) or a pharmaceutically acceptable salt thereof is present in an amount of 70±2% by weight of tablet; the bulking agent or filler is present in an amount of 12±2% by weight of tablet; the binder is present in an amount of 3±1% by weight of tablet; the disintegrant is present in an amount of 4±1% by weight of tablet;
and the lubricant is present in an amount of 4±2% by weight of tablet.
8 . The tablet of claim 6 , which further comprises a coating agent in an amount within the range of from 3 to 10% by weight of tablet.
9 . The tablet of claim 3 , wherein the lubricant is talc and sodium stearyl fumarate.
10 . The tablet according to claim 1 , wherein a) compound (A) hemihydrate is present in an amount of about 204 mg; b) D-mannitol is present in an amount of about 36 mg; c) hydroxypropyl cellulose is present in an amount of about 8 mg; d) croscarmellose sodium is present in an amount of about 11.2 mg; e) talc is present in an amount of about 2.8 mg; and f) sodium stearyl fumarate is present in an amount of about 8 mg.
11 . The tablet according to claim 1 , wherein a) compound (A) hemihydrate is present in an amount of about 102 mg; b) D-mannitol is present in an amount of about 18 mg; c) hydroxypropyl cellulose is present in an amount of about 4 mg; d) croscaimellose sodium is present in an amount of about 5.6 mg; e) talc is present in an amount of about 1.4 mg; and f) sodium stearyl fumarate is present in an amount of about 4 mg.
12 . Use of the tablet of claim 1 for treating or delaying the progression or onset of diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids, elevated blood levels of glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, atherosclerosis, or hypertension.
13 . Use of the tablet of claim 1 for treating or delaying the progression or onset of type II diabetes or obesity.
14 . Use of the tablet of claim 1 for treating or delaying the progression or onset of diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids, elevated blood levels of glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, atherosclerosis, or hypertension, whereby optionally an anti-diabetic agent, an anti-hyperglycemic agent, a hypolipidemic or lipid lowering agent, an anti-obesity agent, an anti-hypertensive agent, or an appetite suppressant is to be administered in combination.
15 . A method for treatment or delaying the progression or onset of diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids, elevated blood levels of glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, diabetic complications, atherosclerosis, or hypertension, which comprises administering to a mammalian species in need of treatment a therapeutically effective amount of the tablet as set forth in claim 1 .
16 . A method for treatment of type 1 or type 2 diabetes mellitus, which comprises administering to a mammalian species in need of treatment a therapeutically effective amount of the tablet as set forth in claim 1 alone, or in combination with another antidiabetic agent, an agent for treating diabetic complications, an anti-obesity agent, an anti-hypertensive agent, an anti-platelet agent, an anti-atherosclerotic agent and/or a hypolipidemic agent.
17 . The tablet of claim 1 for treating or delaying the progression or onset of diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids, elevated blood levels of glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, atherosclerosis, or hypertension.
18 . The tablet according to claim 2 , wherein compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of 65% to 90% by weight of the tablet.
19 . The tablet according to claim 3 , wherein compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of 65% to 90% by weight of the tablet.
20 . The tablet according to claim 4 , wherein compound (A) or a pharmaceutically acceptable salt thereof is present in an amount within the range of 65% to 90% by weight of the tablet.