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Claims for Patent: 8,361,972

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Claims for Patent: 8,361,972

Title:Pharmaceutical formulations containing an SGLT2 inhibitor
Abstract: Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate ##STR00001## and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release.
Inventor(s): Bindra; Dilbir S. (New Brunswick, NJ), Dali; Mandar V. (New Brunswick, NJ), Parab; Prakash V. (New Brunswick, NJ), Patel; Jatin M. (New Brunswick, NJ), Tao; Li (New Brunswick, NJ), Tejwani; Ravindra W. (New Brunswick, NJ), Vatsaraj; Nipa (New Brunswick, NJ), Wu; Yongmei (New Brunswick, NJ)
Assignee: Bristol Myers-Squibb Company (Princeton, NJ)
Application Number:13/529,463
Patent Claims: 1. A method for treating or delaying the progression or onset of Type I and Type II diabetes, impaired glucose tolerance, insulin resistance, nephropathy, retinopathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hypercholesterolemia, dyslipidemia, elevated blood levels of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, hypertension, or Syndrome X (Metabolic Syndrome) comprising administering to a mammalian subject or patient in need of such treatment a therapeutically effective amount of an immediate release pharmaceutical formulation comprising dapagliflozin propylene glycol hydrate and a pharmaceutically acceptable carrier, wherein the dapagliflozin propylene glycol hydrate formulation is in a form selected from the group consisting of a tablet, a stock granulation, and a capsule, wherein the dapagliflozin propylene glycol hydrate is present in an amount to provide a daily dose within the range of from about 0.1 to about 750 mg per day in single or divided doses or multiple doses, which is administered 1 to 4 times, wherein the dapagliflozin propylene glycol hydrate is present in an amount within the range of from 0.1% to 70% of tablet or capsule fill; and the pharmaceutically acceptable carrier comprises: one or more bulking agents/binders in an amount within the range of from 1% to 95% by weight of tablet or capsule fill, the one or more bulking agents/binders comprising one or more of anhydrous lactose in an amount within the range of 0% to 95% by weight of tablet or capsule fill, microcrystalline cellulose in an amount within the range of 0% to 95% by weight of tablet or capsule fill, and pregelatinized starch in an amount within the range of 0 to 95% by weight of tablet or capsule fill; one or more disintegrants in an amount within the range of from 0% to 20% by weight of tablet or capsule fill, the one or more disintegrants comprising one or more of croscarmellose sodium in an amount within the range of 0% to 20% by weight of tablet or capsule fill, crospovidone in an amount within the range of 0% to 12% by weight of tablet or capsule fill, and sodium starch glycolate in an amount within the range of 0% to 20% by weight of tablet or capsule fill; one or more glidants and/or anti-adherents comprising one or more of talc and silicon dioxide in an amount within the range from 0% to 10% by weight of tablet or capsule fill; and one or more lubricants comprising magnesium stearate in an amount within the range of 0.1% to 5% by weight of tablet or capsule fill.

2. The method according to claim 1, wherein the dapagliflozin propylene glycol hydrate is ##STR00018##

3. The method according to claim 1, wherein the formulation is in capsule form.

4. The method according to claim 1, wherein the formulation is in tablet form.

5. The method according to claim 1, wherein the formulation comprises: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount within the range of from about 0.1% to about 30% by weight of tablet or capsule fill; b) bulking agents in a total amount within the range of from about 10% to about 85% by weight of tablet or capsule fill comprising one or more of lactose present in an amount within the range of from about 20% to about 75% by weight of tablet or capsule fill, and microcrystalline cellulose present in an amount within the range of from about 20% to about 75% by weight of tablet or capsule fill; c) a binder comprising pregelatinized starch present in an amount within the range of from about 10% to about 75% by weight of tablet or capsule fill; d) disintegrants in a total amount within the range of from about 2% to about 10% by weight of tablet or capsule fill, comprising one or more of croscarmellose sodium present in an amount within the range of from about 2% to about 10% by weight of tablet or capsule fill, crospovidone present in an amount within the range of from about 4% to about 10% by weight of tablet or capsule fill, and sodium starch glycolate present in an amount within the range of from about 2% to about 10% by weight of tablet or capsule fill; e) one or more glidants and/or anti-adherents comprising talc and/or silicon dioxide, wherein the total amount of glidant and/or anti-adherent is present in an amount within the range of from about 1% to about 10% by weight of tablet or capsule fill; f) a lubricant comprising magnesium stearate present in an amount within the range of from about 0.2% to about 2% by weight of tablet or capsule fill; and g) optionally further comprises an outer protective coating layer comprising a coating polymer and optionally comprising one or more of the following: a plasticizer(s), anti-tacking agent(s), glidant(s), and colorant(s), wherein the total amount of the outer protective coating layer is present in an amount within the range of from about 1% to about 5% by weight of tablet or capsule fill.

6. The method according to claim 1, wherein the formulation is in capsule form, wherein the capsule is filled with a stock granulation comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 10% by weight of capsule fill; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of 68.75% by weight of capsule fill; c) pregelatinized starch, wherein the pregelatinized starch is present in an amount of 15% by weight of capsule fill; d) sodium starch glycolate, wherein the sodium starch glycolate is present in an amount of 3% by weight of capsule fill; e) silicon dioxide, wherein the silicon dioxide is present in an amount of 2% by weight of capsule fill; and f) magnesium stearate, wherein the magnesium stearate is present in an amount of 1.25% by weight of capsule fill.

7. The method according to claim 1, wherein the formulation is in capsule form, wherein the capsule is filled with a stock granulation comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 22.8% by weight of capsule fill; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of 55.95% by weight of capsule fill; c) pregelatinized starch, wherein the pregelatinized starch is present in an amount of 15% by weight of capsule fill; d) sodium starch glycolate, wherein the sodium starch glycolate is present in an amount of 3% by weight of capsule fill; e) silicon dioxide, wherein the silicon dioxide is present in an amount of 2% by weight of capsule fill; and f) magnesium stearate, wherein the magnesium stearate is present in an amount of 1.25% by weight of capsule fill.

8. The method according to claim 1, wherein the formulation is in the form of a 2.5 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 3.08 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of 67.11 mg; c) anhydrous lactose, wherein the anhydrous lactose is present in an amount of 25 mg; d) crospovidone, wherein the crospovidone is present in an amount of 8.75 mg; e) croscarmellose sodium, wherein the croscarmellose sodium is present in an amount of 3.75 mg; f) talc, wherein the talc is present in an amount of 12.5 mg; g) silicon dioxide, wherein the silicon dioxide is present in an amount of 2.88 mg; and h) magnesium stearate, wherein the magnesium stearate is present in an amount of 1.94 mg.

9. The method according to claim 1, wherein the formulation is in the form of a 10 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 12.3 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of 57.89 mg; c) anhydrous lactose, wherein the anhydrous lactose is present in an amount of 25 mg; d) crospovidone, wherein the crospovidone is present in an amount of 8.75 mg; e) croscarmellose sodium, wherein the croscarmellose sodium is present in an amount of 3.75 mg; f) talc, wherein the talc is present in an amount of 12.5 mg; g) silicon dioxide, wherein the silicon dioxide is present in an amount of 2.88 mg; and h) magnesium stearate, wherein the magnesium stearate is present in an amount of 1.94 mg.

10. The method according to claim 1, wherein the formulation is in the form of a 50 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 61.66 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of 114.09 mg; c) anhydrous lactose, wherein the anhydrous lactose is present in an amount of 62.6 mg; d) crospovidone, wherein the crospovidone is present in an amount of 21.91 mg; e) croscarmellose sodium, wherein the croscarmellose sodium is present in an amount of 9.39 mg; f) talc, wherein the talc is present in an amount of 31.3 mg; g) silicon dioxide, wherein the silicon dioxide is present in an amount of 7.2 mg; and h) magnesium stearate, wherein the magnesium stearate is present in an amount of 4.85 mg.

11. The method according to claim 1, wherein the formulation comprises: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount within the range of from about 0.1% to about 15% by weight of tablet or capsule fill; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount sufficient to make the total weight of the tablet or capsule fill 100%; c) lactose, wherein the lactose is present in an amount within the range of from about 10% to about 30% by weight of tablet or capsule fill; d) crospovidone, wherein the crospovidone is present in an amount within the range of from about 3% to about 10% by weight of tablet or capsule fill; e) silicon dioxide, wherein the silicon dioxide is present in an amount within the range of from about 0.5% to about 4% by weight of tablet or capsule fill; and f) magnesium stearate, wherein the magnesium stearate is present in an amount within the range of from about 0.5% to about 2% by weight of tablet or capsule fill.

12. The method according to claim 1, wherein said formulation is in the form of a 1.0 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 1.23 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of about 50 mg to about 90 mg; c) lactose, wherein the lactose is present in an amount of about 10 mg to about 30 mg; d) crospovidone, wherein the crospovidone is present in an amount of about 2 mg to about 10 mg; e) silicon dioxide, wherein the silicon dioxide is present in an amount of about 0.5 mg to about 4.0 mg; f) magnesium stearate, wherein the magnesium stearate is present in an amount of about 0.5 mg to about 2.0 mg; and g) an antioxidant and/or chelating agent, wherein the antioxidant and/or chelating agent is present in an amount of about 0 mg to about 0.5 mg.

13. The method according to claim 1, wherein said formulation is in the form of a 2.5 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 3.075 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of about 60 mg to about 115 mg; c) lactose, wherein the lactose is present in an amount of about 12.5 mg to about 38 mg; d) crospovidone, wherein the crospovidone is present in an amount of about 2.5 mg to about 13 mg; e) silicon dioxide, wherein the silicon dioxide is present in an amount of about 0.6 mg to about 5.0 mg; f) magnesium stearate, wherein the magnesium stearate is present in an amount of about 0.6 mg to about 2.5 mg; and g) an antioxidant and/or chelating agent, wherein the antioxidant and/or chelating agent is present in an amount of about 0 mg to about 0.6 mg.

14. The method according to claim 1, wherein said formulation is in the form of a 5.0 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 6.15 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of about 60 mg to about 115 mg; c) lactose, wherein the lactose is present in an amount of about 12.5 mg to about 38 mg; d) crospovidone, wherein the crospovidone is present in an amount of about 2.5 mg to about 13 mg; e) silicon dioxide, wherein the silicon dioxide is present in an amount of about 0.6 mg to about 5.0 mg; f) magnesium stearate, wherein the magnesium stearate is present in an amount of about 0.6 mg to about 2.5 mg; and g) an antioxidant and/or chelating agent, wherein the antioxidant and/or chelating agent is present in an amount of about 0 mg to about 0.6 mg.

15. The method according to claim 1, wherein said formulation is in the form of a 10 mg dapagliflozin dose tablet comprising: a) dapagliflozin propylene glycol hydrate, wherein the dapagliflozin propylene glycol hydrate is present in an amount of 12.3 mg; b) microcrystalline cellulose, wherein the microcrystalline cellulose is present in an amount of about 120 mg to about 230 mg; c) lactose, wherein the lactose is present in an amount of about 25 mg to about 75 mg; d) crospovidone, wherein the crospovidone is present in an amount of about 5 mg to about 25 mg; e) silicon dioxide, wherein the silicon dioxide is present in an amount of about 1.0 mg to about 10 mg; f) magnesium stearate, wherein the magnesium stearate is present in an amount of about 1.0 mg to about 5 mg; and g) an antioxidant and/or chelating agent, wherein the antioxidant and/or chelating agent is present in an amount of about 0 mg to about 1.25 mg.

16. A method according to claim 1, wherein the method is for treating or delaying the progression or onset of Type II diabetes.

17. A method according to claim 2, wherein the method is for treating or delaying the progression or onset of Type II diabetes.

18. A method according to claim 11, wherein the method is for treating or delaying the progression or onset of Type II diabetes.

19. A method according to claim 1, further comprising administering to the mammalian subject or patient in need of such treatment one or more agents selected from the group consisting of anti-diabetic agents, anti-hyperglycemic agents, hypolipidemic or lipid lowering agents, anti-obesity agents, anti-hypertensive agents, and appetite suppressants.

20. A method according to claim 19, wherein the method is for treating or delaying the progression or onset of type II diabetes.

21. The method of claim 20, wherein the agents(s) is an anti-diabetic agent(s).

22. A method according to claim 2, wherein the method is for treating or delaying the progression or onset of Type II diabetes, further comprising administering to the mammalian subject or patient in need of such treatment one or more anti-diabetic agents.
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