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Details for Patent: 8,703,202

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Details for Patent: 8,703,202

Title:Coated tablets
Abstract: Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.
Inventor(s): Vachon; Michael (Montreal, CA), Awadhesh; Mishra K. (San Diego, CA), Snow; Robert A. (Westchester, PA), Guivarc'h; Pol-Henri (Paris, FR)
Assignee: Jagotec AG (Muttenz, CH)
Filing Date:Jul 24, 2006
Application Number:11/492,373
Claims:1. A method of treating dyslipidemia and dyslipoproteinemia in a patient comprising administering to a patient an oral dosage form of a pharmaceutical composition having phospholipid surface active substance-stabilized fenofibrate microparticles, said dosage form in the form of a tablet comprising each of the following present in the indicated amounts (w/w of the tablet): about 15% to about 20% fenofibrate; about 1% to about 8% phospholipid; about 0.1% to about 0.5% of a buffer salt; about 7% to about 20% of one or more water-soluble bulking agents selected from maltodextrin and mannitol; about 3% to about 8% of a cellulosic additive present; about 12% to about 16% beads or crystals of a pharmaceutically acceptable water soluble excipient support material; about 5% to about 30% polyvinylpyrrolidone or crospovidone; about 1% to about 6% croscarmellose sodium; about 3% to about 30% granular mannitol; about 1% to about 4% sodium dodecyl sulfate; about 1% silicon dioxide; and about 1% of a stearate; wherein the fenofibrate is in the form of microparticles coated with phospholipid, wherein the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and wherein the surface of the beads or crystals of the pharmaceutically acceptable water-soluble excipient is coated with the matrix.

2. The method of claim 1, wherein the meal contains at least 1000 calories, 50% of which are from fat.

3. The method of claim 1, wherein the quantity of fenofibrate active species provided when fasted is at least 95% of the quantity of fenofibrate active species provided by said amount to said patient when fed.

4. The method of claim 1, wherein the dyslipidemia is selected from the group consisting of hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, and combinations thereof.

5. The method of claim 1, wherein dosage form contains a weight of fenofibrate in the range from 50 mg to 300 mg.

6. The method of claim 1, wherein dosage form contains a weight of fenofibrate selected from the group consisting of 50 mg, 51 mg, 52 mg, 53 mg, 54 mg, 67 mg, 100 mg, 102 mg, 103 mg, 104 mg, 134 mg, 150 mg, 153 mg, 156 mg, 159 mg, 160 mg, 200 mg, 213 mg, 250 mg, and 300 mg of fenofibrate.

7. The method of claim 1, wherein the phospholipid surface active substance is LIPOID E80.

8. The method of claim 1, wherein the phospholipid is selected from the group consisting of saturated phospholipids, unsaturated phospholipids, naturally derived phospholipids, synthetic phospholipids, and semisynthetic phospholipids.

9. The method of claim 1, wherein the phospholipid is selected from the group consisting of egg phospholipid, egg phosphatidylcholine, LIPOID SPC, dimyristoyl phosphatidylglycerol (DMPG), a hydrogenated soybean phosphatidylcholine, a 100% hydrogenated soy phosphatidylcholine, 90% hydrogenated soy phosphatidylcholine, LIPOID SPC-3, egg phospholipid, purified egg phopholipid, and mixtures thereof.

10. The method of claim 1, wherein the dosage form is a capsule or a tablet.

11. The method of claim 1, wherein the dosage form comprises a powder dispersible in water or in a beverage.

12. The method of claim 1, wherein the dosage form further comprises a carbohydrate-derived alcohol.

13. The method of claim 12, wherein the tablet is selected from the group consisting of a film-coated tablet, a moisture resistant tablet, and a tablet coated with a pharmaceutically acceptable polymer.

14. The method of claim 1, wherein the dosage form provides a therapeutically effective level of fenofibrate active species to the patient when fasted that is at least 90% of the quantity of fenofibrate active species provided by the dosage form when fed a meal containing fat.

15. The method of claim 14, wherein the meal contains at least 1000 calories, 50% of which are from fat.

16. The method of claim 14, wherein the quantity of fenofibrate active species provided when fasted is at least 95% of the quantity of fenofibrate active species provided by said amount to said patient when fed.

17. The method of claim 14, wherein the dyslipidemia is selected from the group consisting of hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, and combinations thereof.

18. The method of claim 14, wherein the dosage form contains a weight of fenofibrate in the range from 50 mg to 300 mg.

19. The method of claim 14, wherein dosage form contains a weight of fenofibrate selected from the group consisting of 50 mg, 51 mg, 52 mg, 53 mg, 54 mg, 67 mg, 100 mg, 102 mg, 103 mg, 104 mg, 134 mg, 150 mg, 153 mg, 156 mg, 159 mg, 160 mg, 200 mg, 213 mg, 250 mg, and 300 mg of fenofibrate.

20. The method of claim 14, wherein the phospholipid surface active substance is LIPOID E80.

21. The method of claim 14, wherein the phospholipid is selected from the group consisting of saturated phospholipids, unsaturated phospholipids, naturally derived phospholipids, synthetic phospholipids, and semi synthetic phospholipids.

22. The method of claim 14, wherein the phospholipid is selected from the group consisting of egg phospholipid, egg phosphatidylcholine, LIPOID SPC, dimyristoyl phosphatidylglycerol (DMPG), a hydrogenated soybean phosphatidylcholine, a 100% hydrogenated soy phosphatidylcholine, 90% hydrogenated soy phosphatidylcholine, LIPOID SPC-3, egg phospholipid, purified egg phopholipid, and mixtures thereof.

23. The method of claim 14, wherein the dosage form is a capsule or a tablet.

24. The method of claim 14, wherein the dosage form comprises a powder dispersible in water or in a beverage.

25. The method of claim 14, wherein the dosage form further comprises a bulking agent.

26. The method of claim 14, wherein the dosage form further comprises a carbohydrate-derived alcohol.

27. The method of claim 25, wherein the tablet is selected from the group consisting of a film-coated tablet, a moisture resistant tablet, and a tablet coated with a pharmaceutically acceptable polymer.

28. A pharmaceutical composition comprising phospholipid surface active substance-stabilized fenofibrate microparticles, wherein said compositions is a tablet dosage form and said composition comprising each of the following present in the indicated amounts (w/w of the tablet): about 15% to about 20% fenofibrate; about 1% to about 8% phospholipid; about 0.1% to about 0.5% of a buffer salt; about 7% to about 20% of one or more water-soluble bulking agents selected from maltodextrin and mannitol; about 3% to about 8% of a cellulosic additive present; about 12% to about 16% beads or crystals of a pharmaceutically acceptable water-soluble excipient support material; about 5% to about 30% polyvinylpyrrolidone or crospovidone; about 1% to about 6% croscarmellose sodium; about 3% to about 30% granular mannitol; about 1% to about 4% sodium dodecyl sulfate; about 1% silicon dioxide; and about 1% of a stearate; wherein the fenofibrate is in the form of microparticles coated with phospholipid, wherein the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and wherein the surface of the beads or crystals of the pharmaceutically acceptable water-soluble excipient is coated with the matrix, wherein said composition is prepared by a process comprising (a) mixing at high shear an admixture of fenofibrate and a phospholipid substance in an aqueous carrier in the absence of an organic solvent within a first temperature range at or above the melting point of fenofibrate to form a heated suspension wherein fenofibrate is molten; (b) homogenizing the heated suspension in a first pressure range and within the first temperature range to form a heated homogenate containing fenofibrate; (c) cooling the heated homogenate to a second temperature range below the melting temperature of fenofibrate to form a transiently stable cooled homogenate containing fenofibrate; (d) applying a particle stabilizing energetic process to the cooled homogenate within a second temperature range below the melting temperature of fenofibrate and in a second pressure range to form a cooled dispersion of microparticles containing fenofibrate, and e) drying the cooled dispersion to form dried microparticles containing fenofibrate; and the pharmaceutically acceptable excipient, wherein the pharmaceutical composition provides a therapeutically effective level of fenofibrate active species to the patient when fasted that is at least 90% of the quantity of fenofibrate active species provided by the dosage form when fed a meal containing fat.

29. The pharmaceutical composition of claim 28, containing a weight of fenofibrate in the range from 50 mg to 300 mg.

30. The pharmaceutical composition of claim 28, containing a weight of fenofibrate selected from the group consisting of 50 mg, 51 mg, 52 mg, 53 mg, 54 mg, 67 mg, 100 mg, 102 mg, 103 mg, 104 mg, 134 mg, 150 mg, 153 mg, 156 mg, 159 mg, 160 mg, 200 mg, 213 mg, 250 mg, and 300 mg of fenofibrate.

31. The pharmaceutical composition of claim 28, wherein the phospholipid surface active substance is LIPOID E80.

32. The pharmaceutical composition of claim 28, wherein the phospholipid is selected from the group consisting of saturated phospholipids, unsaturated phospholipids, naturally derived phospholipids, synthetic phospholipids, and semisynthetic phospholipids.

33. The pharmaceutical composition of claim 28, wherein the phospholipid is selected from the group consisting of egg phospholipid, egg phosphatidylcholine, LIPOID SPC, dimyristoyl phosphatidylglycerol (DMPG), a hydrogenated soybean phosphatidylcholine, a 100% hydrogenated soy phosphatidylcholine, 90% hydrogenated soy phosphatidylcholine, LIPOID SPC-3, egg phospholipid, purified egg phopholipid, and mixtures thereof.

34. The pharmaceutical composition of claim 28, further comprising carbohydrate-derived alcohol.

35. The pharmaceutical composition of claim 28, wherein the tablet is selected from the group consisting of a film-coated tablet, a moisture resistant tablet, and a tablet coated with a pharmaceutically acceptable polymer.

36. The method of claim 14, wherein the particle size is <1 .mu.m.
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