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Details for Patent: 7,927,627

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Details for Patent: 7,927,627

Title:Nanoparticulate fibrate formulations
Abstract: The present invention is directed to fibrate compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The fibrate particles of the composition have an effective average particle size of less than about 2000 nm.
Inventor(s): Ryde; Tuula (Malvern, PA), Gustow; Evan E. (Villanova, PA), Ruddy; Stephen B. (Schwenksville, PA), Jain; Rajeev (Collegeville, PA), Patel; Rakesh (Bensalem, PA), Wilkins; Michael John (Midleton, IE)
Assignee: Elan Pharma International, Ltd. (Athlone County, Westmeath, IE) Fournier Laboratories Ireland, Ltd. (Carrigtwohill, County Cork, IE)
Filing Date:May 23, 2007
Application Number:11/802,542
Claims:1. A stable nanoparticulate fibrate composition comprising: (a) particles of a fibrate or a salt thereof having an effective average particle size of less than about 2000 nm; and (b) associated with the surface thereof hypromellose, dioctyl sodium sulfosuccinate, and sodium lauryl sulfate as surface stabilizers; wherein the composition is phospholipid-free.

2. The composition of claim 1, wherein the fibrate is 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester or a salt thereof.

3. A stable nanoparticulate fibrate composition comprising: (a) particles of a fibrate or a salt thereof, wherein the particles have an effective average particle size of less than about 2000 nm; and (b) associated with the surface thereof dioctyl sodium sulfosuccinate and hypromellose.

4. The composition of claim 3, wherein the fibrate is 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester or a salt thereof.

5. The composition of claim 3, further comprising sodium lauryl sulfate.

6. The composition of claim 3, wherein the pharmacokinetic profile of the fibrate or a salt thereof is not affected by the fed or fasted state of a subject ingesting the composition.

7. The composition of claim 3, wherein administration of the composition to a subject in a fasted state is bioequivalent to administration of the composition to a subject in a fed state.

8. A fibrate composition comprising the following: (a) about 50 to about 500 g/kg 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester or a salt thereof; (b) about 10 to about 70 g/kg hypromellose; (c) about 1 to about 10 g/kg docusate sodium; (d) about 100 to about 500 g/kg sucrose; (e) about 1 to about 40 g/kg sodium lauryl sulfate; (f) about 50 to about 400 g/kg lactose monohydrate; (g) about 50 to about 300 g/kg silicified microcrystalline cellulose; (h) about 20 to about 300 g/kg crospovidone; and (i) about 0.5 to about 5 g/kg magnesium stearate.

9. The composition of claim 8, further comprising a coating agent.

10. A fibrate composition comprising the following: (a) about 100 to about 300 g/kg 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester or a salt thereof; (b) about 30 to about 50 g/kg hypromellose; (c) about 0.5 to about 10 g/kg docusate sodium; (d) about 100 to about 300 g/kg sucrose; (e) about 1 to about 30 g/kg sodium lauryl sulfate; (f) about 100 to about 300 g/kg lactose monohydrate; (g) about 50 to about 200 g/kg silicified microcrystalline cellulose; (h) about 50 to about 200 g/kg crospovidone; and (i) about 0.5 to about 5 g/kg magnesium stearate.

11. The composition of claim 10, further comprising a coating agent.

12. A fibrate composition comprising the following: (a) about 200 to about 225 g/kg 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester or a salt thereof; (b) about 42 to about 46 g/kg hypromellose; (c) about 2 to about 6 g/kg docusate sodium; (d) about 200 to about 225 g/kg sucrose; (e) about 12 to about 18 g/kg sodium lauryl sulfate; (f) about 200 to about 205 g/kg lactose monohydrate; (g) about 130 to about 135 g/kg silicified microcrystalline cellulose; (h) about 112 to about 118 g/kg crospovidone; and (i) about 0.5 to about 3 g/kg magnesium stearate.

13. The composition of claim 12, further comprising a coating agent.

14. A fibrate composition comprising the following: (a) about 119 to about 224 g/kg 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester or a salt thereof; (b) about 42 to about 46 g/kg hypromellose; (c) about 2 to about 6 g/kg docusate sodium; (d) about 119 to about 224 g/kg sucrose; (e) about 12 to about 18 g/kg sodium lauryl sulfate; (f) about 119 to about 224 g/kg lactose monohydrate; (g) about 129 to about 134 g/kg silicified microcrystalline cellulose; (h) about 112 to about 118 g/kg crospovidone; and (i) about 0.5 to about 3 g/kg magnesium stearate.

15. The composition of claim 14, further comprising a coating agent.

16. A method of making a nanoparticulate fibrate composition comprising contacting fibrate or a salt thereof particles with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate fibrate composition having an effective average particle size of less than about 2000 nm, wherein said contacting comprises grinding; and wherein the composition is phospholipid-free.

17. The method of claim 16, wherein said grinding comprises wet grinding.

18. A method of making a nanoparticulate fibrate composition comprising contacting fibrate or a salt thereof particles with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate fibrate composition having an effective average particle size of less than about 2000 nm, wherein said contacting comprises: (a) dissolving the particles of a fibrate or a salt thereof in a solvent; (b) adding the resulting fibrate solution to a solution comprising at least one surface stabilizer; and (c) precipitating the solubilized fibrate having at least one surface stabilizer adsorbed on the surface thereof by the addition thereto of a non-solvent; wherein the composition is phospholipid-free.

19. A method of making a nanoparticulate fibrate composition comprising contacting fibrate or a salt thereof particles with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate fibrate composition having an effective average particle size of less than about 2000 nm, wherein the composition comprises hypromellose, dioctyl sodium sulfosuccinate, and sodium lauryl sulfate as surface stabilizers; and wherein the composition is phospholipid-free.

20. A method of treating a subject in need with a nanoparticulate fibrate formulation comprising administering to the subject an effective amount of a nanoparticulate composition comprising particles of a fibrate or a salt thereof having at least one surface stabilizer associated with the surface thereof, wherein the fibrate or a salt thereof particles have an effective average particle size of less than about 2000 nm, wherein the composition comprises hypromellose, dioctyl sodium sulfosuccinate, and sodium lauryl sulfate as surface stabilizers; and wherein the composition is phospholipid-free.
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