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Claims for Patent: 8,124,125

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Claims for Patent: 8,124,125

Title:Solid dosage form comprising a fibrate
Abstract: The invention provides stable, solid dosage forms and pharmaceutical compositions in particulate form comprising a fibrate, for example fenofibrate, dissolved in an non-aqueous vehicle in order to ensure improved bioavailability of the active ingredient upon oral administration relative to known fibrate formulations.
Inventor(s): Holm; Per (Vanlose, DK), Norling; Tomas (Lyngby, DK)
Assignee: Veloxis Pharmaceuticals A/S (Horsholm, DK)
Application Number:12/642,563
Patent Claims: 1. A tablet comprising (a) a solid carrier, and (b) fenofibrate in a vehicle, the vehicle comprising poloxamer and a hydrophilic polymer, wherein the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, the weight ratio of fenofibrate to poloxamer is from about 3:1 to about 1:20, the weight ratio of hydrophilic polymer to poloxamer is from about 1:1 to about 5:1, and at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

2. A tablet comprising (a) a solid carrier, and (b) fenofibrate in a vehicle, the vehicle comprising (i) poloxamer and (ii) a water-miscible polar lipid, higher alcohol, glyceryl monooleate, substituted or unsubstituted monoglyceride, substituted or unsubstituted diglyceride, or a mixture thereof, wherein the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, and at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

3. The tablet of claim 1, wherein the vehicle further comprises one or more of polyvinylpyrrolidones, polyvinyl-polyvinylacetate copolymers-(PVP-PVA), polyvinyl alcohol (PVA), PVP polymers, acrylic polymers, polymethacrylic polymers, myristyl alcohol, cellulose derivatives, pectins, cyclodextrins, galactomannans, alginates, carragenates, xanthan gums and mixtures thereof.

4. A tablet comprising (a) a solid carrier, and (b) fenofibrate in a vehicle, the vehicle comprising (i) poloxamer and (ii) polyoxyethylene oxide, polyoxyethylene stearate, poly-epsiloncaprolactone or any mixture thereof, wherein the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, and at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

5. The tablet of claim 1, wherein the poloxamer is poloxamer 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403 or 407.

6. A tablet comprising (a) a solid carrier, and (b) fenofibrate in a vehicle, the vehicle comprising poloxamer 188, wherein the weight ratio of fenofibrate to poloxamer is from about 3:1 to about 1:20, the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, and at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

7. The tablet of claim 1, wherein the poloxamer is poloxamer 407.

8. A tablet comprising fenofibrate in a vehicle, the vehicle comprising poloxamer and a hydrophilic polymer, wherein (i) the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, the weight ratio of fenofibrate to poloxamer is from about 3:1 to about 1:20, and the weight ratio of hydrophilic polymer to poloxamer is from about 1:1 to about 5:1, (ii) the tablet is prepared by (a) spraying a mixture of fenofibrate and poloxamer onto a solid carrier, and (b) forming a tablet form the product of step (a), and (iii) at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

9. A tablet comprising fenofibrate in a vehicle, the vehicle comprising (i) poloxamer and (ii) a water-miscible polar lipid, higher alcohol, glyceryl monooleate, substituted or unsubstituted monoglyceride, substituted or unsubstituted diglyceride, or a mixture thereof, wherein (i) the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, (ii) the tablet is prepared by (a) spraying a mixture of fenofibrate and vehicle onto a solid carrier, and (b) forming a tablet form the product of step (a), and (iii) at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

10. The tablet of claim 8, wherein the mixture further comprises one or more of polyvinylpyrrolidones, polyvinyl-polyvinylacetate copolymers-(PVP-PVA), polyvinyl alcohol (PVA), PVP polymers, acrylic polymers, polymethacrylic polymers, myristyl alcohol, cellulose derivatives, pectins, cyclodextrins, galactomannans, alginates, carragenates, xanthan gums and mixtures thereof.

11. A tablet comprising fenofibrate in a vehicle, the vehicle comprising (i) poloxamer and (ii) polyoxyethylene oxide, polyoxyethylene stearate, poly epsiloncaprolactone or any mixture thereof, wherein (i) the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, (ii) the tablet is prepared by (a) spraying a mixture of fenofibrate and vehicle onto a solid carrier, and (b) forming a tablet form the product of step (a), and (iii) at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

12. A tablet comprising fenofibrate in a vehicle, the vehicle comprising poloxamer 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403 or 407, wherein (i) the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, (ii) the tablet is prepared by (a) spraying a mixture of fenofibrate and poloxamer onto a solid carrier, and (b) forming a tablet form the product of step (a), (iii) the weight ratio of fenofibrate to poloxamer is from about 3:1 to about 1:20, and (iv) at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

13. The tablet of claim 8, wherein the poloxamer is poloxamer 188.

14. The tablet of claim 8, wherein the poloxamer is poloxamer 407.

15. A method of reducing total cholesterol (total-C), LDL-C, apo-lipoprotein B, or total triglycerides in a patient in need thereof, the method comprising orally administering a tablet comprising (a) a solid carrier, and (b) fenofibrate in a vehicle, the vehicle comprising poloxamer and a hydrophilic polymer, wherein the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, the weight ratio of fenofibrate to poloxamer is from about 3:1 to about 1:20, the weight ratio of hydrophilic polymer to poloxamer is from about 1:1 to about 5:1, and at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.

16. The tablet of claim 3, where the cellulose derivatives are selected from hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), methylcellulose, sodium carboxymethylcellulose, hydroxyethyl cellulose, and combinations thereof.

17. The tablet of claim 10, where the cellulose derivatives are selected from hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), methylcellulose, sodium carboxymethylcellulose, hydroxyethyl cellulose, and combinations thereof.

18. The tablet of claim 12, wherein the poloxamer is poloxamer 188.

19. A method of reducing total cholesterol (total-C), LDL-C, apo-lipoprotein B, or total triglycerides in a patient in need thereof, the method comprising orally administering a tablet comprising (a) a solid carrier, and (b) fenofibrate in a vehicle, the vehicle comprising poloxamer 188, wherein the weight ratio of fenofibrate to poloxamer is from about 3:1 to about 1:20, the tablet comprises 10 to 35% by weight of fenofibrate, based upon 100% total weight of the fenofibrate and vehicle, and at least 75% of the fenofibrate is released within about 45 minutes when tested according to Ph. Eur. Dissolution test (paddle) employing water with 0.75% sodium lauryl sulfate as the dissolution medium and at 50 rpm and a temperature of about 37.degree. C.
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