Fenofibrate formulation
View Patent ↗Various fenofibrate dosage forms contain a plurality of beads or particles, where the beads or particles include a pharmaceutical composition comprising fenofibrate; from 0.3% to 10% by weight of the beads or particles of a surfactant; and from about 5% to about 15% by weight of the beads or particles of a water soluble or water dispersible cellulosic binder. The mass ratio of the drug to the binder in the dosage form is between about 3.5:1 and 4.5:1; and the dosage form produces a first Cmax in vivo that is between about 10% and about 50% higher than a comparative Cmax produced by a comparative dosage form. The comparative dosage form comprises the drug and the binder in a ratio of between about 5:1 and 15:1.
1. A dosage form comprising a plurality of beads or particles, each of said beads or particles having a coating, said coating comprising:
from 25% to 60% by weight of said beads or particles of a drug selected from the group consisting of fenofibric acid, pharmaceutically acceptable salts thereof, pharmaceutically acceptable esters thereof, and prodrugs thereof;
from 0.3% to 10% by weight of said beads or particles of a surfactant; and
from about 5% to about 15% by weight of said beads or particles of a water soluble or water dispersible cellulosic binder;
wherein the mass ratio of said drug to said binder in said dosage form is between about 3.5:1 and 4.5:1; and
wherein said dosage form produces a first Cmax in vivo that is between about 10% and about 50% higher than a comparative Cmax produced by a comparative dosage form comprising said drug and said binder in a ratio of between about 5:1 and 15:1 and from 1% to 10% by weight of said surfactant;
said dosage form and said comparative dosage form having the same amount of drug.
2. The dosage form according to claim 1 , wherein each of said beads or particles comprises an inert core.
3. The dosage form according to claim 1 , wherein said dosage form produces a first Cmax in vivo that is between about 20% and about 45% higher than a comparative Cmax produced by a comparative dosage form comprising said drug and said binder in a ratio of between about 5:1 and 15:1 and from 1% to 10% by weight of said surfactant.
4. The dosage form according to claim 1 , wherein:
each of said beads or particles comprises 45% to about 55% by weight of said drug; and
said dosage form produces said first Cmax in vivo that is between about 10% and about 30% higher than said comparative Cmax.
5. The dosage form according to claim 1 , wherein:
each of said beads or particles comprises 25% to about 35% by weight of said drug; and
said dosage form produces said first Cmax in vivo that is between about 35% and about 50% higher than said comparative Cmax.
6. The dosage form according to claim 1 , wherein said plurality of beads or Particles includes a plurality of first beads or first particles, and a plurality of second beads or second particles;
each of said first beads or first particles comprising from about 45% to about 55% by weight of said drug, where the mass ratio of said drug to said binder in said first beads or first particles is between about 3.5:1 and 4.5:1; and
each of said second beads or second particles comprising from about 25% to about 35% by weight of said drug, where the mass ratio of said drug to said binder in said second beads or second particles is between about 3.5:1 and 4.5:1;
wherein said dosage form produces said first Cmax in vivo that is between about 20% and about 40% higher than said comparative Cmax.
7. The dosage form according to claim 4 , wherein:
said dosage form and said comparative dosage form each comprise 130 mg fenofibrate; and
said first Cmax is between about 4900 ng/mL and about 5800 ng/mL.
8. The dosage form according to claim 5 , wherein:
said dosage form and said comparative dosage form each comprise 130 mg fenofibrate; and
said first Cmax is between about 5400 ng/mL and about 7200 ng/mL.
9. A dosage form comprising a plurality of beads or particles, said beads or particles comprising a pharmaceutical composition comprising:
from about 20% to about 55% by weight of said beads or particles of a drug selected from the group consisting of fenofibric acid, pharmaceutically acceptable salts thereof, pharmaceutically acceptable esters thereof, and prodrugs thereof;
from 0.3% to 10% by weight of said beads or particles of a surfactant; and
from about 5% to about 15% by weight of said beads or particles of a water soluble or water dispersible cellulosic binder; and
wherein said dosage form produces a first Cmax in vivo that is between about 10% and about 50% higher than a comparative Cmax produced by a comparative dosage form comprising from about 60% to 70% by weight of said drug, from about 5% to about 15% by weight of said water soluble or water dispersible cellulosic binder, and from 1% to 10% by weight of said surfactant;
said dosage form and said comparative dosage form having the same amount of drug.
10. The dosage form according to claim 9 , wherein:
said pharmaceutical composition comprises 45% to about 55% by weight of said drug; and
said dosage form produces said first Cmax in vivo that is between about 10% and about 30% higher than said comparative Cmax.
11. The dosage form according to claim 9 , wherein:
said pharmaceutical composition comprises 25% to about 35% by weight of said drug; and
said dosage form produces said first Cmax in vivo that is between about 35% and about 50% higher than said comparative Cmax.
12. The dosage form according to claim 10 , wherein:
said dosage form and said comparative dosage form each comprise 130 mg fenofibrate; and
said first Cmax is between about 4900 ng/mL and about 5800 ng/mL.
13. The dosage form according to claim 11 , wherein:
said dosage form and said comparative dosage form each comprise 130 mg fenofibrate; and
said first Cmax is between about 5400 ng/mL and about 7200 ng/mL.
14. A dosage form comprising a plurality of beads or particles, said beads or particles comprising a pharmaceutical composition comprising:
from about 20% to about 55% by weight of a drug selected from the group consisting of fenofibric acid, pharmaceutically acceptable salts thereof, pharmaceutically acceptable esters thereof, and prodrugs thereof;
from 0.3% to 10% by weight of said beads or particles of a surfactant; and
from about 5% to about 15% by weight of a water soluble or water dispersible cellulosic binder;
wherein the mass ratio of said drug to said binder in said dosage form is between about 3.5:1 and 4.5:1.
15. A method of reducing a cholesterol level in a patient at risk of cardiovascular disease, comprising administering a dosage form according to claim 1 to said patient.
16. The method of claim 15 , wherein said dosage form is administered in conjunction with a statin.
17. A method of increasing high-density lipoprotein levels in a patient at risk of cardiovascular disease, comprising administering a dosage form according to claim 1 to said patient.
18. The method of claim 17 , wherein said dosage form is administered in conjunction with a statin.