EXTENDED RELEASE PHARMACEUTICAL COMPOSITIONS

Abstract

The present invention relates to extended release pharmaceutical compositions comprising a beta-blocker drug or a pharmaceutically acceptable salt thereof, wherein said composition comprises at least two extended release portions, each portion having an in vitro dissolution profile that is different from another portion.

Description

Claims

1. A pharmaceutical dosage form comprising a plurality of particles containing a drug substance and having an extended drug release profile, and at least one other plurality of particles containing the drug substance and having a different extended drug release profile.

2. The pharmaceutical dosage form of claim 1, which is in the form of a compressed solid.

3. The pharmaceutical dosage form of claim 1, which is in the form of a capsule containing a plurality of particles.

4. The pharmaceutical dosage form of claim 1, wherein a drug substance comprises a beta-adrenergic receptor blocking agent.

5. The pharmaceutical dosage form of claim 1, wherein a drug substance comprises propranolol or a salt thereof.

6. A pharmaceutical dosage form comprising a plurality of first particles containing a drug substance and having an extended drug release profile, and a plurality of second particles containing the drug substance and having an extended drug release profile, drug release profiles of first particles and second particles in a medium being different.

7. The pharmaceutical dosage form of claim 6, which is in the form of a compressed solid.

8. The pharmaceutical dosage form of claim 6, which is in the form of a capsule containing a plurality of particles.

9. The pharmaceutical dosage form of claim 6, wherein a drug substance comprises a beta-adrenergic receptor blocking agent.

10. The pharmaceutical dosage form of claim 6, wherein a drug substance comprises propranolol or a salt thereof.

11. The pharmaceutical dosage form of claim 6, wherein extended release results from providing a coating on particles, a coating being formed from a composition comprising: a hydrophilic substance, a hydrophobic substance, or a mixture thereof; an organic solvent; and water.

12. The pharmaceutical composition of claim 11, wherein first particles and second particles are similar, except for coating thickness.

13. The pharmaceutical dosage form of claim 6, wherein extended release results from providing a coating on particles, a coating being formed from a composition comprising a hydrophilic substance, a hydrophobic substance, an organic solvent, and water.

14. The pharmaceutical composition of claim 13, wherein first particles and second particles are similar, except for coating thickness.

15. A pharmaceutical composition comprising a plurality of particles comprising a salt of propranolol and at least one pharmaceutical excipient, a fraction of particles being coated to obtain an extended propranolol release profile and another fraction of particles being coated to obtain a different extended propranolol release profile.

16. The pharmaceutical composition of claim 15, wherein a pharmaceutical excipient comprises a cellulose.

17. The pharmaceutical composition of claim 15, wherein fractions of particles are coated with a coating composition comprising a hydrophilic polymer, a hydrophobic polymer, an organic solvent, and water, different fractions receiving different amounts of coating composition.

18. The pharmaceutical composition of claim 17, wherein a hydrophilic polymer comprises hydroxypropyl methylcellulose and a hydrophobic polymer comprises ethylcellulose.

19. The pharmaceutical composition of claim 15, wherein particles comprise granulates comprising a cellulose.

20. The pharmaceutical composition of claim 15, in the form of a capsule containing a plurality of particles.

21. A process for preparing a pharmaceutical composition, comprising: forming particles from a solid mixture comprising a salt of propranolol;dividing particles into at least two fractions; andcoating particles with a coating composition comprising a hydrophilic polymer, a hydrophobic polymer, an organic solvent, and water;wherein different fractions of particles are coated with different amounts of coating composition.