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Claims for Patent: 6,340,695

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Claims for Patent: 6,340,695

Title: Rapid onset formulation
Abstract:Provided herein is a novel enterically-coated pyridoxine HCl and doxylamine succinate rapid onset formulation comprising a disintegrating agent such that the following dissolution profiles are satisfied when measured in 1000 ml phosphate buffer at pH 6.8 and 37.degree. C. in a type 2 dissolution apparatus at 100 rpm: (a) at least about 40% of the total pyridoxine HCl and doxylamine succinate is dissolved after 30 minutes of measurement; (b) at least about 70% of the total pyridoxine HCl and doxylamine succinate is dissolved after 60 minutes of measurement; (c) at least about 80% of the total pyridoxine HCl and doxylamine succinate is dissolved after 90 minutes of measurement; (d) at about 90% of the total pyridoxine HCl and doxylamine succinate is dissolved after 120 minutes of measurement. Preferably the formulation will contain a core coated with at least one enteric coating, the core comprising pyridoxine HCl, doxylamine succinate and the following non-active excipients: a filler or binder, a disintegrating agent, a lubricant, a silica flow conditioner and a stabilizing agent.
Inventor(s): Gervais; Eric (Laval, CA)
Assignee: Duchesnay Inc. (Laval, CA)
Application Number:09/885,051
Patent Claims: 1. An enterically-coated pyridoxine HCl and doxylamine succinate rapid onset formulation comprising a disintegrating agent such that the following dissolution profiles are satisfied when measured in 1000 ml phosphate buffer at pH 6.8 and 37.degree. C. in a type 2 dissolution apparatus at 100 rpm:

(a) at least about 40% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 30 minutes of measurement;

(b) at least about 70% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 60 minutes of measurement;

(c) at least about 80% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 90 minutes of measurement;

(d) at least about 90% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 120 minutes of measurement.

2. An enterically-coated pyridoxine HCl and doxylamine succinate rapid onset formulation as in claim 1, wherein the following dissolution characteristics are also satisfied when measured in 1000 ml phosphate buffer at pH 6.8 and 37.degree. C. in a type 2 dissolution apparatus at 100 rpm:

(a) at least about 20% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 15 minutes of measurement;

(b) at least about 60% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 45 minutes of measurement;

(c) at least about 80% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved after 75 minutes of measurement.

3. The rapid onset formulation of claim 1, wherein at least about 40% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved within 5 minutes when measured in 1000 ml phosphate buffer at pH 6.8 and 37.degree. C. in a type 2 dissolution apparatus at 100 rpm.

4. The rapid onset formulation of claim 2, wherein at least about 40% of the total amounts of each of pyridoxine HCl and doxylamine succinate are dissolved within 5 minutes when measured in 1000 ml phosphate buffer at pH 6.8 and 37.degree. C. in a type 2 dissolution apparatus at 100 rpm.

5. The rapid onset formulation of claim 1, wherein said formulation contains a core coated with at least one enteric coating, said core comprising pyridoxine HCl, doxylamine succinate and the following non-active excipients: a filler or binder, a disintegrating agent, a lubricant, a silica flow conditioner and a stabilizing agent.

6. The rapid onset formulation of claim 2, wherein said formulation contains a core coated with at least one enteric coating, said core comprising pyridoxine HCl, doxylamine succinate and the following non-active excipients: a filler or binder, a disintegrating agent, a lubricant, a silica flow conditioner and a stabilizing agent.

7. The rapid onset formulation of claim 5, wherein said filler or binder consists of microcrystalline cellulose.

8. The rapid onset formulation of claim 6, wherein said filler or binder consists of microcrystalline cellulose.

9. The rapid onset formulation of claim 5, wherein said disintegrating agent consists of sodium crosscarmellose.

10. The rapid onset formulation of claim 6, wherein said disintegrating agent consists of sodium crosscarmellose.

11. The rapid onset formulation of claim 5, wherein said lubricant consists of magnesium stearate.

12. The rapid onset formulation of claim 6, wherein said lubricant consists of magnesium stearate.

13. The rapid onset formulation of claim 5, wherein said silica flow conditioner consists of silicon dioxide.

14. The rapid onset formulation of claim 6, wherein said silica flow conditioner consists of silicon dioxide.

15. The rapid onset formulation of claim 5, wherein said stabilizing agent consists of magnesium trisilicate.

16. The rapid onset formulation of claim 6, wherein said stabilizing agent consists of magnesium trisilicate.

17. The rapid onset formulation of claim 1, wherein said core comprises:

(a) about 4-10% by weight of pyridoxine HCl;

(b) about 4-10% by weight of doxylamine succinate;

(c) about 40-80% by weight of microcrystalline cellulose;

(d) about 10-30% by weight of magnesium trisilicate;

(e) about 0.5-5% by weight of silicon dioxide;

(f about 0.5-5% by weight of sodium croscarmellose; and

(g) about 0.5-5% by weight of magnesium stearate.

18. The rapid onset formulation of claim 2, wherein said core comprises:

(a) about 4-10% by weight of pyridoxine HCl;

(b) about 4-10% by weight of doxylamine succinate;

(c) about 40-80% by weight of microcrystalline cellulose;

(d) about 10-30% by weight of magnesium trisilicate;

(e) about 0.5-5% by weight of silicon dioxide;

(f) about 0.5-5% by weight of sodium croscarmellose; and

(g) about 0.5-5% by weight of magnesium stearate.

19. The rapid onset formulation of claim 17, wherein said core comprises:

(a) about 7% by weight of pyridoxine HCl;

(b) about 7% by weight of doxylamine succinate;

(c) about 62% by weight of microcrystalline cellulose;

(d) about 18% by weight of magnesium trisilicate;

(e) about 1% by weight of silicon dioxide;

(f) about 3% by weight of sodium croscarmellose; and

(g) about 3% by weight of magnesium stearate.

20. The rapid onset formulation of claim 18, wherein said core comprises:

(a) about 7% by weight of pyridoxine HCl;

(b) about 7% by weight of doxylamine succinate;

(c) about 62% by weight of microcrystalline cellulose;

(d) about 18% by weight of magnesium trisilicate;

(e) about 1% by weight of silicon dioxide;

(f) about 3% by weight of sodium croscarmellose; and

(g) about 3% by weight of magnesium stearate.

21. The rapid onset formulation of claim 5, wherein said enteric coating(s) is (are) aqueous based.

22. The rapid onset formulation of claim 6, wherein said enteric coating(s) is (are) aqueous based.

23. The rapid onset formulation of claim 21, wherein said enteric coating consists of a seal coat applied to the core, an enteric coating per se applied on the seal coat and an aesthetic top coat applied on the enteric coating per se.

24. The rapid onset formulation of claim 22, wherein said enteric coating consists of a seal coat applied to the core, an enteric coating per se applied on the seal coat and an aesthetic top coat applied on the enteric coating per se.

25. A method of treating nausea and vomiting comprising administering a therapeutically effective amount of the rapid onset formulation of claim 1 to a patient in need thereof.

26. A method of treating nausea and vomiting comprising administering a therapeutically effective amount of the rapid onset formulation of claim 2 to a patient in need thereof.

27. A method of treating nausea and vomiting during pregnancy comprising administering a therapeutically effective amount of the rapid onset formulation of claim 1.

28. A method of treating nausea and vomiting during pregnancy comprising administering a therapeutically effective amount of the rapid onset formulation of claim 2.

29. A medicament for attenuating the symptoms associated with nausea and vomiting consisting essentially of the formulation of claim 5.

30. A medicament for attenuating the symptoms associated with nausea and vomiting consisting essentially of the formulation of claim 6.
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