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Claims for Patent: 6,066,339

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Claims for Patent: 6,066,339

Title: Oral morphine multiparticulate formulation
Abstract:An oral morphine multiparticulate formulation for once-daily administration to a patient, comprising sustained release particles each having a core containing water soluble morphine and an osmotic agent, the core being coated with a rate-controlling polymer coat comprised of ammonio methacrylate copolymers in an amount sufficient to achieve therapeutically effective plasma levels of morphine over at least 24 hours in the patient.
Inventor(s): Stark; Paul (Althone, IE), Cunningham; Sean (Althone, IE), Moodley; Jagathesan (Althone, IE)
Assignee: Elan Corporation, plc (Dublin, IE)
Application Number:08/977,965
Patent Claims: 1. An oral morphine multiparticulate formulation for once-daily administration to a patient, comprising sustained release particles each having a core containing water soluble morphine and an osmotic agent, the core being coated with a rate-controlling polymer coat comprised of ammonia methacrylate copolymers in an amount sufficient to achieve therapeutically effective plasma levels of morphine over at least 24 hours in the patient wherein the said osmotic agent is an organic agent.

2. A formulation according to claim 1, wherein a portion or all of the sustained release particles further comprise an immediate release coating applied onto the rate-controlling polymer coat, which immediate release coating comprises water soluble morphine.

3. A formulation according to claim 1, further comprising a portion of immediate release particles each comprising a core of water soluble morphine.

4. A formulation according to claim 1, which comprises at least two populations of sustained release particles having different in vitro dissolution profiles.

5. A formulation according to claim 1, which releases morphine in vivo following single dose administration such that the duration over which the plasma level of morphine is equal to or greater than 50% of the peak plasma concentration is 20 hours or greater.

6. A formulation according to claim 5, wherein the duration is 24 hours or greater.

7. A formulation according to claim 5, wherein the duration is 30 hours or greater.

8. A formulation according to claim 1, which releases morphine in vivo following single dose administration such that the duration over which the plasma level of morphine is equal to or greater than 75% of the peak plasma concentration is 6 hours or greater.

9. A formulation according to claim 8, wherein the duration is 12 hours or greater.

10. A formulation according to claim 8, wherein the duration is 18 hours or greater.

11. A formulation according to claim 1, which releases morphine in vivo at steady state such that the plasma level of morphine over the 24 hour dosing period is equal to or greater than 50% of the peak plasma concentration.

12. A formulation according to claim 1, which releases morphine in vivo at steady state such that the duration over which the plasma level of morphine over the 24 hour dosing period is equal to or greater than 75% of the peak plasma concentration is 12 hours or greater.

13. A formulation according to claim 1, which provides a dissolution profile in aqueous media such that about 3 to 25% of the water soluble morphine is released after 1 hour; about 5 to 35% is released after 4 hours; about 25 to 65% is released after 9 hours; about 35 to 75% is released after 12 hours and at least 70% is released after 24 hours.

14. A formulation according to claim 1, which provides a dissolution profile in aqueous media such that about 10 to 15% of the water soluble morphine is released after 1 hour; about 15 to 30% is released after 4 hours; about 35 to 50% is released after 9 hours; about 45 to 65% is released after 12 hours and at least 80% is released after 24 hours.

15. A formulation according to claim 1, wherein greater than 80% of the formulation is comprised of sustained release particles.

16. A formulation according to claim 1, wherein the rate-controlling polymer coat contains Ammonio Methacrylate Copolymers as described in USP/NF in a ratio of 5:95.

17. A formulation according to claim 1, wherein the organic acid is selected from fumaric acid, adipic acid, ascorbic acid, citric acid, tartaric acid, lactic acid, malic acid or succinic acid.

18. A formulation according to claim 1, wherein the organic acid is fumaric acid.

19. A formulation according to claim 1, wherein the water soluble morphine and osmotic agent are present in the core in a ratio of 1:1.

20. A formulation according to claim 1, wherein the water soluble morphine is morphine sulfate or a hydrate thereof.

21. A formulation according to claim 1, which has a moisture content of about 3-6% by weight.

22. A formulation according to claim 1, wherein the cores for the sustained release particles are equilibrated at ambient conditions or dried at humidified conditions prior to being coated with the rate-controlling polymer coat so as to obtain a moisture content of about 3-6% by weight.

23. A formulation according to claim 1, wherein the sustained release particles following application of the rate-controlling polymer coat are dried at a temperature of about 40-50.degree. C. and about 30-60% relative humidity.

24. A formulation according to claim 1, which contains between 10 mg and 200 mg of morphine sulfate or the equivalent amount of water soluble morphine.

25. A formulation according to claim 1, which is encapsulated.

26. The formulation according to claim 1, wherein the core comprises an

inert core upon which a blend comprising the water soluble morphine and an osmotic agent is applied.

27. An oral morphine multiparticulate formulation for once-daily administration to a patient, comprising sustained release particles each having a core containing water soluble morphine and an osmotic agent, the core being coated with a rate-controlling polymer coat comprised of ammonia methacrylate copolymers in an amount sufficient to achieve therapeutically effective plasma levels of morphine over at least 24 hours in the patient, wherein the said osmotic agent is an organic acid, wherein the formulation is characterised by a rapid onset of action and a substantially flat morphine plasma profile.
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