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Claims for Patent: 8,562,980

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Claims for Patent: 8,562,980

Title:Stable digestive enzyme compositions
Abstract: Compositions of the present invention, comprising at least one digestive enzyme (e.g., pancrelipase) are useful for treating or preventing disorders associated with digestive enzyme deficiencies. The compositions of the present invention can comprise a plurality of coated particles, each of which is comprised of a core coated with an enteric coating comprising at least one enteric polymer and 4-10% of at least one alkalinizing agent, or have moisture contents of about 3% or less, water activities of about 0.6 or less, or exhibit a loss of activity of no more than about 15% after six months of accelerated stability testing.
Inventor(s): Ortenzi; Giovanni (Monza, IT), Marconi; Marco (Cinisello Balsamo, IT), Mapelli; Luigi (Milan, IT)
Assignee: Aptalis Pharma Limited (Wicklow, IE)
Application Number:13/019,856
Patent Claims: 1. A pharmaceutical composition comprising a plurality of coated particles, said coated particles comprising a core comprising at least one digestive enzyme, coated with an enteric coating; wherein the enteric coating comprises: 10-20 wt. % of at least one enteric polymer; and 4-10 wt. % of talc; wherein each said wt. % is based on the total weight of the coated particles.

2. The pharmaceutical composition of claim 1, wherein the coated particles exhibit a loss of digestive enzyme activity of no more than 25% after six months of accelerated stability testing.

3. The pharmaceutical composition of claim 2, wherein the loss of digestive enzyme activity is no more than 15% after six months of accelerated stability testing.

4. The pharmaceutical composition of claim 2, wherein the loss of digestive enzyme activity is no more than 10% after six months of accelerated stability testing.

5. The pharmaceutical composition of claim 2, wherein the loss of digestive enzyme activity is no more than 8% after six months of accelerated stability testing.

6. The pharmaceutical composition of claim 1, wherein the enteric polymer is selected from the group consisting of cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, shellac, acrylic acid polymers or copolymers, methacrylic acid polymers or copolymers, and methacrylic acid/methylmethacrylate copolymers.

7. The pharmaceutical composition of claim 6, wherein the enteric polymer is hydroxypropylmethylcellulose phthalate.

8. The pharmaceutical composition of claim 1, wherein the core further comprises a stabilizer.

9. The pharmaceutical composition of claim 8, wherein the stabilizer is selected from the group consisting of proline, trehalose, dextran, maltose, sucrose, mannitol, polyols, silica gel, aminoguanidine, pyridoxamine, anhydrous metal salts, magnesium oxide, calcium oxide, aluminum oxide, and mixtures thereof.

10. The pharmaceutical composition of claim 9, wherein the stabilizer is colloidal silicon dioxide.

11. The pharmaceutical composition of claim 1, wherein the core further comprises a binder.

12. The pharmaceutical composition of claim 11, wherein the binder is selected from the group consisting of starches, sugars, lactose, sugar alcohols, xylitol, sorbitol, maltitol, cellulose, microcrystalline cellulose, modified celluloses, hydroxypropylcellulose, carboxymethylcellulose sodium, alginic acid, polyvinyl pyrrolidone, and mixtures thereof.

13. The pharmaceutical composition of claim 12, wherein the binder is microcrystalline cellulose.

14. The pharmaceutical composition of claim 1, wherein the core further comprises a disintegrant.

15. The pharmaceutical composition of claim 14, wherein the disintegrant is selected from the group consisting of dibasic calcium phosphate, dibasic calcium phosphate dihydrate, tribasic calcium phosphate, alginic acid, hydroxypropylcellulose, carboxymethylcellulose calcium, carboxymethylcellulose sodium, cross-linked carboxymethylcellulose sodium, swellable ion exchange resins, alginates, formaldehyde-casein, cellulose, croscarmellose sodium, crospovidone, microcrystalline cellulose, sodium carboxymethyl starch, sodium starch glycolate, starches, corn starch, rice starch, and mixtures thereof.

16. The pharmaceutical composition of claim 15, wherein the disintegrant is croscarmellose sodium.

17. The pharmaceutical composition of claim 1, wherein the core further comprises a plasticizer.

18. The pharmaceutical composition of claim 17, wherein the amount plasticizer ranges from 0.5-1.0 wt. % based on the total weight of the coated particles.

19. The pharmaceutical composition of claim 18, wherein the plasticizer is hydrogenated castor oil.

20. The pharmaceutical composition of claim 1, wherein the core further comprises a stabilizer, a binder, and a disintegrant, wherein the stabilizer is colloidal silicon dioxide, the binder is microcrystalline cellulose, and the disintegrant is croscarmellose sodium, and the enteric coating comprises hydroxypropylmethylcellulose phthalate.

21. The pharmaceutical composition of claim 20, wherein the core further comprises a hydrogenated castor oil.

22. The pharmaceutical composition of claim 1, wherein the digestive enzyme comprises pancrelipase.

23. The pharmaceutical composition of claim 22, wherein the pancrelipase is porcine derived.

24. The pharmaceutical composition of claim 1, wherein the coating further comprises 1-2 wt. % of at least one plasticizer, based on the total weight of the coated particles.

25. The pharmaceutical composition of claim 24, wherein the plasticizer is selected from the group consisting of triacetin, tributyl citrate, tri-ethyl citrate, acetyl tri-n-butyl citrate, diethyl phthalate, dibutyl sebacate, polyethylene glycol, polypropylene glycol, castor oil, acetylated mono-glyceride, acetylated di-glyceride, and mixtures thereof.

26. The pharmaceutical composition of claim 25, wherein the plasticizer is tri-ethyl citrate.

27. The pharmaceutical composition of claim 1, wherein the digestive enzyme comprises protease and lipase having a ratio of protease to lipase activity of about 1.8-6.2.

28. The pharmaceutical composition of claim 27, wherein the ratio of protease to lipase activity is about 2.0-6.1.

29. The pharmaceutical composition of claim 1, wherein the digestive enzyme comprises amylase and lipase having a ratio of amylase to lipase activity of about 1.8-8.2.

30. The pharmaceutical composition of claim 29, wherein the ratio of amylase to lipase activity is about 2.0-8.2.

31. The pharmaceutical composition of claim 1, wherein the digestive enzyme comprises lipase, protease, and amylase having a ratio of lipase:protease:amylase activities ranging from about 1:10:10 to about 10:1:1.

32. A method of treating a disorder associated with digestive enzyme deficiency comprising administering a pharmaceutical composition of claim 1 to a mammal in need thereof.

33. The method of claim 32, wherein the mammal is a human.

34. The method of claim 32, wherein said pharmaceutical composition is administered in combination with a medicament which increases GI tract pH.

35. The method of claim 34, wherein the medicament which increases GI tract pH is selected from the group consisting of proton pump inhibitors and antacids.
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