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1. WO2020115256 - SOLID COMPOSITION COMPRISING MESALAZINE

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[ EN ]

CLAIMS

1. A method of producing a coatable core for a modified release drug formulation for oral administration, the coatable core having a high drug load of at least 70 wt % based on the total weight of the coatable core, the method comprising:

granulating a composition comprising a drug and at least one binder to form granules;

blending the granules with a pharmacologically acceptable disintegrant and optionally one or more additional pharmacologically acceptable excipients to form a compression blend, wherein the disintegrant is present in an amount from about 0.5 wt % to about 5 wt %, based on the total weight of the coatable core; and

compressing the compression blend using an external lubrication compression method to form a coatable core.

2. A method as claimed in Claim 1 , wherein said composition further comprises at least one granulation liquid, and wherein said method further comprises the step of drying said granules to form dry granules.

3. A method as claimed in Claim 2, wherein said granulation liquid is water.

4. A method as claimed in any preceding claim, wherein the coatable core has a drug load of from about 85 wt % to about 95 wt %, based on the total weight of the coatable core.

5. A method as claimed in any preceding claim, wherein the binder is present in an amount of about 3 wt % or less, preferably about 2 wt % or less, based on the total weight of the coatable core.

6. A method as claimed in any preceding claim, wherein the disintegrant is present in an amount of about 0.5 wt % to about 3 wt %, based on the total weight of the coatable core.

7. A method as claimed in any preceding claim, wherein the one or more additional pharmacologically acceptable excipient comprises a lubricant.

8. A method as claimed in Claim 7, wherein the lubricant is present in an amount of about 0.5 wt % or less, preferably about 0.25 wt % or less, more preferably about 0.1 wt % or less, and most preferably about 0.05 wt % or less, based on the total weight of the coatable core.

9. A method as claimed in any preceding claim, wherein the drug is present in the core in an amount of from about 350 mg to about 1650 mg, or from about 450 mg to about 1650 mg, or from about 750 mg to about 1650 mg, or from about 1150 mg to about 1650 mg, or from about 1450 mg to about 1650 mg, or from about 1550 mg to about 1650 mg.

10. A method as claimed in Claim 9, wherein the drug is present in the core in an amount selected from about 400 mg, about 800 mg, about 1200 mg, about 1500 mg, or about 1600 mg.

11. A method as claimed in any preceding claim, wherein the granules have a bulk density of at least about 540 g/l.

12. A method as claimed in any preceding claim, wherein the compression blend has a bulk density of at least about 600 g/l.

13. A coatable core for a modified release drug formulation for oral administration, the coatable core having a high drug load of at least 70 wt %, based on the total weight of the coatable core, the core comprising:

a drug in an amount of more than about 1200 mg;

a pharmacologically acceptable lubricant in an amount of less than about 0.5 wt %, based on the total weight of the coatable core;

a pharmacologically acceptable disintegrant in an amount of from about 0.5 wt % to about 5 wt %, based on the total weight of the coatable core; and

optionally one or more additional pharmacologically acceptable excipients.

14. A coatable core as claimed in Claim 13, wherein the coatable core has a friability of more than 0% to about 0.5%, preferably from about 0.1 % to about 0.25%, most preferably from about 0.1 to about 0.2%.

15. A coatable core as claimed in Claim 13 or Claim 14, wherein the coatable core has a disintegration time of less than about 10 minutes, preferably less than about 5 minutes.

16. A coatable core as claimed in any one of Claims 13 to 15, wherein the coatable core has a drug load of from about 85 wt % to about 95 wt %, based on the total weight of the coatable core.

17. A coatable core as claimed in any one of Claims 13 to 16, wherein the disintegrant is present in an amount of about 0.5 wt % to about 3 wt %, based on the total weight of the coatable core.

18. A coatable core as claimed in any one of Claims 13 to 17, wherein the lubricant is present in an amount of about 0.25 wt % or less, more preferably about 0.1 wt % or less, most preferably about 0.05 wt % or less, based on the total weight of the coatable core.

19. A coatable core as claimed in any one of Claims 13 to 18, wherein the drug is present in the core in an amount of from about 1250 mg to about 1650 mg, or from about 1450 mg to about 1650 mg, or from about 1550 mg to about 1650 mg, or about 1600 mg.

20. A delayed release drug formulation for oral administration to deliver a drug to the intestine of a subject, said formulation comprising:

a core having a high drug load of at least 70 wt %, based on the total weight of the coatable core, the core comprising:

a drug in an amount of more than about 1200 mg;

a pharmacologically acceptable lubricant in an amount of less than about 0.5 wt %, based on the total weight of the coatable core;

a pharmacologically acceptable disintegrant in an amount of from about 0.5 wt % to about 5 wt %, based on the total weight of the coatable core; and

optionally one or more additional pharmacologically acceptable excipients;

a coating for the core, the coating comprising an outer layer, and optionally at least one layer between the core and the outer layer selected from the group consisting of an isolation layer and an inner layer;

said outer layer comprising a film-forming enteric polymer having a pH threshold at about pH 5 or above, and optionally, an enzymatically degradable polymer that is degraded by colonic enzymes;

said inner layer comprising a polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base;

said isolation layer comprising a non-ionic polymer which is soluble in intestinal fluid or gastrointestinal fluid.

21. A delayed release drug formulation as claimed in Claim 20, wherein said outer layer comprises an enzymatically degradable polymer that is degraded by colonic enzymes.

22. A delayed release drug formulation as claimed in Claim 21 , wherein said outer layer comprises a film-forming enteric polymer having a pH threshold at about pH 5 or above, and an enzymatically degradable polymer that is degraded by colonic enzymes; and wherein said outer layer is applied to the core using a coating preparation formed by combining said enzymatically degradable polymer in an aqueous medium with said film-forming enteric polymer in an organic medium.

23. A delayed release drug formulation as claimed in any one of Claims 20 to 22, wherein the coatable core has a friability of more than 0% to about 0.5%, preferably from about 0.1% to about 0.25%, most preferably from about 0.1 to about 0.2%.

24. A delayed release drug formulation as claimed in any one of Claims 20 to 23, wherein the coatable core has a disintegration time of less than about 10 minutes, preferably less than about 5 minutes.

25. A delayed release drug formulation as claimed in any one of Claims 20 to 24, wherein the coatable core has a drug load of from about 85 wt % to about 95 wt %, based on the total weight of the coatable core.

26. A delayed release drug formulation as claimed in any one of Claims 20 to 25, wherein the disintegrant is present in an amount of from about 0.5 wt % to about 3 wt %, based on the total weight of the coatable core.

27. A delayed release drug formulation as claimed in any one of Claims 20 to 26, wherein the lubricant is present in an amount of about 0.25 wt % or less, more preferably about 0.1 wt % or less, most preferably 0.05 wt % or less.

28. A delayed release drug formulation as claimed in any one of Claims 20 to 27, wherein the drug is present in the core in an amount of from about 1250 mg to about 1650 mg, or from about 1450 mg to about 1650 mg, or from about 1550 mg to about 1650 mg, or about 1600 mg.