Enteric and colonic delivery using HPMC capsules
View Patent ↗The invention provides a drug delivery system for delivering a drug to either the small intestine (enteric) or the colon comprising a HPMC capsule containing the drug and wherein the HPMC capsule is provided with a suitable coating such that the drug is released from the capsule either in the small intestine or the colon.
1. A drug delivery composition consisting essentially of a coated HPMC capsule capable of containing a drug, wherein the HPMC capsule comprises a single aqueous coating such that the drug is not released from the capsule in the stomach.
2. A drug delivery composition according to claim 1 , wherein the HPMC capsule is provided with a coating such that the drug is predominately released from the capsule in the small intestine.
3. A drug delivery composition according to claim 1 , wherein the HPMC capsule is provided with a coating such that the drug is predominately released from the capsule in the colon and/or terminal ileum.
4. A drug delivery composition according to claim 2 wherein the coating comprises a material which dissolves at a pH of 5.5 or above.
5. A drug delivery composition according to claim 3 wherein the coating comprises a material which dissolves at a pH 7 or above.
6. A drug delivery composition according to claim 2 wherein the coating comprises cellulose acetate trimellitiate (CAT).
7. A drug delivery composition according to claim 2 wherein the coating comprises hydroxypropylmethyl cellulose phthalate (HPMCP).
8. A drug delivery composition according to claim 2 wherein the coating comprises polyvinyl acetate phthalate (PVAP).
9. A drug delivery composition according to claim 2 wherein the coating comprises shellac.
10. A drug delivery composition according to claim 2 wherein the coating comprises a copolymer of methacrylic acid and methylmethacrylate.
11. A drug delivery composition according to claim 3 wherein the coating composition comprises a material which is redox-sensitive.
12. A drug delivery composition according to claim 3 wherein the coating composition comprises an azopolymer or a disulphide polymer.
13. A drug delivery composition according to claim 3 wherein the coating composition comprises a material which is degraded by enzymes or bacteria present in the colon.
14. A drug delivery composition according to claim 3 wherein the coating composition comprises a copolymer of methacrylic acid and methylmethacrylate to which has been added during polymerisation the monomer methyl acrylate.
15. A drug delivery composition according to claim 3 wherein the coating composition comprises a cellulose ester.
16. A drug delivery composition according to claim 3 wherein the coating composition comprises polyvinyl acetate phthalate.
17. A drug delivery composition according to claim 2 wherein the coating is applied in the range of 5–15 mg per cm 2 of capsule surface.
18. A drug delivery composition according to claim 3 wherein the coating is applied in the range 5–20 mg per cm 2 of capsule surface.
19. A drug delivery composition according to claim 2 wherein the drug is one which is effective in the small intestine.
20. A drug delivery composition according to claim 1 wherein the drug is one which acts locally in the colon.
21. A drug delivery composition according to claim 1 wherein the coating is applied separately to empty HPMC capsule body and cap.
22. A drug delivery composition according to claim 1 wherein two equal HPMC capsule halves are filled with a caplet.
23. A drug delivery composition according to claim 22 wherein the coating is applied separately to equal empty HPMC capsule halves.
24. A drug delivery composition according to claim 22 wherein one half is coated with an insoluble polymer and the other half is enteric or colonic coated.
25. A drug delivery composition according to claim 1 wherein the HPMC capsule is coated with a film which is non-dissolving at pH<3 to 4 and dissolving at pH>5.5.
26. A drug delivery composition according to claim 1 wherein the HPMC content of the capsule shell is in the range of from 10 to 90% by weight.
27. A drug delivery composition according to claim 1 wherein stomach resistant coating is applied to HPMC capsules having a sealing on the gap between capsule body and cap.
28. A drug delivery composition consisting essentially of an HPMC capsule capable of containing a drug, wherein: (a) drug is not released from the capsule in the stomach; (b) one half of the capsule is enteric coated and the other half is colonic coated; (c) the enteric coating is at least one member selected from the group consisting of cellulose acetate trimellitiate, hydroxypropylmethyl cellulose phthalate, polyvinyl acetate phthalate, shellac, and a copolymer of methacrylic acid and ethyl acrylate: and (d) the colonic coating is a member selected from the group consisting of azopolymers, disulphide polymers and amylose.