Claims
- 1. A process for the preparation of a high drug load enteric-coated pharmaceutical composition comprising the steps of:(a) preparing a dry blend comprising a medicament, a binder, and a disintegrant, and setting a portion of said dry blend aside; (b) forming a wet mass from the remainder of said dry blend not set aside in step (a); (c) extruding said wet mass to form an extrudate and spheronizing said extrudate into high-potency beadlets by dusting said wet mass extrudate with said portion of said dry blend set aside in step (a); (d) coating said beadlets with an enteric coating polymer and plasticizer in an aqueous media; and (e) blending said coated beadlets with an anti-adherent, wherein the process further comprising the step of separating said spheronized high potency beadlets formed in step ĉ into 10/18 mesh sized beadlets prior to said coating step (d).
- 2. The process of claim 1, wherein said medicament is an acid labile drug.
- 3. The process of claim 2, wherein said acid labile drug is selected from the group consisting of ddl, pravastatin, erythromycin, digoxin, pancreatin, ddA, and ddC.
- 4. The process of claim 3, wherein said medicament is ddl.
- 5. The process of claim 1, wherein said binder is sodium carboxymethylcellulose.
- 6. The process of claim 1, wherein said disintegrant is sodium starch glycolate.
- 7. The process of claim 1, wherein the wet mass is formed by the addition of a granulation solvent.
- 8. The process of claim 7, wherein said granulation solvent is water.
- 9. The process of claim 1, wherein said plasticizer is diethyl phthalate.
- 10. The process of claim 9, wherein said enteric coating comprises methacrylic acid copolymer and diethyl phthalate.
- 11. The process of claim 10, wherein said copolymer is methacrylic acid copolymer, Type C.
- 12. The process of claim 1, wherein said anti-adherent is talc.
- 13. The process of claim 1, further comprising the step of filling said coated beadlets prepared in step (e) into a capsule.
- 14. The process of claim 13, wherein said capsule is a size 0 gelatin capsule.
- 15. The process of claim 14, wherein the beadlets in said capsule comprise 400 mg ddl.
- 16. A process for the preparation of enteric-coated 2′,3′-dideoxyinosine (ddl) beadlets comprising the steps of:(a) preparing a dry blend comprising ddl, a binder, and a disintegrant, and setting a portion of said dry blend aside; (b) forming a wet mass from the remainder of said dry blend not set aside in step (a); (c) extruding said wet mass to form an extrudate and spheronizing said extrudate into high-potency beadlets by dusting said wet mass extrudate with said portion of said dry blend set aside in step (a); (d) coating said beadlets with an enteric coating polymer and plasticizer in an aqueous media; and (e) blending said coated beadlets with an anti-adherent, wherein the process further comprising the step of separating said spheronized high potency beadlets formed in step ĉ into 10/18 mesh sized beadlets prior to said coating step (d).
- 17. The process of claim 16, wherein said binder is sodium carboxymethylcellulose.
- 18. The process of claim 16, wherein said disintegrant is sodium starch glycolate.
- 19. The process of claim 16, wherein the wet mass is formed by the addition of a granulation solvent.
- 20. The process of claim 19, wherein said granulation solvent is water.
- 21. The process of claim 16, wherein said plasticizer is diethyl phthalate.
- 22. The process of claim 21, wherein said enteric coating comprises methacrylic acid copolymer and diethyl phthalate.
- 23. The process of claim 22, wherein said copolymer is methacrylic acid copolymer, Type C.
- 24. The process of claim 16, wherein said anti-adherent is talc.
- 25. The process of claim 16, further comprising the step of filling said coated beadlets prepared in step (e) into a dissolvable capsule.
- 26. The process of claim 25, wherein said capsule is a size 0 gelatin capsule.
- 27. The process of claim 26, wherein the beadlets in said capsule comprise 400 mg ddl.
- 28. A process for the preparation of a high drug load enteric-coated pharmaceutical composition comprising the steps of:(a) preparing a dry blend comprising from about 80 to about 100% medicament; from 0 to about 10% binder; and from 0 to about 10% disintegrant, all % by weight, and setting a portion of said dry blend aside; (b) forming a wet mass from the remainder of said dry blend not set aside in step (a); (c) extruding said wet mass to form an extrudate and spheronizing said extrudate into high-potency beadlets by dusting said wet mass extrudate with said portion of said dry blend set aside in step (a); (d) coating said beadlets with an enteric coating polymer and plasticizer in an aqueous media; and (e) blending said coated beadlets with an anti-adherent, wherein the process further comprising the step of separating said spheronized high potency beadlets formed in step ĉ into 10/18 mesh sized beadlets prior to said coating step (d).
- 29. The process of claim 28 wherein the medicament comprises 2′,3′-dideoxyinosine.
- 30. The process of claim 29 wherein the medicament comprises 95-100% ddl.
- 31. The process of claim 28, wherein said dry blend consists essentially of from about 80 to about 100% ddl, from 0 to about 10% binder, and from 0 to about 10% disintegrant.
- 32. The process of claim 31, wherein said dry blend consists essentially of about 95% ddl, about 1% sodium carboxymethylcellulose, and about 5% sodium starch glycolate.
- 33. The process of claim 28, wherein said binder is sodium carboxymethylcellulose.
- 34. The process of claim 28, wherein said disintegrant is sodium starch glycolate.
- 35. The process of claim 28, wherein the wet mass if formed by the addition of a granulation solvent.
- 36. The process of claim 34, wherein said granulation solvent is water.
- 37. The process of claim 28, wherein said plasticizer is diethyl phthalate.
- 38. The process of claim 36, wherein said enteric coating comprises methacrylic acid copolymer and diethyl phthalate.
- 39. The process of claim 37, wherein said copolymer is methacrylic acid copolymer, Type C.
- 40. The process of claim 28, wherein said anti-adherent is talc.
- 41. The process of claim 28, further comprising the step of filling said coated beadlets prepared in step (e) into a capsule.
- 42. The process of claim 40, wherein said capsule is a size 0 gelatin capsule.
- 43. The process of claim 41, wherein the beadlets in said capsule comprise 400 mg ddl.
- 44. The process of claim 1 further comprising the steps of drying the 10/18 mesh sized beadlets and then separating said dried beadlets into 10/20 mesh sized beadlets prior to said coating step (d).
- 45. The process of claim 28 further comprising the steps of drying the 10/18 mesh sized beadlets and then separating said dried beadlets into 10/20 mesh sized beadlets prior to said coating step (d).
Parent Case Info
This application is a divisional of U.S. application Ser. No. 09/083,597, filed May 22, 1998, abandoned.
US Referenced Citations (24)
Foreign Referenced Citations (3)
Number |
Date |
Country |
0754452 |
Jan 1997 |
EP |
0781549 |
Jul 1997 |
EP |
9403160 |
Feb 1994 |
WO |
Non-Patent Literature Citations (2)
Entry |
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