Claims for Patent: 6,893,662

Summary for Patent: 6,893,662

Title:	Pharmaceutical dosage form with multiple coatings for reduced impact of coating fractures
Abstract:	The present invention relates to a pharmaceutical composition in a solid unit dosage form for oral administration in a human or lower animal comprising: a. a safe and effective amount of a therapeutically active agent; b. an inner coating layer selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:2, poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures thereof; and c. an outer coating layer comprising an enteric polymer or film coating material; wherein the inner coating layer is not the same as the outer coating layer; wherein if the inner coating layer is poly(methacrylic acid, methyl methacrylate) 1:1 then the outer coating layer is not poly(methacrylic acid, methyl methacrylate) 1:2 or is not a mixture of poly(methacrylic acid, methyl methacrylate) 1:1 and poly(methacrylic acid, methyl methacrylate) 1:2; and wherein the inner coating layer and the outer coating layer do not contain any therapeutically active agent. This invention further relates to a method of maintaining the desired site of delivery of a therapeutic agent in the gastrointestinal tract by administering the above compositions to a human or lower animal.
Inventor(s):	Dittmar; Gregory Paul (Norwich, NY), Amante; Joseph Michael (Norwich, NY), Cronk; Tony Ryan (Mishawaka, IN), Newby; Daniel Gary (New Berlin, NY)
Assignee:	The Procter & Gamble Company (Cincinnati, OH)
Application Number:	09/996,555
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,893,662
Patent Claims:	1. A pharmaceutical composition in a solid unit dosage form for oral administration in a human or lower animal consisting essentially of: a. a safe and effective amount of a therapeutically active agent; b. an inner coating layer selected from the group consisting of poly(methiacrylic acid, methyl methacrylate) 1:2, poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures thereof; and c. an outer coating layer, applied to the inner coating layer, said outer coating layer comprising an enteric polymer that begins to dissolve in an aqueous medium at a pH of less than about 7, said enteric polymer being selected from the group consisting of polymethacrylates, anionic polymethacrylates, poly(methacrylic acid, methyl methacrylate) 1:1, mixtures of poly(methacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1;1, polyvinyl acetate phthalate, poly(methacrylic acid, ethyl acrylate) 1:1, and compatible mixtures thereof; wherein the inner coating layer is not the same as the outer coating layer; wherein if the inner coating layer is poly(methacrylic acid, methyl methacrylate) 1:1 then the outer coating layer is not poly(methacrylic acid, methyl methacrylate) 1:2 or is not a mixture of poly(methacrylic acid, methyl methacrylate) 1:1 and poly(methacrylic acid, methyl methacrylate) 1:2; and wherein the inner coating layer and the outer coating layer contain no therapeutically active agent. 2. The composition of claim 1 wherein the inner coating layer is poly(methacrylic acid, methyl methacrylate) 1:2. 3. The composition of claim 1 wherein the outer coating layer is selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures of poly(methacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1:1. 4. The composition of claim 3 wherein the outer coating layer is a mixture of poly(methacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1:1. 5. The composition of claim 1 wherein the total coating thickness of the inner and outer coating layers combined is from about 5 mg/cm.sup.2 to about 40 mg/cm.sup.2. 6. The composition of claim 5 wherein the total coating thickness is from about 10 mg/cm.sup.2 to about 15 mg/cm.sup.2. 7. The composition of claim 6 wherein the solid dosage form is coated by continuous spray methods wherein the outer coating layer is applied after the inner coating layer but before the inner coating layer is dried or cured. 8. The composition of claim 1 wherein the therapeutically active agent is selected from the group consisting of laxatives, anti-diarrheals, nonsteroidal anti-inflammatory agents, 5-amino salicylic acid, glucocorticoids, antimicrobials, immunosuppressants, chemotherapeutics or anti-cancer drugs, peptides, proteins, cardiovascular drugs, psychotropic drugs, H2-blockers, antiasthmatic agents, and antihistamines. 9. The composition of claim 8 wherein the therapeutically active agent is a nonsteroidal anti-inflammatory agent. 10. The composition of claim 9 wherein the therapeutically active agent is 5-amino salicylic acid. 11. A pharmaceutical composition in a solid unit dosage form for oral admininstration in a human or lower animal consisting essentially of: a. a safe and effective amount of a therapeutically active agent; b. an inner coating layer comprising poly(methacrylic acid, methyl methacrylate) 1:2; and c. an outer coating layer, applied to the inner coating layer, said outer coating layer comprising an enteric polymer that begins to dissolve in an aqueous medium at a pH of less than about 7, said enteric polymer being selected from the group consisting of polymethacrylates, anionic polymethacrylates, poly(methacrylic acid, methyl methacrylate) 1:1, mixtures of poly(methacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1:1, polyvinyl acetate phthalate, poly(methacrylic acid, ethyl acrylate) 1:1, and compatible mixtures thereof; wherein the inner coating layer is not the same as the outer coating layer. 12. The composition of claim 11 wherein the outer coating layer is selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:1 and mixtures of poly(methacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1:1. 13. The composition of claim 12 wherein the outer coating layer is a mixture of poly(methacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1:1. 14. The composition of claim 11 wherein the total coating thickness of the inner and outer coating layers combined is from about 5 mg/cm.sup.2 to about 40 mg/cm.sup.2. 15. The composition of claim 14 wherein the total coating thickness is from about 10 mg/cm.sup.2 to about 15 mg/cm.sup.2. 16. The composition of claim 15 wherein the solid dosage form is coated by continuous spray methods wherein the outer coating layer is applied after the inner coating layer but before the inner coating layer is dried or cured. 17. The composition of claim 11 wherein the therapeutically active agent is selected from the group consisting of laxatives, anti-diarrheals, nonsteroidal anti-inflammatory agents, 5-amino salicylic acid, glucocorticoids, antimicrobial, immunosuppressants, chemotherapeutics or anti-cancer drugs, peptides, proteins, cardiovascular drugs, psychotropic drugs, H2-blockers, antiasthmatic agents, and antihistamines. 18. The composition of claim 17 wherein the therapeutically active agent is a nonsteroidal anti-inflammatory agent. 19. The composition of claim 18 the therapeutically active agent is 5-amino salicylic acid. 20. The composition of claim 11 wherein the solid dosage form is a compressed tablet. 21. A method of consistent and reliable delivery and release of a therapeutically active agent to the desired region of delivery by orally administering the composition of claim 1. 22. A method of consistent and reliable delivery and release of a therapeutically active agent to the desired region of delivery by orally administering the composition of claim 11. 23. The composition of claim 1 wherein the solid dosage form is a compressed tablet. 24. The composition of claim 1 wherein the solid unit dosage form has a total weight from about 600 mg to about 1200 mg. 25. The composition of claim 10 wherein the 5-amino salicylic acid is present in an amount from about 700 mg to about 900 mg per solid unit dosage form. 26. The composition of claim 1 wherein the outer coating layer has a minimum thickness from about 10 .mu.m to about 200 .mu.m. 27. The composition of claim 4 wherein the outer coating layer has a minimum thickness from about 10 .mu.m to about 50 .mu.m. 28. The composition of claim 27 wherein the outer coating layer has a minimum thickness from about 20 .mu.m to about 40 .mu.m. 29. The composition of claim 11 wherein the solid unit dosage form has a total weight from about 600 mg to about 1200 mg. 30. The composition of claim 19 wherein the 5-amino salicylic acid is present in an amount from about 700 mg to about 900 mg per solid unit dosage form. 31. The composition of claim 11 wherein the outer coating layer has a minimum thickness from about 10 .mu.m to about 200 .mu.m. 32. The composition of claim 13 wherein the outer coating layer has a minimum thickness from about 10 .mu.m to about 50 .mu.m. 33. The composition of claim 32 wherein the outer coating layer has a minimum thickness from about 20 .mu.m to about 40 .mu.m. 34. A pharmaceutical composition in a solid unit dosage form for oral administration in a human or lower animal consisting essentially of: a. a safe and effective amount of 5-amino salicylic acid; b. an inner coating layer comprising poly(methacrylic acid, methyl methacrylate) 1:2; and c. an outer coating layer, applied to the inner coating layer, said outer coating layer comprising an enteric polymer that begins to dissolve in an aqueous medium at a pH of less than about 7, said enteric polymer being a mixture of poly(methiacrylic acid, methyl methacrylate) 1:2 and poly(methacrylic acid, methyl methacrylate) 1:1. 35. A method of consistent and reliable delivery and release of 5-amino salicylic acid to the desired region of delivery by orally administering the composition of claim 34.