발생일자 2015.06.26 

사건번호 1:15-cv-00109 

법원국가 UNITED STATES OF AMERICA 

관할법원명 D.C.N.D.WestVirginia(지방법원) 

침해권리 특허 

원고명 Salix Pharmaceuticals, Inc/ Dr Falk Pharma GmbH ( 미국 / 외국기업 )  

피고명 Mylan Pharmaceuticals, Inc./ Mylan, Inc. ( 미국 / 외국기업 )  

소송유형 침해금지 

[Salix Pharmaceuticals, Inc et al v. Mylan Pharmaceuticals, Inc. et al] 사건번호 1:15-cv-00109에 따르면 원고 Salix Pharmaceuticals, Inc/ Dr Falk Pharma GmbH는 피고 Mylan Pharmaceuticals, Inc./ Mylan, Inc.을(를) 상대로 특허 US6551620|US8337886|US8496965|US8865688을(를) 침해하였다는 이유로 미국 웨스트버지니아 북부 지방법원에 소를 제기하였다. 

분쟁결과 분쟁중 

산업분류 화학∙바이오 > 의약품 

계쟁제품 Generic version of 375mg mesalamine oral extended release capsules - Generic version of AprisoⓇ 

지재권번호/명칭

US6551620   Pellet formulation for the treatment of the intestinal tract 

US8337886   Pellet formulation for the treatment of the intestinal tract 

US8496965   Pellet formulation for the treatment of the intestinal tract 

US8865688   Pellet formulation for the treatment of the intestinal tract 

An orally adminsterable pharmaceutical pellet formulation for the treatment of the intestinal tract is disclosed, which comprises a core and an enteric coating, the core including, as a pharmaceutical active compound, aminosalicylic acid or a pharmaceutically tolerable salt or a derivative thereof. 

1. An orally administrable pharmaceutical pellet formulation having a controlled release profile for the treatment of the intestinal tract, which comprises a core and an enteric coating and optionally pharmaceutically tolerable additives, the core including, as a pharmaceutical active compound, aminosalicylic acid or a pharmaceutically acceptable salt, wherein the active compound is present in the core in a non gel-forming polymer matrix which is essentially insoluble in the intestinal tract and permeable to intestinal fluids and the active compound, the matrix-forming polymer making up at least 1% by weight of the total weight of the core, and wherein the matrix-forming polymer is selected from the group consisting of poly(ethyl acrylate, methyl methacrylate) and poly(ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate chloride). 

2. The pellet formulation as claimed in claim 1, wherein the matrix-forming polymer makes up 4-10% by weight of the total weight of the core. 

3. The pellet formulation as claimed in claim 1 wherein the polymer matrix extends through the entire core and the active compound is homogeneously dispersed in the polymer matrix. 

4. The pellet formulation as claimed in claim 1, wherein the active compound is 5-aminosalicylic acid. 

5. The pellet formulation as claimed in claim 1, wherein the enteric coating comprises a methacrylic acid copolymer or methylhydroxypropyl-cellulose phthalate. 

6. The pellet formulation as claimed in claim 5, wherein the enteric coating contains poly(methacrylic acid, methyl methacrylate), the polymer containing free carboxyl groups as functional groups. 

7. The pellet formulation as claimed in claim 1, wherein the pellet only comprises one coating layer. 

8. The pellet formulation as claimed in claim 1, comprising, as an active compound, 5-aminosalicylic acid in a poly(ethyl acrylate, methyl methacrylate) 2:1 matrix, the polymer containing ester groups as functional groups, in the core and an enteric coating which comprises poly(methacrylic acid, methyl methacrylates) 1:1 or 1:2, the polymer containing free carboxyl groups as functional groups, and optionally pharmaceutically tolerable additives. 

9. The pellet formulation as claimed in claim 1, wherein the release of active compound in 0.1 M HCl after 2 hours is less than 10%, and in artificial gastric juice at pH of about 6.8 after 30 minutes is 10-30%, after 2 hours is 40-60%, and after 6 hours is at least 80%. 

10. A pharmaceutical formulation, which comprises pellets as claimed in claim 1. 

11. The pharmaceutical formulation as claimed in claim 10, which is a gelatin capsule or a tablet which contains the pellets. 

12. A method for treating, or preventing the recurrence of intestinal disorders, secondary disorders resulting therefrom, or intestinal cancer comprising administering the pellet formulation of claim 1 to a patient in need thereof. 

13. The method of claim 12, wherein the intestinal disorder is an inflammatory intestinal disorder in the active or remission phase. 

14. The method of claim 12, wherein the intestinal disorder is a polyp in the gastrointestinal tract. 

15. The method of claim 14, wherein the polyp is an adenoma or shows polypous growth. 

16. The method of claim 14, wherein the pellet formulation lowers the recurrence rate of adenomas or colorectal polyps compared to a method free of administering the formulation. 

17. A method for treating colon cancer comprising administering the pellet formulation of claim 1 to a patient in need thereof. 

An orally adminsterable pharmaceutical pellet formulation for the treatment of the intestinal tract is disclosed, which comprises a core and an enteric coating, the core including, as a pharmaceutical active compound, aminosalicylic acid or a pharmaceutically tolerable salt or a derivative thereof. 

 1. A controlled release pellet formulation for treatment of the intestinal tract, said formulation comprising a core comprising: 1) a homogeneously dispersed pharmaceutically active compound in a non gel-forming polymer matrix and 2) an enteric coating, wherein the non gel-forming polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluid made by the process comprising: mixing the pharmaceutically active compound and the non gel-forming polymer matrix; scattering in a pharmaceutically tolerable additive; and extruding a moist mass of the matrix-forming polymer and the active compound. 

 2. The controlled release pharmaceutical pellet formulation of claim 1, wherein the process further comprises applying an enteric coating to a pellet made from the moist mass. 

 3. The controlled release pharmaceutical pellet formulation of claim 1, wherein the enteric coating comprises a methacrylic acid containing copolymer or methylhydroxypropyl cellulose phthalate. 

 4. The controlled release pharmaceutical pellet formulation of claim 3, wherein the methacrylic acid containing copolymer comprises co-poly(methacrylic acid, methyl methacrylate), wherein the co-polymer comprises free carboxylic acid functional groups. 

 5. The controlled release pharmaceutical pellet formulation of claim 1, wherein the process further comprises cutting the moist mass into pieces. 

 6. The controlled release pharmaceutical pellet formulation of claim 5, wherein the pieces are about 1 mm long. 

 7. The controlled release pharmaceutical pellet formulation of claim 5, wherein the process further comprises rounding the pieces in a spheronizer. 

 8. The controlled release pharmaceutical pellet formulation of claim 7, wherein the process further comprises drying the pieces. 

 9. The controlled release pharmaceutical pellet formulation of claim 8, wherein the pieces are dried at about 60.degree. C. 

 10. The controlled release pharmaceutical pellet formulation of claim 8, wherein the process further comprises: dissolving poly(methacrylic acid, methylmethacrylate) 1:1 in an ethanol/water mixture; suspending triethyl citrate, talc, titanium dioxide and magnesium stearate in the mixture; and coating the pieces with the suspended mixture. 

 11. The controlled release pharmaceutical pellet formulation of claim 1, wherein the matrix-forming polymer is selected from the group consisting of poly(ethyl acrylate, methyl methacrylate) and poly(ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate chloride). 

 12. The controlled release pharmaceutical pellet formulation of claim 1, wherein the non gel-forming polymer matrix makes up at least 1% by weight of the total weight of the core. 

 13. The controlled release pharmaceutical pellet formulation of claim 1, wherein the pharmaceutically active compound comprises 5-aminosalicylic acid, balsalazide, sulfasalazine or a pharmaceutically acceptable salt thereof. 

 14. The controlled release pharmaceutical pellet formulation of claim 1, wherein the pharmaceutical pellet formulation is used for the treatment of recurrence of inflammatory intestinal disorders, formation of polyps, intestinal cancer, colorectal polyps or colorectal cancer. 

 15. The controlled release pharmaceutical pellet formulation of claim 14, wherein the inflammatory intestinal disorders comprise Crohn's disease or ulcerative colitis. 

 16. The controlled release pharmaceutical pellet formulation of claim 1, wherein the pharmaceutical pellet formulation is used for the maintenance of remission of ulcerative colitis. 

 17. The controlled release pharmaceutical pellet formulation of claim 1, wherein the pellet formulation further comprises pharmaceutically tolerable additives. 

 18. The controlled release pharmaceutical pellet formulation of claim 1, wherein the pellets of the formulation are about 0.1 mm to about 3 mm in size. 

 19. A controlled release pellet formulation for treatment of the intestinal tract, said formulation comprising: 1) a core comprising a homogeneously dispersed pharmaceutically active compound in a non gel-forming polymer matrix and 2) an enteric coating, wherein the non gel-forming polymer matrix is essentially insoluble in the intestinal tract and permeable to intestinal fluids, and wherein the non gel-forming polymer matrix makes up at least 1% by weight of the total weight of the core, and wherein the matrix-forming polymer is selected from the group consisting of poly(ethyl acrylate, methyl methacrylate) and poly(ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate chloride). 

 20. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pharmaceutically active compound comprises 5-aminosalicylic acid, balsalazide, sulfasalazine or a pharmaceutically acceptable salt thereof. 

 21. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pharmaceutical pellet formulation is contained in capsules. 

 22. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pharmaceutical pellet formulation is contained in sachets. 

 23. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pharmaceutical pellet formulation is used for the treatment of recurrence of inflammatory intestinal disorders, formation of polyps, intestinal cancer, colorectal polyps or colorectal cancer. 

 24. The controlled release pharmaceutical pellet formulation of claim 23, wherein the inflammatory intestinal disorders comprise Crohn's disease or ulcerative colitis. 

 25. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pharmaceutical pellet formulation is used for the maintenance of remission of ulcerative colitis. 

 26. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pellet formulation further comprises pharmaceutically tolerable additives. 

 27. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pellets of the formulation are about 0.1 mm to about 3 mm in size. 

 28. The controlled release pharmaceutical pellet formulation of claim 19, wherein the pellet formulation further comprises one or more of microcrystalline cellulose, magnesium stearate, talc, or titanium dioxide. 

 29. A method of maintaining the remission of ulcerative colitis comprising, administering a controlled release pharmaceutical pellet formulation for the treatment of the intestinal tract, which controlled release pharmaceutical pellet formulation is as defined in claim 1. 

 30. The method of claim 29, wherein the pharmaceutically active compound comprises 5-aminosalicylic acid, balsalazide, sulfasalazine or a pharmaceutically acceptable salt thereof. 

 31. The method of claim 29, wherein the pharmaceutical pellet formulation is contained in capsules. 

 32. The method of claim 29, wherein the pharmaceutical pellet formulation is contained in sachets. 

 33. The method of claim 29, wherein the pharmaceutical pellet formulation is used for the prevention of, treatment of or the prevention of recurrence of inflammatory intestinal disorders, formation of polyps, intestinal cancer, colorectal polyps or colorectal cancer. 

 34. The method of claim 33, wherein the inflammatory intestinal disorders comprise Crohn's disease or ulcerative colitis. 

 35. The method of claim 29, wherein the pharmaceutical pellet formulation is used for the maintenance of remission of ulcerative colitis. 

 36. The method of claim 29, wherein the pellet formulation further comprises pharmaceutically tolerable additives. 

 37. The method of claim 29, wherein the pellets of the formulation are about 0.1 mm to about 3 mm in size. 

 38. The method of claim 29, wherein the pellet formulation further comprises one or more of microcrystalline cellulose, magnesium stearate, talc, or titanium dioxide.