발생일자 2015.02.17 

사건번호 1:15-cv-00164 

법원국가 UNITED STATES OF AMERICA 

관할법원명 D.C.Delaware(지방법원) 

침해권리 특허 

원고명 Cosmo Technologies Limited/ Santarus, Inc. ( 아일랜드 / NPEs )  

피고명 ACTAVIS LABORATORIES FL, Inc. ( 미국 / 외국기업 )  

소송유형 침해금지 

[Cosmo Technologies Limited/ Santarus, Inc. v. ACTAVIS LABORATORIES FL, Inc.] 사건번호 1:15-cv-00164에 따르면 원고 Cosmo Technologies Limited/ Santarus, Inc.는 피고 ACTAVIS LABORATORIES FL, Inc.을 상대로 특허 RE43799, US7410651, US7431943, US8293273, US8784888, US8895064을 침해하였다는 이유로 미국 델라웨어 지방법원에 소를 제기하였다. 

분쟁결과 분쟁중 

산업분류 화학∙바이오 > 의약품 

계쟁제품 Tablets containing 9 mg of budesonide, generic version of Uceris 

지재권번호/명칭 RE43799  Controlled release and taste masking oral pharmaceutical composition 

US7410651   Controlled release and taste masking oral pharmaceutical composition 

US7431943   Controlled release and taste masking oral pharmaceutical compositions 

US8293273   Controlled release and taste masking oral pharmaceutical composition 

US8784888   Controlled release and taste masking oral pharmaceutical composition 

US8895064   Controlled release and taste masking oral pharmaceutical composition 

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract. 

 1. A controlled release oral pharmaceutical composition containing budesonide as active ingredient consisting essentially of: a) a lipophilic matrix consisting of lipophilic compounds with a melting point between 40.degree. C. and 90 C. in which the active ingredient is at least partially inglobated; b) an amphiphilic matrix; c) an outer hydrophilic matrix consisting of hydrogel forming compounds in which the lipophilic matrix and the amphiphilic matrix are dispersed, wherein the combination of the matrices from a), b), and c) provides controlled release. 

 2. The composition according to claim 1 in which the active ingredient is mixed and at least partially inglobated in the amphiphilic matrix of point b). 

 3. The composition according to claim 1, wherein the active ingredient is mixed and at least partially inglobated in the lipophilic matrix. 

 4. The composition according to claim 1, wherein, the lipophilic matrix consists of compounds selected from the group consisting of C6-C 20 alcohols, C8-C 20 fatty acids, and esters of fatty acids with, glycerol, sorbitol or other polyalcohols with carbon atom chain not higher than six. 

 5. The composition according to claim 1, wherein the amphiphilic compounds are selected from the group consisting of polar lipids of type I or II, ceramides, glycol alkyl ethers, esters of fatty acids with polyethylene glycols, and diethylene glycols. 

 6. The composition according to claim 1, wherein the lipophilic matrix consists of a compound selected from the group consisting of unsaturated or hydrogenated alcohols or fatty acids, salts, esters or amides thereof; mono-, di- or triglycerides of fatty acids, polyethoxylated derivatives thereof; waxes; and cholesterol derivatives. 

 7. The composition according to claim 1, wherein the hydrophilic matrix consists of compounds selected from the group consisting of acrylic or methacrylic acid polymers or copolymers, alkylvinyl polymers, hydroxyalkylcellulose, carboxyalkylcellulose, polysaccharides, dextrins, pectins, starches and derivatives, alginic acid, natural or synthetic gums, and polyalcohols. 

 8. The composition according to claim 1, wherein the active ingredient is wholly contained in the lipophilic/amphiphilic matrix, in the form of tablets, capsules or minitablets. 

 9. The composition according to claim 1, wherein the active ingredient is dispersed both in the hydrophilic matrix and in the lipophilic/amphiphilic matrix, in the form of tablets, capsules or minitablets. 

 10. The composition according to claim 1, wherein said composition is in the form of tablets chewable or erodible in the buccal cavity or in the first portion of the gastrointestinal tract. 

 11. A method for the treatment of Inflammatory Bowel Disease and Irritable Bowel Syndrome, comprising administering the composition according to claim 1 to a patient in need of such a treatment. 

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract. 

 1. A controlled release tablet or mini-tablet composition, consisting essentially of: a hydrophilic first matrix comprising a lipophilic phase and an amphiphilic phase, wherein said lipophilic phase and said amphiphilic phase are in a second matrix together, and said second matrix is dispersed throughout the hydrophilic first matrix, wherein said hydrophilic first matrix consists of compounds selected from the group consisting of acrylic or methacrylic acid polymers, acrylic copolymers, methacrylic copolymers, alkyl vinyl polymers, hydroxyalkylcellulose, carboxyalkylcellulose, polysaccharides, dextrins, pectines, starches, starch derivatives, alginic acid, natural gums, synthetic gums, and poylyalcohols, wherein said lipophilic phase is in a granular form and consists of compounds with a melting point between 40 and 90.degree. C. and an active ingredient at least partially incorporated in said lipophilic phase, wherein said amphiphilic phase comprises an active ingredient at least partially incorporated in said amphiphilic phase. 

 2. The composition according to claim 1, further comprising compounds that are polar lipids of type I or II, ceramides, glycol alkyl ethers, esters of fatty acids with polyethylene glycols or diethylene glycols. 

 3. The composition according to claim 1, wherein the lipophilic phase comprises one or more compounds selected from the group consisting of unsaturated or hydrogenated alcohols or fatty acids, salts, esters or amides thereof, mono-, di- or triglycerides of fatty acids, the polyethoxylated derivatives thereof, waxes, and cholesterol derivatives. 

 4. The composition according to claim 1, wherein the hydrophilic matrix consists of hydrogel-forming compounds. 

 5. The composition according to claim 1, further comprising a gastro-resistant coating. 

 6. The composition according to claim 5, wherein the gastro-resistant coating consists of methacrylic acid polymers or cellulose derivatives. 

 7. The composition according to claim 1, wherein said composition is in the form of tablets. 

 8. The composition according to claim 1, wherein said composition is in the form of minitablets. 

 9. The composition according to claim 1, in which the active ingredient belongs to the therapeutical classes of analgesics, antitussives, bronchodilators, antipsychotics, selective .beta. 2 antagonists, calcium antagonists, antiparkinson drugs, non-steroidal anti-inflammatory drugs, antihistamines, antidiarrheals and intestinal antiinflammatories, spasmolytics, anxiolytics, oral anti-diabetics, cathartics, antiepileptics, topical antimicrobials. 

 10. The composition according to claim 1, wherein the active ingredient is selected from the group consisting of mesalazine (5-aminosalicylic acid), budesonide, metformin, octylonium bromide, gabapentin, carbidopa, nimesulide, propionylilcarnitine, isosorbide mono- and dinitrate, naproxen, ibuprofen, ketoprofen, diclofenac, thiaprophenic acid, nimesulide, chlorhexidine, benzydamine, tibezonium iodide, cetylpyridinium chloride, benzalkonium chloride, and sodium fluoride. 

 11. The composition according to claim 1, further comprising bioadhesive substances. 

 12. A pharmaceutical composition, comprising the composition according to claim 1, in the form of tablets chewable or erodible in the buccal cavity or in the first portion of the gastrointestinal tract. 

 13. The method according to claim 1, wherein the amphiphilic matrix comprises 5 to 95% by weight of an active ingredient.