발생일자 2015.02.04 

사건번호 3:15-cv-00826 

법원국가 UNITED STATES OF AMERICA 

관할법원명 D.C.NewJersey(지방법원) 

침해권리 특허 

원고명 Orexo AB ( 스웨덴 / 외국기업 )  

피고명 ACTAVIS LABORATORIES FL, Inc./ Actavis, Inc./ Andrx Corporation/ ACTAVIS PHARMA, Inc. ( 미국 / 외국기업 )  

소송유형 침해금지 

[Orexo AB v. ACTAVIS LABORATORIES FL, Inc. et al] 사건번호 3:15-cv-00826에 따르면 원고 Orexo AB는 피고 ACTAVIS LABORATORIES FL, Inc./ Actavis, Inc./ Andrx Corporation/ ACTAVIS PHARMA, Inc.을 상대로 특허 US6759059, US6761910, US7910132 을 침해하였다는 이유로 미국 뉴저지 지방법원에 소를 제기하였다. 

분쟁결과 분쟁중 

산업분류 화학∙바이오 > 의약품 

계쟁제품 Generic version of Abstral

지재권번호/명칭

US6759059   Fentanyl composition for the treatment of acute pain 

US6761910   Pharmaceutical composition for the treatment of acute disorders 

US7910132   Pharmaceutical composition for the treatment of acute disorders 

A pharmaceutical composition for the treatment of acute pain by sublingual administration is described. The composition comprises an essentially water-free, ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles which are adhered to the surface of carrier particles which are substantially larger than the particles of fentanyl, and are essentially water-soluble. In a preferred embodiment, the composition also contains a bioadhesion and/or mucoadhesion promoting agent. The invention also relates to the preparation of the composition, and to the use of the composition for the treatment of acute pain. 

1. A pharmaceutical composition for the treatment of acute pain by sublingual administration, comprising an essentially water-free, ordered mixture of microparticles of fentanyl or a pharmaceutically acceptable salt thereof adhered to the surfaces of carrier particles, said carrier particles being substantially larger than said microparticles of fentanyl and being essentially water-soluble, and a bioadhesion and/or mucoadhesion promoting agent mainly adhered to the surfaces of said carrier particles. 

2. A composition according to claim 1, comprising from 0.05 to 20 weight percent of fentanyl. 

3. A composition according to claim 1, comprising from 0.05 to 5 weight percent of fentanyl. 

4. A composition according to claim 1, wherein the particles of fentanyl have a weight based mean diameter of less than 10 .mu.m. 

5. A composition according to claim 1, wherein the mean sieve diameter of the carrier particles is less than 750 .mu.m. 

6. A composition according to claim 1, wherein the carrier comprises a brittle material which will fragmentize easily when compressed. 

7. A composition according to claim 1, wherein the carrier particles contain from 0.1 to 25 weight percent of the bio/mucoadhesion promoting agent based on the total composition. 

8. A composition according to claim 7, wherein the bio/mucoadhesion promoting agent is selected from the group consisting of acrylic polymers, cellulose derivatives, natural polymers having mucoadhesive properties, and mixtures thereof. 

9. A composition according to claim 8, wherein the bio/mucoadhesion promoting agent is selected from the group consisting of cellulose derivatives and comprising hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, methyl cellulose, ethyl hydroxyethyl cellulose, carboxymethyl cellulose, and modified cellulose gum; crosscaramellose; modified starch; acrylic polymers comprising carbomer and its derivatives; polyethylene oxide; chitosan; gelatin; sodium alginate; pectin; scleroglucan; xanthan gum; guar gum; poly-co-(methyl vinyl ether-maleic anhydride); and mixtures thereof. 

10. A composition according to claim 1, further comprising a pharmaceutically acceptable surfactant in a finely dispersed form and intimately mixed with the fentanyl. 

11. A composition according to claim 10, wherein the surfactant is present in an amount from 0.5 to 5 weight percent of the composition. 

12. A composition according to claim 10, wherein the surfactant is selected from the group consisting of sodium lauryl sulfate, polysorbates, bile acid salts and mixtures thereof. 

13. A composition according to claim 1, wherein the carrier particles comprise a water-soluble, pharmaceutically acceptable carbohydrate and/or inorganic salt. 

14. A composition according to claim 13, wherein the carrier particles comprise one or more of the materials mannitol, lactose, calcium phosphate and sugar. 

15. A composition according to claim 1, wherein the carrier particles contain at least one pharmaceutical disintegrating agent promoting the dispersion of the microparticles of fentanyl over the sublingual mucosa. 

16. A composition according to claim 15, wherein the disintegrating agent is selected from the group consisting of cross-linked polyvinylpyrrolidone, carboxymethyl starch, natural starch, microcrystalline cellulose, cellulose gum, and mixtures thereof. 

17. A composition according to claim 15, wherein the disintegrating agent is present in an amount from 1 to 10 weight percent of the composition. 

18. A method for the treatment of acute pain, comprising administering to an individual in need thereof, an effective amount of fentanyl or a pharmaceutically acceptable salt thereof in microparticle form for the preparation of an essentially water-free pharmaceutical composition for the treatment of acute pain, wherein microparticles are adhered to surfaces of carrier particles which are substantially larger than said microparticles and are essentially water-soluble, and a bioiadhesion and/or mucoadhesion promoting agent is mainly adhered to the surfaces of said carrier particles. 

19. A method for the treatment of acute pain, wherein to an individual afflicted with acute pain is administered sublingually at least one dose unit of an essentially water-free pharmaceutical composition containing an effective amount of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles adhered to the surfaces or carrier particles, which are substantially larger than said microparticles and are essentially water-soluble, and a bioadhesion and/or mucoadhesion promoting agent mainly adhered to the surfaces of said carrier particles. 

20. A method according to claim 19, wherein the fentanyl is administered in an amount from 0.05 to 20 mg, preferably then from 0.1 to 5 mg, per dose unit. 

A pharmaceutical composition for the treatment of acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders. 

1. A pharmaceutical composition for the treatment of acute disorders by sublingual administration, comprising an essentially water-free, ordered mixture of microparticles of at least one pharmaceutically active agent adhered to the surfaces of carrier particles, said particles being substantially larger than said microparticles and being water-soluble, and a bioadhesion and/or mucoadhesion promoting agent mainly adhered to the surfaces of the carrier particles. 

2. A composition according to claim 1, wherein the microparticles of said active agent or agents have a weight based mean diameter of less than 10 .mu.m. 

3. A composition according to claim 1, wherein the mean sieve diameter of the carrier particles is between 100 and 600 .mu.m. 

4. A composition according to claim 1, wherein the carrier particles comprise a brittle material which will fragmentize easily when compressed. 

5. A composition according to claim 1, wherein the carrier particles contain from 0.1 to 25 weight percent of the bio/mucoadhesion promoting agent. 

6. A composition according to claim 5, wherein the bio/mucoadhesion promoting agent is selected from the group consisting of acrylic polymers, cellulose derivatives, natural polymers having bio/mucoadhesive properties, and mixtures thereof. 

7. A composition according to claim 6, wherein the bio/mucoadhesion promoting agent is selected from the group consisting of cellulose derivatives and comprising hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, methyl cellulose, ethyl hydroxyethyl cellulose, carboxymethyl cellulose, and modified cellulose gum; crosscaramellose; modified starch; acrylic polymers comprising carbomer and its derivatives; polyethylene oxide; chitosan; gelatin; sodium alginate; pectin; scleroglucan; xanthan gum; guar gum; poly-co-(methyl vinyl ether-maleic anhydride); and mixtures thereof. 

8. A composition according to claim 1, further comprising a pharmaceutically acceptable surfactant in a finely dispersed form and intimately mixed with the active agent or agents. 

9. A composition according to claim 8, wherein the surfactant is present in an amount from 0.5 to 5 weight percent of the composition. 

10. A composition according to claim 8, wherein the surfactant is selected from the group consisting of sodium lauryl sulfate polysorbates, bile acid salts and mixtures thereof. 

11. A composition according to claim 1, wherein the carrier particles comprise a water-soluble, pharmaceutically acceptable carbohydrate and/or an inorganic salt. 

12. A composition according to claim 11, wherein the carrier particles comprise at least one of the materials mannitol, lactose, calcium phosphate and sugar. 

13. A composition according to claim 1, wherein the carrier particles contain at least one pharmaceutical disintegrating agent promoting the dispersion of the microparticles of the active agent or agents over the sublingual mucosa. 

14. A composition according to claim 13, wherein the disintegrating agent is selected from the group consisting of cross-linked polyvinylpyrrolidone, carboxymethyl starch, natural starch, microcrystalline cellulose, cellulose gum, and mixtures thereof. 

15. A composition according to claim 13, wherein the disintegrating agent is present in an amount from 1 to 10 weight percent of the composition. 

16. A composition according to claim 1, wherein the pharmaceutically active agent is fentanyl or a pharmaceutically acceptable salt thereof. 

17. A composition according to claim 1, for the treatment of acute disorders by sublingual administration. 

18. A composition according to claim 16, for the treatment of acute or breakthrough pain by sublingual administration of fentanyl or a pharmaceutically acceptable salt thereof. 

19. A method for the treatment of acute disorders, wherein to an individual afflicted with said disorder is administered sublingually at least one dose unit of an essentially water-free pharmaceutical composition containing an effective amount of at least one pharmaceutically active agent in the form of microparticles adhered to the surfaces of carrier particles, which are substantially larger than said microparticles and are essentially water-soluble, and a bioadhesion and/or mucoadhesion promoting agent. 

20. A method according to claim 19, wherein the pharmaceutically active agent is fentanyl or a pharmaceutically acceptable salt thereof. 

21. A method according to claim 20, wherein the fentanyl is administered in an amount from 0.05 to 20 mg.