발생일자 2015.01.14 

사건번호 1:15-cv-00043 

법원국가 UNITED STATES OF AMERICA 

관할법원명 D.C.Delaware(지방법원) 

침해권리 특허 

원고명 Horizon Pharma Ireland Limited/ Horizon Pharma USA Inc/ HZNP Limited ( 아일랜드 / 외국기업 )  

피고명 Paddock Laboratories, LLC/ Perrigo Company ( 미국 / 외국기업 )  

소송유형 침해금지 

[Horizon Pharma Ireland Limited et al v. Paddock Laboratories, LLC et al] 사건번호 1:15-cv-00043에 따르면 원고 Horizon Pharma Ireland Limited/ Horizon Pharma USA Inc/ HZNP Limited는 피고 Paddock Laboratories, LLC/ Perrigo Company을 상대로 특허 US8217078, US8252838, US8546450, US8563613, US8618164, US8871809 을 침해하였다는 이유로 미국 델라웨어 지방법원에 소를 제기하였다. 

분쟁결과 분쟁중 

산업분류 화학∙바이오 > 기초재료화학기술 

계쟁제품 Diclofenac sodium topical solution 2% w/w - Generic version PENNSAID� 

지재권번호/명칭

 US8217078   Treatment of pain with topical diclofenac 

 US8252838   Diclofenac topical formulation 

 US8546450   Treatment of pain with topical diclofenac compounds 

 US8563613   Diclofenac topical formulation 

 US8618164   Treatment of pain with topical diclofenac compounds 

 US8871809   Diclofenac topical formulation 

The field involves compositions useful for pain relief, including diclofenac solution and gel formulations, in particular methods of use thereof, articles of manufacture and kits that provide novel preclinical, clinical and other information to users. 

What is claimed is: 

 1. A method for applying topical agents to a knee of a patient with pain, said method comprising: applying a first medication consisting of a topical diclofenac preparation to an area of the knee of said patient to treat osteoarthritis of the knee of said patient, wherein the topical diclofenac preparation comprises a therapeutically effective amount of diclofenac and 40-50% w/w dimethyl sulfoxide; waiting for the treated area to dry; and subsequently applying a second medication consisting of a topical medication, which is other than said first medication and is selected from the group consisting of an NSAID, tretinoin, minoxidil, a corticosteroid, to said treated area after said treated area is dry, wherein said subsequent application occurs during a course of treatment of said patient with said topical diclofenac preparation. 

 2. The method according to claim 1, wherein said diclofenac preparation comprises about 45.5% w/w dimethyl sulfoxide. 

 3. The method according to claim 1, wherein said therapeutically effective amount of diclofenac is 1.5% w/w diclofenac sodium. 

 4. The method according to claim 1, wherein said diclofenac preparation further comprises ethanol, propylene glycol, glycerine, and water. 

 5. The method according to claim 1, wherein said therapeutically effective amount of diclofenac comprises a pharmaceutically acceptable salt of diclofenac selected from a sodium salt, a potassium salt, a diethylamine salt, or an epolamine salt. 

 6. The method according to claim 1, wherein said step of subsequently applying comprises subsequently applying said second medication, which is an NSAID. 

 7. The method according to claim 6, wherein said topical medication other than said first medication comprises a medical compound or composition in an amount sufficient to induce a desired biological, pharmaceutical, or therapeutic result, wherein the result relates to alleviation of a sign, a symptom, or a cause of a disease or disorder or condition, or any other desired alteration of a biological system. 

 8. The method according to claim 1, wherein the topical medication other than said first medication is tretinoin. 

 9. The method according to claim 5, wherein said therapeutically effective amount of diclofenac comprises diclofenac sodium. 

 10. The method according to claim 1, wherein the topical medication other than said first medication is minoxidil. 

 11. The method according to claim 1, wherein the topical medication other than said first medication is a corticosteroid. 

 12. A method for applying topical agents to a knee of a patient with pain, said method comprising: applying a first medication consisting of a topical diclofenac preparation to an area of the knee of said patient to treat osteoarthritis of the knee of said patient, wherein the topical diclofenac preparation comprises a therapeutically effective amount of diclofenac and 40-50% w/w dimethyl sulfoxide; waiting for the treated area to dry; and subsequently applying a second medication consisting of a topical medication, which is other than said first medication and comprises an NSAID, to said treated area after said treated area is dry, wherein said subsequent application occurs during a course of treatment of said patient with said topical diclofenac preparation. 

 13. The method according to claim 12, wherein said therapeutically effective amount of diclofenac is 1.5% w/w diclofenac sodium. 

 14. A method for applying topical agents to a knee of a patient with pain, said method comprising: applying a first medication consisting of a topical diclofenac preparation to an area of the knee of said patient to treat osteoarthritis of the knee of said patient, wherein the topical diclofenac preparation comprises a therapeutically effective amount of diclofenac and 40-50% w/w dimethyl sulfoxide; waiting for the treated area to dry; and subsequently applying a second medication consisting of a topical medication, which is other than said first medication and comprises a corticosteroid, to said treated area after said treated area is dry, wherein said subsequent application occurs during a course of treatment of said patient with said topical diclofenac preparation. 

 15. The method according to claim 14, wherein said therapeutically effective amount of diclofenac is 1.5% w/w diclofenac sodium. 

The present invention provides a gel formulation comprising diclofenac sodium which has superior transdermal flux properties, which may be used for the topical treatment of pain, such as in osteoarthritis. 

Treatment of pain with topical diclofenac compounds 

The field involves compositions useful for pain relief, including diclofenac solution and gel formulations, in particular methods of use thereof, articles of manufacture and kits that provide novel preclinical, clinical and other information to users. 

 1. A method for treating a patient with combination therapy, said combination therapy comprising: administering a therapeutically effective amount of an oral NSAID; and applying a topical diclofenac preparation to a knee of said patient to treat osteoarthritis of the knee of said patient, wherein said topical diclofenac preparation comprises a therapeutically effective amount of a diclofenac salt and 40-50% w/w dimethyl sulfoxide, wherein the therapeutically effective amount of oral NSAID is the amount required to achieve a therapeutic effect in the absence of applying a topical diclofenac preparation. 

 2. The method according to claim 1, wherein the patient is treated for severe knee pain. 

 3. The method according to claim 1, wherein the patient is treated for breakthrough knee pain. 

 4. The method according to claim 1, further comprising: conducting periodic laboratory evaluations regarding said patient and the combination therapy. 

 5. The method according to claim 1, wherein said diclofenac preparation comprises about 45.5% w/w dimethyl sulfoxide. 

 6. The method according to claim 1, wherein said diclofenac preparation further comprises ethanol, propylene glycol, glycerine, and water. 

 7. The method according to claim 1, wherein said therapeutically effective amount of diclofenac comprises a pharmaceutically acceptable salt of diclofenac selected from a sodium salt, a potassium salt, a diethylamine salt, or an epolamine salt. 

 8. The method according to claim 1, wherein said therapeutically effective amount of diclofenac is 1.5% w/w diclofenac sodium. 

 9. The method according to claim 1, wherein said oral NSAID is a member selected from the group consisting of a COX-2 selective NSAID, diclofenac, tenoxicam, meloxicam, celecoxib, diflunisal, etodolac, fenoprofen, flurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, mefenamic acid, nabumetone, naproxen, oxaprozin, piroxicam, sulindac, and tolmetin. 

 10. A method for applying topical agents to a knee of a patient with pain, said method comprising: applying a first medication consisting of a topical diclofenac preparation to an area of the knee of said patient to treat osteoarthritis of the knee of said patient, wherein the topical diclofenac preparation comprises a therapeutically effective amount of a diclofenac salt and 40-50% w/w dimethyl sulfoxide; waiting for the treated area to dry; subsequently applying a sunscreen, or an insect repellant to said treated area after said treated area is dry, wherein said step of applying a first medication does not enhance the systemic absorption of the subsequently applied sunscreen, or insect repellant; and wherein said subsequent application occurs during a course of treatment of said patient with said topical diclofenac preparation. 

 11. The method according to claim 10, wherein said diclofenac preparation comprises about 45.5% w/w dimethyl sulfoxide. 

 12. The method according to claim 10, wherein said therapeutically effective amount of diclofenac is 1.5% w/w diclofenac sodium. 

 13. The method according to claim 10, wherein said diclofenac preparation further comprises ethanol, propylene glycol, glycerine, and water. 

 14. The method according to claim 10, wherein said therapeutically effective amount of diclofenac comprises a pharmaceutically acceptable salt of diclofenac selected from a sodium salt, a potassium salt, a diethylamine salt, or an epolamine salt. 

 15. The method according to claim 10, wherein said step of subsequently applying comprises subsequently applying said sunscreen. 

 16. The method according to claim 15, wherein said sunscreen comprises oxybenzone. 

 17. The method according to claim 10, wherein said step of subsequently applying comprises subsequently applying said insect repellant. 

 18. The method according to claim 17, wherein said insect repellant comprises N,N-diethyl-m-toluamide (DEET). 

 19. The method according to claim 17, wherein said insect repellant comprises 2,4 D dimethylamine salt (2,4 D). 

 20. The method according to claim 14, wherein said therapeutically effective amount of diclofenac comprises diclofenac sodium. 

The field involves compositions useful for pain relief, including diclofenac solution and gel formulations, in particular methods of use thereof, articles of manufacture and kits that provide novel preclinical, clinical and other information to users. 

 1. A method for applying topical agents to a knee of a patient with pain, said method comprising: applying a first medication comprising a topical diclofenac preparation to an area of the knee of said patient to treat osteoarthritis of the knee of said patient, wherein the topical diclofenac preparation comprises a therapeutically effective amount of diclofenac or a pharmaceutically acceptable salt thereof, and 40-50% w/w dimethyl sulfoxide; waiting for the treated area to dry; and subsequently applying a second prescription medication consisting of a topical medication other than said first medication to said treated area after said treated area is dry, wherein said subsequent application occurs during a course of treatment of said patient with said topical diclofenac preparation. 

 2. The method according to claim 1, wherein said diclofenac preparation comprises about 45.5% w/w dimethyl sulfoxide. 

 3. The method according to claim 1, wherein said therapeutically effective amount of diclofenac is 1.5% w/w diclofenac sodium. 

 4. The method according to claim 1, wherein said diclofenac preparation further comprises ethanol, propylene glycol, glycerine, and water. 

 5. The method according to claim 1, wherein said therapeutically effective amount of diclofenac comprises a pharmaceutically acceptable salt of diclofenac selected from a sodium salt, a potassium salt, a diethylamine salt, or an epolamine salt. 

 6. The method according to claim 5, wherein said therapeutically effective amount of diclofenac comprises diclofenac sodium. 

 7. The method according to claim 1, wherein said step of applying a first medication does not enhance the systemic absorption of the subsequently applied second medication consisting of a topical medication other than said first medication. 

 8. A method for applying topical agents to a knee of a patient with pain, said method comprising: applying a first medication comprising a topical diclofenac preparation to an area of the knee of said patient to treat osteoarthritis of the knee of said patient, wherein the topical diclofenac preparation comprises a therapeutically effective amount of diclofenac and 40-50% w/w dimethyl sulfoxide; waiting for the treated area to dry; subsequently applying a second prescription medication consisting of a topical medication other than said first medication to said treated area after said treated area is dry, wherein said subsequent application occurs during a course of treatment of said patient with said topical diclofenac preparation; and wherein said step of applying a first medication does not enhance the systemic absorption of the subsequently applied second prescription medication consisting of a topical medication other than said first medication. 

Diclofenac topical formulation 

Abstract

The present invention provides a gel formulation comprising diclofenac sodium which has superior transdermal flux properties, which may be used for the topical treatment of pain, such as in osteoarthritis. 

 1. A method for treating pain, said method comprising: administering a formulation, the formulation comprising: diclofenac sodium present at 1-5% w/w; DMSO present at 25% to 60% w/w; and a viscosity of 500-5000 centipoise, wherein the administration of the formulation is twice daily, to thereby effectively treat pain. 

 2. The method of claim 1, wherein the formulation comprises: (i) 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, or 5.0% w/w and all fractions in between, of diclofenac sodium; (ii) 30-60% w/w of DMSO; (iii) 1-15% w/w of propylene glycol; (iv) 1-30% w/w of ethanol; (v) optionally glycerine; (vi) water; (vii) at least one thickening agent selected from the group consisting of a cellulose polymer, a carbomer polymer, a carbomer derivative, a cellulose derivative, and mixtures thereof. 

 3. The method of claim 1, wherein the concentration of diclofenac sodium is a member selected from the group consisting of 1%, 1.5% and 2% w/w, and all fractions in between. 

 4. The method of claim 2, wherein the concentration of DMSO is about 40% to about 50% w/w. 

 5. The method of claim 4, wherein the concentration of DMSO is a member selected from the group consisting of 40%, 41%, 42%, 43%, 44%, 45%, 46%, 47%, 48%, 49% and 50% w/w, and all fractions in between. 

 6. The method of claim 2, wherein the concentration of ethanol is present at 23-29% w/w. 

 7. The method of claim 2, wherein the at least one thickening agent is selected from the group consisting of a carbomer polymer, a carbomer derivative and mixtures thereof. 

 8. The method of claim 7, wherein the at least one thickening agent is selected from the group consisting of carbopol 971, carbopol 981, carbopol 941, carbopol 1342 and ultrez 10. 

 9. The method of claim 7, wherein glycerine is present. 

 10. The method of claim 2, wherein the at least one thickening agent is selected from the group consisting of a cellulose polymer, a cellulose derivative, and mixtures thereof. 

 11. The method of claim 10, wherein the at least one thickening agent is hydroxypropyl cellulose. 

 12. The method of claim 11, wherein the formulation comprises: (i) 1.5, 2.0, 2.5, 3.0, 3.5, 4.0 or 5.0% w/w, and all fractions in between, of diclofenac sodium; (ii) 40-50% w/w of DMSO; (iii) 23-29% w/w of ethanol; and (iv) 10-12% w/w of propylene glycol. 

 13. The method of claim 12, wherein the concentration of diclofenac sodium is a member selected from the group consisting of 1.5% and 2% w/w, and all fractions in between. 

 14. The method of claim 12, wherein the concentration of DMSO is a member selected from the group consisting of 40%, 41%, 42%, 43%, 44%, 45%, 46%, 47%, 48%, 49% and 50% w/w, and all fractions in between. 

 15. The method of claim 12, wherein the concentration of ethanol is present at 26.5% w/w. 

 16. The method of claim 1, wherein the formulation has improved absorption on a per dose basis compared to a comparative liquid composition. 

 17. The method of claim 1, wherein the pain is due to osteoarthritis.