Liquid formulations for treatment of diseases or conditions
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-038/13
A61K-031/436
A61K-031/045
A61K-047/10
A61K-009/00
A61K-047/44
A61K-031/44
A61K-031/4745
A61K-047/12
출원번호
US-0741103
(2013-01-14)
등록번호
US-8927005
(2015-01-06)
발명자
/ 주소
Mudumba, Sreenivasu
Dor, Philippe J M
Nivaggioli, Thierry
Weber, David A.
Farooq, Sidiq
출원인 / 주소
Santen Pharmaceutical Co., Ltd.
대리인 / 주소
Morrison & Foerster LLP
인용정보
피인용 횟수 :
1인용 특허 :
138
초록▼
Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; liquid formulations, compris
Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration in a subject.
대표청구항▼
1. A method for treating uveitis in a human subject, the method comprising administering to the human subject by periocular injection a volume of a liquid formulation comprising an effective amount of a therapeutic agent to treat uveitis in the human subject for at least one month, whereinthe liquid
1. A method for treating uveitis in a human subject, the method comprising administering to the human subject by periocular injection a volume of a liquid formulation comprising an effective amount of a therapeutic agent to treat uveitis in the human subject for at least one month, whereinthe liquid formulation comprises between 0.5% (w/w) to 6.0% (w/w) of the therapeutic agent, between 80% (w/w) to 99% (w/w) of polyethylene glycol, and ethanol,the therapeutic agent is rapamycin or a pharmaceutical acceptable salt thereof, andthe liquid formulation is a liquid solution that forms a non-dispersed mass when injected between the sclera and the conjunctiva. 2. The method of claim 1, wherein the periocular injection is subconjunctival injection. 3. The method of claim 1, wherein the at least one month is at least two months. 4. The method of claim 1, wherein the at least one month is at least three months. 5. The method of claim 1, wherein the polyethylene glycol and the ethanol diffuse out of the non-dispersed mass upon said injection leaving a precipitate of the therapeutic agent. 6. The method of claim 1, wherein the non-dispersed mass does not form a gel or gel-like substance upon injection. 7. The method of claim 1, wherein the liquid formulation has a viscosity of between 40 and 120 centipoise. 8. The method of claim 1, wherein the liquid formulation as a viscosity of between 60 and 80 centipoise. 9. The method of claim 1, wherein the therapeutic agent is rapamycin. 10. The method of claim 9, wherein the liquid formulation comprises about 2% (w/w) rapamycin, about 94% (w/w) PEG 400, and about 4% (w/w) ethanol. 11. The method of claim 9, wherein the volume of liquid formulation contains between 20 μg to 2 mg rapamycin. 12. The method of claim 1, wherein the therapeutic agent comprises between 0.628% to 5.233% of the total weight of the liquid formulation. 13. The method of claim 1, wherein the therapeutic agent comprises between 1% to 5% of the total weight of the liquid formulation. 14. The method of claim 1, wherein the polyethylene glycol is PEG 300 or PEG 400. 15. The method of claim 1, wherein the polyethylene glycol is PEG 400. 16. The method of claim 1, wherein the at least one month is from one to three months. 17. A method of administering a liquid formulation, the method comprising: administering to a human subject by periocular injection a volume of a liquid formulation comprising between 0.5% (w/w) to 6.0% (w/w) of a therapeutic agent, between 80% (w/w) to 99% (w/w) of polyethylene glycol, and ethanol, whereinthe therapeutic agent is rapamycin or a pharmaceutical acceptable salt thereof,the human subject has uveitis, andthe liquid formulation is a liquid solution that forms a non-dispersed mass when injected between the sclera and the conjunctiva. 18. The method of claim 17, wherein the administering is done once every two to three months. 19. The method of claim 17, wherein the therapeutic agent is rapamycin. 20. The method of claim 17, wherein the periocular injection is subconjunctival injection.
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