Sustained release small molecule drug formulation
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IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/14
A61K-031/519
A61K-009/06
A61K-009/16
A61K-009/00
A61K-051/12
출원번호
US-0422626
(2017-02-02)
등록번호
US-10058554
(2018-08-28)
발명자
/ 주소
Luk, Andrew S.
Junnarkar, Gunjan H.
Chen, Guohua
출원인 / 주소
Indivior UK Limited
대리인 / 주소
Mintz Levin Cohn Ferris Glovsky and Popeo, P.C.
인용정보
피인용 횟수 :
0인용 특허 :
135
초록▼
An injectable depot formulation includes a biocompatible polymer, an organic solvent combined with the biocompatible polymer to form a viscous gel, and a small molecule drug incorporated in the viscous gel such that the formulation exhibits an in vivo release profile having Cmax to Cmin ratio less t
An injectable depot formulation includes a biocompatible polymer, an organic solvent combined with the biocompatible polymer to form a viscous gel, and a small molecule drug incorporated in the viscous gel such that the formulation exhibits an in vivo release profile having Cmax to Cmin ratio less than 200 and lag time less than 0.2.
대표청구항▼
1. A method of administering risperidone base to a subject, comprising: implanting in the subject a formulation comprising:a copolymer of lactic acid and glycolic acid having a number average molecular weight ranging from 1000 Daltons to 30,000 Daltons;an organic solvent combined with the copolymer
1. A method of administering risperidone base to a subject, comprising: implanting in the subject a formulation comprising:a copolymer of lactic acid and glycolic acid having a number average molecular weight ranging from 1000 Daltons to 30,000 Daltons;an organic solvent combined with the copolymer to form a viscous gel, the organic solvent comprising N-methyl-2-pyrrolidone; andrisperidone base in particle form incorporated in the viscous gel,wherein the copolymer and the N-methyl-pyrrolidone comprise a vehicle, the copolymer is present in the vehicle in an amount ranging from 40% to 55% by weight, and the organic solvent is present in the vehicle in an amount ranging from 45% to 60% by weight. 2. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from about 100:0 to 60:40. 3. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from 100:0 to 75:25. 4. The method of claim 1, wherein the copolymer has a number average molecular weight ranging from 5000 Daltons to 30,000 Daltons. 5. The method of claim 1, wherein the organic solvent consists of N-methyl-2-pyrrolidone. 6. The method of claim 1, wherein the risperidone base is present in the formulation in an amount ranging from 5 wt % to 40 wt %. 7. The method of claim 1, wherein the risperidone base is present in the formulation in an amount ranging from 10 wt % to 30 wt %. 8. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from about 100:0 to 60:40, and the copolymer has a number average molecular weight ranging from 5000 Daltons to 30,000 Daltons. 9. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from 100:0 to 75:25, and the copolymer has a number average molecular weight ranging from 5000 Daltons to 30,000 Daltons. 10. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from about 100:0 to 60:40, and the organic solvent consists of N-methyl-2-pyrrolidone. 11. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from 100:0 to 75:25, the copolymer has a number average molecular weight ranging from 5000 Daltons to 30,000 Daltons, and the organic solvent consists of N-methyl-2-pyrrolidone. 12. The method of claim 1, wherein the organic solvent consists of N-methyl-2-pyrrolidone, and the risperidone base is present in the formulation in an amount ranging from 10 wt % to 30 wt %. 13. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from about 100:0 to 60:40, the organic solvent consists of N-methyl-2-pyrrolidone, and the risperidone base is present in the formulation in an amount ranging from 10 wt % to 30 wt %. 14. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from 100:0 to 75:25, the copolymer has a number average molecular weight ranging from 5000 Daltons to 30,000 Daltons, the organic solvent consists of N-methyl-2-pyrrolidone, and the risperidone base is present in the formulation in an amount ranging from 10 wt % to 30 wt %. 15. The method of claim 1, wherein the copolymer of lactic acid and glycolic acid has a monomer ratio of lactic acid to glycolic acid ranging from 100:0 to 75:25, the organic solvent consists of N-methyl-2-pyrrolidone, and the risperidone base is present in the formulation in an amount ranging from 10 wt % to 30 wt %. 16. The method of claim 1, wherein the formulation exhibits a lag time less than 0.2. 17. The method of claim 1, wherein the risperidone base in particle form comprises particles having an average particle size ranging from 0.1 μm to 125 μm. 18. The method of claim 1, wherein the risperidone base is released from the formulation for one week. 19. The method of claim 1, wherein the risperidone base is released from the formulation for one month. 20. The method of claim 1, wherein the risperidone base in particle form comprises particles having a particle size less than 38 μm.
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Dunn Richard L. (451 Boardwalk Dr. RLD ; Apt. 501 Fort Collins CO 80526) English James P. (2500 Melinda Cir. Birmingham AL 35214) Cowsar Donald R. (4657 Round Forest Dr. Birmingham AL 35213) Vanderbi, Biodegradable in-situ forming implants and methods of producing the same.
Dunn Richard L. (Fort Collins CO) English James P. (Birmingham AL) Cowsar Donald R. (Birmingham AL) Vanderbilt David P. (Birmingham AL), Biodegradable in-situ forming implants and methods of producing the same.
Dunn Richard L. (Fort Collins CO) Tipton Arthur J. (Fort Collins CO) Southard George L. (Fort Collins CO) Rogers Jack A. (Fort Collins CO), Biodegradable polymer composition.
Langer Robert S. (Somerville MA) Rosen Howard (Montara CA) Linhardt Robert J. (Iowa City IA) Leong Kam (Cambridge MA), Bioerodible polyanhydrides for controlled drug delivery.
Gavin, Paul; Gianello, Robert; Ogru, Esra, Carrier comprising one or more di and/or mono-(electron transfer agent) phosphate derivatives or complexes thereof.
Temtsin Krayz, Galia; Averbuch, Maryana; Zelkind, Ilya; Gitis, Larisa, Compositions comprising lipophilic active compounds and method for their preparation.
Drust Eugene G. (Norwich NY) Kasting Gerald B. (Wyoming OH) Smith Ronald L. (West Chester OH) Szkutak Joan B. (West Chester OH), Compositions for the transdermal delivery of pharmaceutical actives.
Chandrashekar Bhagya L. ; Zhou Mingxing ; Jarr Eileen M. ; Dunn Richard L., Controlled release liquid delivery compositions with low initial drug burst.
Gibson, John W.; Miller, Stacey S.; Middleton, John C.; Tipton, Arthur J., High viscosity liquid controlled delivery system and medical or surgical device.
John W. Gibson ; Stacey A. Sullivan ; John C. Middleton ; Arthur J. Tipton, High viscosity liquid controlled delivery system and medical or surgical device.
Tice Thomas R. (Birmingham AL) Lewis Danny H. (Gardendale AL) Cowsar Donald R. (Birmingham AL) Beck Lee R. (Birmingham AL), Injectable, long-acting microparticle formulation for the delivery of anti-inflammatory agents.
Cohen Smadar (Petach-Tickva ILX) Bano Carmen (Valencia PA ESX) Visscher Karyn B. (State College PA) Chow Marie (Brookline MA) Allcock Harry R. (State College PA) Langer Robert S. (Newton MA), Ionically cross-linked polymeric microcapsules.
Michal, Eugene T.; Lerner, Daniel J.; Pollman, Matthew J., Local delivery of water-soluble or water-insoluble therapeutic agents to the surface of body lumens.
Michal, Eugene T.; Lerner, Daniel J.; Pollman, Matthew J., Local delivery of water-soluble or water-insoluble therapeutic agents to the surface of body lumens.
Sinclair John D. (Espoo FIX), Method and means for treating alcoholism by extinguishing the alcohol-drinking response using a transdermally administer.
Steven G. Wright ; Michael E. Rickey ; J. Michael Ramstack ; Shawn L. Lyons ; Joyce M. Hotz, Method for preparing microparticles having a selected polymer molecular weight.
Wright Steven G. ; Rickey Michael E. ; Ramstack J. Michael ; Lyons Shawn L. ; Hotz Joyce M., Method for preparing microparticles having a selected polymer molecular weight.
Wright, Steven G.; Rickey, Michael E.; Ramstack, J. Michael; Lyons, Shawn L.; Hotz, Joyce M., Method for preparing microparticles having a selected polymer molecular weight.
Mesens Jean (Wechelderzande BEX) Rickey Michael E. (Loveland OH) Atkins Thomas J. (Cincinnati OH), Method of inhibiting neurotransmitter activity using microencapsulated 3-piperidiny2-substituted 1,2-benzisoxazoles and.
Cleland Jeffrey L. (San Carlos CA) Lim Amy (San Bruno CA) Powell Michael Frank (San Francisco CA), Methods and compositions for microencapsulation of adjuvants.
Gole Dilip J. (Ann Arbor MI) Levinson R. Saul (Chesterfield MO) Wilkinson Paul K. (Ann Arbor MI) Davies J. Desmond (Grosse Pointe Farms MI), Pharmaceutical and other dosage forms.
Dunn, Richard L.; Garrett, John Steven; Ravivarapu, Harish; Chandrashekar, Bhagya L, Polymeric delivery formulations of leuprolide with improved efficacy.
Dunn, Richard L.; Garrett, John Steven; Ravivarapu, Harish; Chandrashekar, Bhagya L., Polymeric delivery formulations of leuprolide with improved efficacy.
Michael E. Rickey ; J. Michael Ramstack ; Danny H. Lewis, Preparation of biodegradable, biocompatible microparticles containing a biologically active agent.
Rickey Michael E. ; Ramstack J. Michael ; Lewis Danny H., Preparation of biodegradable, biocompatible microparticles containing a biologically active agent.
Rickey Michael E. ; Ramstack J. Michael ; Lewis Danny H., Preparation of biodegradable, biocompatible microparticles containing a biologically active agent.
Rickey Michael E. ; Ramstack J. Michael ; Lewis Danny H., Preparation of biodegradable, biocompatible microparticles containing a biologically active agent.
Rickey Michael E. ; Ramstack J. Michael ; Lewis Danny H. ; Mesens Jean,BEX, Preparation of extended shelf-life biodegradable, biocompatible microparticles containing a biologically active agent.
Ramstack, J. Michael; Riley, M. Gary I.; Zale, Stephen E.; Hotz, Joyce M.; Johnson, Olufunmi L., Preparation of injectable suspensions having improved injectability.
Venkatasubramanian, Radhakrishnan Tarur; Govind, Sathe Dhananjay; Vasantrao, Suryavanshi Chandrakant, Process for the preparation of anti-psychotic 3-[2-[-4-(6-fluoro-1,2-benziosoxazol-3-yl)-1-piperidinyl] ethyl]-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one.
Kino Shigemi (Fukuoka JPX) Osajima Tomonori (Fukuoka JPX) Mizuta Hiroaki (Fukuoka JPX), Sustained release microsphere preparation containing antipsychotic drug and production process thereof.
Richard Sterling Tuthill ; William Theodore Bechtel, II ; Jeffrey Arthur Benoit ; Stephen Hugh Black ; Robert James Bland ; Guy Wayne DeLeonardo ; Stefan Martin Meyer ; Joseph Charles Taura ;, Swozzle based burner tube premixer including inlet air conditioner for low emissions combustion.
Chen Yu-Ling (Cupertino CA) Chun Leslie L. (Palo Alto CA) Enscore David J. (Sunnyvale CA), Transdermal therapeutic systems for the administration of naloxone, naltrexone and nalbuphine.
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