Injectable nanoparticulate olanzapine formulations 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
US2006154918 A1 2006-07-13 [US20060154918]US7910577 B2 2011-03-22 [US7910577] / 2006-07-132011-03-22
申请号/申请日
2005US-11274887 / 2005-11-16
发明人
LIVERSIDGE GARY;JENKINS SCOTT;LIVERSIDGE ELAINE MERISKO;
申请人
ALKERMES;ALKERMES CONTROLLED THERAPEUTICS;ALKERMES PHARMA IRELAND;
主分类号
IPC分类号
A01N-043/00A01N-043/46A61K-031/55C07D-243/10
摘要
(US7910577) Described are injectable formulations of nanoparticulate olanzapine that produce a prolonged duration of action upon administration, and methods of making and using such formulations.  The injectable formulations comprise nanoparticulate olanzapine.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2004US-60628748 2004-11-16 2005US-11274887 2005-11-16
主权利要求
(US7910577) What we claim is: 1.  An injectable nanoparticulate olanzapine composition comprising: (a) olanzapine nanoparticles having an effective average particle size that results in a therapeutic efficacy of about one week or greater; (b) at least one surface stabilizer; and (c) a pharmaceutically acceptable carrier, wherein said effective average particle size is between about 300 nm and about 5000 nm. 2. The composition of claim 1, wherein the composition is administered via intramuscular or subcutaneous injection so as to form a depot. 3. The composition of claim 2, wherein the depot releases the olanzapine at therapeutic levels for a period of time from about two to about six weeks. 4. The composition of claim 2, wherein the depot releases the olanzapine at therapeutic levels for a period of time from about two to about twelve weeks. 5. The composition of claim 2, wherein the depot releases the olanzapine at therapeutic levels for a period of time selected from one week to about two weeks, from about one week to about three weeks, from about one week to about four weeks, from about one week to about five weeks, from about one week to about six weeks, from about one week to about seven weeks, from about one week to about eight weeks, from about one week to about nine weeks, from about one week to about ten weeks, from about one week to about eleven weeks, or from about one week to about twelve weeks. 6. The composition of claim 1, wherein the olanzapine is selected from the group consisting of a crystalline phase, an amorphous phase, a semi-crystalline phase, a semi-amorphous phase, and mixtures thereof. 7. The composition of claim 1, wherein the effective average particle size of the olanzapine particles is about 4900 nm, about 4800 nm, about 4700 nm, about 4600 nm, about 4500 nm, about 4400 nm, about 4300 mm, about 4200 nm, about 4100 nm, about 4 microns, about 3900 nm, about 3800 nm, about 3700 nm, about 3600 nm, about 3500 nm, about 3400 mm, about 3300 nm, about 3200 nm, about 3100 nm, about 3 microns, about 2900 mm, about 2800 nm, about 2700 nm, about 2600 nm, about 2500 nm, about 2400 nm, about 2300 nm, about 2200 nm, about 2100 nm, about 2000 nm, about 1900 nm, about 1800 nm, about 1700 nm, about 1600 nm, about 1500 nm, about 1400 nm, about 1300 nm, about 1200 nm, about 1100 nm, about 1000 nm, about 900 nm, about 800 nm, about 700 nm, about 600 nm, about 500 nm, about 400 nm, or about 300 nm. 8. The composition of claim 1, wherein: (a) the olanzapine is present in an amount from about 99.5% to about 0.001%, from about 95% to about 0.1%, from about 90% to about 0.5%, and from about 5.0% to about 50%, by weight, based on the total combined weight of the olanzapine and at least one surface stabilizer, not including other excipients; and (b) the at least one surface stabilizer is present in an amount selected from the group consisting of from about 0.5% to about 99.999% by weight, from about 5.0% to about 99.9% by weight, from about 10% to about 99.5%, or from about 0.1 to about 50%, by weight, based on the total combined dry weight of the olanzapine and at least one surface stabilizer, not including other excipients. 9. The composition of claim 1, wherein the surface stabilizer is a non-ionic surface stabilizer, an anionic surface stabilizer, a cationic surface stabilizer, or a zwitterionic surface stabilizer. 10. The composition of claim 1, wherein at least one surface stabilizer is cetyl pyridinium chloride, gelatin, casein, phosphatides, dextran, glycerol, gum acacia, cholesterol, tragacanth, stearic acid, benzalkonium chloride, calcium stearate, glycerol monostearate, cetostearyl alcohol, cetomacrogol emulsifying wax, sorbitan esters, polyoxyethylene alkyl ethers, polyoxyethylene castor oils, polyoxyethylene sorbitan fatty acid esters, polyethylene glycols, dodecyl trimethyl ammonium bromide, polyoxyethylene stearates, colloidal silicon dioxide, phosphates, sodium dodecylsulfate, carboxymethylcellulose calcium, hydroxypropyl celluloses, hypromellose, carboxymethylcellulose sodium, methylcellulose, hydroxyethylcellulose, hypromello se phthalate, noncrystalline cellulose, magnesium aluminum silicate, triethanolamine, polyvinyl alcohol, polyvinylpyrrolidone, 4-(1,1,3,3-tetramethylbutyl)-phenol polymer with ethylene oxide and formaldehyde, poloxamers; poloxamines, a charged phospho lipid, dioctylsulfosuccinate, dialkylesters of sodium sulfosuccinic acid, sodium lauryl sulfate, alkyl aryl polyether sulfonates, mixtures of sucrose stearate and sucrose distearate, p-isononylphenoxypoly-(glycidol), decanoyl-N-methylglucamide; n-decyl-beta -D-glucopyranoside; n-decyl beta -D-maltopyranoside; n-dodecyl beta -D-glucopyranoside; n-dodecyl beta -D-maltoside; heptanoyl-N-methylglucamide; n-heptyl- beta -D-glucopyrano side; n-heptyl beta -D-thioglucoside; n-hexyl beta -D-glucopyranoside; nonanoyl-N-methylglucamide; n-noyl beta -D-glucopyranoside; octanoyl-N-methylglucamide; n-octyl- beta -D-glucopyranoside; octyl beta -D-thioglucopyranoside; lysozyme, PEG-phospholipid, PEG-cholesterols, PEG-vitamin A, random copolymers of vinyl acetate and vinyl pyrrolidone, cationic polymers, cationic biopolymers, cationic polysaccharides, cationic cellulosics, cationic alginates, cationic nonpolymeric compounds, cationic phospho lipids, cationic lipids, polymethylmethacrylate trimethylammonium bromide, sulfonium compounds, polyvinylpyrrolidone-2-dimethylaminoethyl methacrylate dimethyl sulfate, hexadecyltrimethyl ammonium bromide, phosphonium compounds, quarternary ammonium compounds, benzyl-di(2-chloroethyl)ethylammonium bromide, coconut trimethyl ammonium chloride, coconut trimethyl ammonium bromide, coconut methyl dihydroxyethyl ammonium chloride, coconut methyl dihydroxyethyl ammonium bromide, decyl triethyl ammonium chloride, decyl dimethyl hydroxyethyl ammonium chloride, decyl dimethyl hydroxyethyl ammonium chloride bromide, C12-15dimethyl hydroxyethyl ammonium chloride, C12-15dimethyl hydroxyethyl ammonium chloride bromide, coconut dimethyl hydroxyethyl ammonium chloride, coconut dimethyl hydroxyethyl ammonium bromide, myristyl trimethyl ammonium methyl sulphate, lauryl dimethyl benzyl ammonium chloride, lauryl dimethyl benzyl ammonium bromide, lauryl dimethyl (ethenoxy)4 ammonium chloride, lauryl dimethyl (ethenoxy)4 ammonium bromide, N-alkyl (C12-18)dimethylbenzyl ammonium chloride, N-alkyl (C14-18)dimethyl-benzyl ammonium chloride, N-tetradecylidmethylbenzyl ammonium chloride monohydrate, dimethyl didecyl ammonium chloride, N-alkyl and (C12-14) dimethyl 1-napthylmethyl ammonium chloride, trimethylammonium halide, alkyl-trimethylammonium salts, dialkyl-dimethylammonium salts, lauryl trimethyl ammonium chloride, ethoxylated alkyamidoalkyldialkylammonium salt, an ethoxylated trialkyl ammonium salt, dialkylbenzene dialkylammonium chloride, N-didecyldimethyl ammonium chloride, N-tetradecyldimethylbenzyl ammonium, chloride monohydrate, N-alkyl(C12-14) dimethyl 1-naphthylmethyl ammonium chloride, dodecyldimethylbenzyl ammonium chloride, dialkyl benzenealkyl ammonium chloride, lauryl trimethyl ammonium chloride, alkylbenzyl methyl ammonium chloride, alkyl benzyl dimethyl ammonium bromide, C12 trimethyl ammonium bromides, C15 trimethyl ammonium bromides, C12 trimethyl ammonium bromides, dodecylbenzyl triethyl ammonium chloride, poly-diallyldimethylammonium chloride (DADMAC), dimethyl ammonium chlorides, alkyldimethylammonium halogenides, tricetyl methyl ammonium chloride, decyltrimethylammonium bromide, dodecyltriethylammonium bromide, tetradecyltrimethylammonium bromide, methyl trioctylammonium chloride, Polyquaternium-10 (POLYQUAT 10 (Registered Trademark) ), tetrabutylammonium bromide, benzyl trimethylammonium bromide, choline esters, benzalkonium chloride, stearalkonium chloride compounds, cetyl pyridinium bromide, cetyl pyridinium chloride, halide salts of quaternized polyoxyethylalkylamines, Polyquaternium-11 (MIRAPOL (Registered Trademark) ), stearyl -dimethylbenzylammonium chloride (ALKAQUAT (Registered Trademark) ), alkyl pyridinium salts; amines, amine salts, amine oxides, imide azolinium salts, protonated quaternary acrylamides, methylated quaternary polymers, or cationic guar. 11. The composition of claim 1, comprising a surface stabilizer selected from the group consisting of a polysorbate, benzalkonium chloride, dextrose, and a combination thereof. 12. The composition of claim 1, further comprising at least one additional olanzapine composition having an effective average particle size which is different than the effective average particle size of the olanzapine composition of claim 1. 13. The composition of claim 1, additionally comprising one or more non-olanzapine active agents. 14. The composition of claim 13, wherein at least one non-olanzapine agent is an antidepressant. 15. The composition of claim 14, wherein the antidepressant is fluoxetine. 16. The composition of claim 1, wherein the composition is syringeable with a 23 gauge needle. 17. The composition of claim 1, wherein the effective average particle size of the olanzapine particles is less than 4900 nm, less than 4800 nm, less than 4700 nm, less than 4600 nm, less than 4500 nm, less than 4400 nm, less than 4300 mm, 4200 nm, less than 4100 nm, less than 4 microns, less than 3900 nm, less than 3800 nm, less than 3700 nm, less than 3600 nm, less than 3500 nm, less than 3400 mm, less than 3300 nm, less than 3200 nm, less than 3100 nm, less than 3 microns, less than 2900 mm, less than 2800 nm, less than 2700 nm, less than 2600 nm, less than 2500 nm, less than 2400 nm, less than 2300 nm, less than 2200 nm, less than 2100 nm, less than 2000 nm, less than 1900 nm, less than 1800 nm, less than 1700 nm, less than 1600 nm, less than 1500 nm, less than 1400 nm, less than 1300 nm, less than 1200 nm, less than 1100 nm, less than 1000 nm, less than 900 nm, less than 800 nm, less than 700 nm, less than 600 nm, less than 500 nm, or less than 400 nm.
法律状态
(US7910577) LEGAL DETAILS FOR US2006154918  Actual or expected expiration date=2029-01-26    Legal state=ALIVE    Status=GRANTED     Event publication date=2005-11-16  Event code=US/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=US US11274887  Application date=2005-11-16  Standardized application number=2005US-11274887     Event publication date=2005-11-16  Event code=US/EXMR  Event type=Administrative notifications  USPTO Examiner Name Primary Examiner: GREENE, IVAN A    Event publication date=2005-11-16  Event code=US/ART  Event type=Administrative notifications  USPTO Art Group  ART=1619     Event publication date=2005-11-16  Event code=US/ENT  Event type=Administrative notifications  Entity Status Set to Undiscounted Business Entity Status: UNDISCOUNTED    Event publication date=2005-11-16  Event code=US/AIA  Event type=Administrative notifications  First Inventor File Indicated:  AIA=No     Event publication date=2005-11-16  Event code=US/DK  Event type=Examination events  Attorney Docket Number Docket Nbr: 34074.00622/01.0123.US    Event publication date=2005-11-16  Event code=US/CUST  Event type=Examination events  Attorney/Agent Customer Number Customer Nbr: 61214    Event publication date=2005-12-20  Event code=US/INCD  Event type=Examination events  Event type=OAO  Notice Mailed--Application Incomplete--Filing Date Assigned    Event publication date=2006-03-20  Event code=US/FPAFF  Event type=Payment or non-payment notifications  Payment of additional filing fee/Preexam    Event publication date=2006-05-11  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2006-07-13  Event code=US/A1  Event type=Examination events  Application published  Publication country=US  Publication number=US2006154918  Publication stage Code=A1  Publication date=2006-07-13  Standardized publication number=US20060154918     Event publication date=2006-08-14  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: ELAN PHARMA INTERNATIONAL LIMITED, IRELAND  Effective date of the event=2006-03-20  ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNORS:LIVERSIDGE, GARY JENKINS, SCOTT LIVERSIDGE, ELAINE MERISKO REEL/FRAME:018181/0877     Event publication date=2006-08-14  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2006-10-24  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2008-03-14  Event code=US/PET  Event type=APL  Petition Entered    Event publication date=2008-03-14  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2008-04-07  Event code=US/POAC  Event type=Change of name or address  Change in Power of Attorney (May Include Associate POA)    Event publication date=2008-07-24  Event code=US/RESTREQ  Event type=Examination events  Event type=Corrections  Event type=OAO  Restriction/Election Requirement    Event publication date=2008-08-27  Event code=US/DISCSEF  Event type=OAI  Electronic Information Disclosure Statement    Event publication date=2008-08-27  Event code=US/ELC  Event type=Examination events  Event type=OAI  Response to Election / Restriction Filed    Event publication date=2008-08-27  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2008-09-05  Event code=US/POAC  Event type=Change of name or address  Change in Power of Attorney (May Include Associate POA)    Event publication date=2008-09-19  Event code=US/CTNF  Event type=Examination events  Event type=OA  Event type=OAO  Non-Final Rejection    Event publication date=2008-10-15  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2008-12-11  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2008-12-19  Event code=US/CTNFR  Event type=Examination events  Event type=OAI  Response after Non-Final Action    Event publication date=2009-03-16  Event code=US/CTFR  Event type=Examination events  Event type=OA  Event type=OAO  Final Rejection    Event publication date=2009-06-16  Event code=US/CTFAR  Event type=Examination events  Event type=OAI  Response after Final Action    Event publication date=2009-06-17  Event code=US/NOAPLF  Event type=APL  Notice of Appeal Filed    Event publication date=2009-06-24  Event code=US/CTAV  Event type=OAO  Advisory Action (PTOL-303)    Event publication date=2009-09-17  Event code=US/APB  Event type=APL  Event type=OAI  Appeal Brief Filed    Event publication date=2009-09-17  Event code=US/136G  Event type=OAO  Request for Extension of Time - Granted    Event publication date=2009-10-08  Event code=US/APLRVC  Event type=APL  Appeal Brief Review Complete    Event publication date=2009-12-19  Event code=US/APEA  Event type=APL  Event type=OAO  Examiner's Answer to Appeal Brief    Event publication date=2010-02-16  Event code=US/APE2  Event type=APL  2nd or Subsequent Examiner's Answer to Appeal Brief    Event publication date=2010-09-29  Event code=US/BPAIR  Event type=APL  BPAI Decision - Examiner Reversed    Event publication date=2010-10-26  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2010-11-16  Event code=US/NOAM  Event indicator=Pos  Event type=Examination events  Event type=OAO  Mail Notice of Allowance    Event publication date=2011-02-14  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: ELAN PHARMA INTERNATIONAL LIMITED, IRELAND  Effective date of the event=2006-01-04  NOTICE OF CHANGE OF ADDRESS ASSIGNOR:ELAN PHARMA INTERNATIONAL LIMITED REEL/FRAME:025785/0861     Event publication date=2011-02-15  Event code=US/APRDY  Event indicator=Pos  Event type=Examination events  Application Is Considered Ready for Issue    Event publication date=2011-03-02  Event code=US/PAT  Event indicator=Pos  Event type=Event indicating In Force  Patented Case    Event publication date=2011-03-02  Event code=US/ISSM  Event indicator=Pos  Event type=Examination events  Event type=OAO  Event type=Restitution or restoration  Issue Notification Mailed    Event publication date=2011-03-22  Event code=US/B2  Event indicator=Pos  Event type=Event indicating In Force  Granted patent as second publication  Publication country=US  Publication number=US7910577  Publication stage Code=B2  Publication date=2011-03-22  Standardized publication number=US7910577     Event publication date=2011-03-22  Event code=US/354  Event indicator=Pos  Event type=Extension of term of duration of protection  Patent term extended under  35 U.S.C 154(b) until/for:  Number of days of extension=1167    Event publication date=2011-05-23  Event code=US/PET  Event type=APL  Petition Entered    Event publication date=2011-06-14  Event code=US/PTEAD  Event type=Administrative notifications  Event type=Extension of term of duration of protection  Adjustment of PTE or PTA Calculation by PTO    Event publication date=2011-08-09  Event code=US/CC  Event type=Corrections  Event type=Restitution or restoration  Certificate of Correction - Post Issue Communication    Event publication date=2011-09-29  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: MORGAN STANLEY SENIOR FUNDING, INC., NEW YORK  Effective date of the event=2011-09-16  PATENT SECURITY AGREEMENT (FIRST LIEN) ASSIGNORS:ALKERMES, INC. ALKERMES PHARMA IRELAND LIMITED ALKERMES CONTROLLED THERAPEUTICS INC. REEL/FRAME:026994/0186     Event publication date=2011-09-29  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: MORGAN STANLEY SENIOR FUNDING, INC., NEW YORK  Effective date of the event=2011-09-16  PATENT SECURITY AGREEMENT (SECOND LIEN) ASSIGNORS:ALKERMES, INC. ALKERMES PHARMA IRELAND LIMITED ALKERMES CONTROLLED THERAPEUTICS INC. REEL/FRAME:026994/0245     Event publication date=2012-09-07  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: EDT PHARMA HOLDINGS LIMITED, IRELAND  Effective date of the event=2011-08-02  ASSET TRANSFER AGREEMENT ASSIGNOR:ELAN PHARMA INTERNATIONAL LIMITED REEL/FRAME:028921/0442     Event publication date=2012-09-07  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: EDT PHARMA HOLDINGS, IRELAND  Effective date of the event=2011-08-15  NOTICE OF CHANGE IN REGISTERED OFFICE ADDRESS ASSIGNOR:EDT PHARMA HOLDINGS REEL/FRAME:028921/0475     Event publication date=2012-09-07  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: ALKERMES PHARMA IRELAND LIMITED, IRELAND  Effective date of the event=2011-09-14  CHANGE OF NAME ASSIGNOR:EDT PHARMA HOLDINGS LIMITED REEL/FRAME:028923/0247     Event publication date=2012-09-07  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: ALKERMES PHARMA IRELAND LIMITED, IRELAND  Effective date of the event=2012-02-23  NOTICE OF CHANGE IN REGISTERED OFFICE ADDRESS ASSIGNOR:ALKERMES PHARMA IRELAND LIMITED REEL/FRAME:028921/0519     Event publication date=2012-10-12  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment Owner: ALKERMES CONTROLLED THERAPEUTICS INC., MASSACHUSET  Effective date of the event=2012-09-24  RELEASE BY SECURED PARTY (SECOND LIEN) ASSIGNOR:MORGAN STANLEY SENIOR FUNDING, INC. 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