JP2011511818A5 - - Google Patents
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- Publication number
- JP2011511818A5 JP2011511818A5 JP2010546257A JP2010546257A JP2011511818A5 JP 2011511818 A5 JP2011511818 A5 JP 2011511818A5 JP 2010546257 A JP2010546257 A JP 2010546257A JP 2010546257 A JP2010546257 A JP 2010546257A JP 2011511818 A5 JP2011511818 A5 JP 2011511818A5
- Authority
- JP
- Japan
- Prior art keywords
- hypromellose
- nominal viscosity
- release system
- flibanserin
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229920003125 hypromellose 2910 Polymers 0.000 claims 13
- 229940031672 hypromellose 2910 Drugs 0.000 claims 13
- PPRRDFIXUUSXRA-UHFFFAOYSA-N flibanserin Chemical compound FC(F)(F)C1=CC=CC(N2CCN(CCN3C(NC4=CC=CC=C43)=O)CC2)=C1 PPRRDFIXUUSXRA-UHFFFAOYSA-N 0.000 claims 12
- 229960002053 flibanserin Drugs 0.000 claims 12
- 229920000609 methyl cellulose Polymers 0.000 claims 10
- 239000001923 methylcellulose Substances 0.000 claims 10
- 235000010981 methylcellulose Nutrition 0.000 claims 10
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 8
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims 8
- 239000004480 active ingredient Substances 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 5
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 5
- 229960003943 hypromellose Drugs 0.000 claims 5
- 229920003130 hypromellose 2208 Polymers 0.000 claims 5
- 229940031707 hypromellose 2208 Drugs 0.000 claims 5
- 239000003002 pH adjusting agent Substances 0.000 claims 5
- 239000011975 tartaric acid Substances 0.000 claims 5
- 235000002906 tartaric acid Nutrition 0.000 claims 5
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 4
- 238000001125 extrusion Methods 0.000 claims 4
- 239000001530 fumaric acid Substances 0.000 claims 4
- 235000011087 fumaric acid Nutrition 0.000 claims 4
- 239000004310 lactic acid Substances 0.000 claims 4
- 235000014655 lactic acid Nutrition 0.000 claims 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 4
- 208000006262 Psychological Sexual Dysfunctions Diseases 0.000 claims 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 230000001568 sexual effect Effects 0.000 claims 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 claims 2
- 201000001880 Sexual dysfunction Diseases 0.000 claims 2
- 208000027520 Somatoform disease Diseases 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 2
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 239000000155 melt Substances 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 208000027753 pain disease Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 239000003340 retarding agent Substances 0.000 claims 2
- 230000000979 retarding effect Effects 0.000 claims 2
- 231100000872 sexual dysfunction Toxicity 0.000 claims 2
- 238000013268 sustained release Methods 0.000 claims 2
- 239000012730 sustained-release form Substances 0.000 claims 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 1
- 208000000103 Anorexia Nervosa Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 206010013954 Dysphoria Diseases 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000008238 Muscle Spasticity Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000029899 Sexual aversion disease Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 239000001361 adipic acid Substances 0.000 claims 1
- 235000011037 adipic acid Nutrition 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 239000011668 ascorbic acid Substances 0.000 claims 1
- 235000010323 ascorbic acid Nutrition 0.000 claims 1
- 229960005070 ascorbic acid Drugs 0.000 claims 1
- 235000003704 aspartic acid Nutrition 0.000 claims 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 208000022371 chronic pain syndrome Diseases 0.000 claims 1
- 235000015165 citric acid Nutrition 0.000 claims 1
- 230000007423 decrease Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000018578 heart valve disease Diseases 0.000 claims 1
- 239000001630 malic acid Substances 0.000 claims 1
- 235000011090 malic acid Nutrition 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 claims 1
- 229960002900 methylcellulose Drugs 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000004112 neuroprotection Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000022821 personality disease Diseases 0.000 claims 1
- 239000004014 plasticizer Substances 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 1
- 230000035946 sexual desire Effects 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 230000007958 sleep Effects 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000018198 spasticity Diseases 0.000 claims 1
- 238000001694 spray drying Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 239000001384 succinic acid Substances 0.000 claims 1
- 235000011044 succinic acid Nutrition 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08101599A EP2090297A1 (en) | 2008-02-13 | 2008-02-13 | Formulations of flibanserin |
| PCT/EP2009/000941 WO2009100886A2 (en) | 2008-02-13 | 2009-02-11 | Formulations of flibanserin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011511818A JP2011511818A (ja) | 2011-04-14 |
| JP2011511818A5 true JP2011511818A5 (enExample) | 2012-03-29 |
Family
ID=39431170
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010546257A Pending JP2011511818A (ja) | 2008-02-13 | 2009-02-11 | フリバンセリンの製剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US20110045090A1 (enExample) |
| EP (2) | EP2090297A1 (enExample) |
| JP (1) | JP2011511818A (enExample) |
| CN (1) | CN101951894A (enExample) |
| AR (1) | AR070367A1 (enExample) |
| BR (1) | BRPI0908455A2 (enExample) |
| CA (1) | CA2714542A1 (enExample) |
| CL (1) | CL2009000322A1 (enExample) |
| IL (1) | IL206577A0 (enExample) |
| MX (1) | MX2010008852A (enExample) |
| PE (1) | PE20091418A1 (enExample) |
| TW (1) | TW200940057A (enExample) |
| WO (1) | WO2009100886A2 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120301541A1 (en) * | 2011-05-24 | 2012-11-29 | Haronsky Elina | Compressed core for pharmaceutical composition |
| TN2016000484A1 (en) * | 2014-05-29 | 2018-04-04 | Novartis Ag | Ceritinib formulation. |
| CN104926734B (zh) * | 2015-07-07 | 2017-04-05 | 苏州立新制药有限公司 | 氟班色林的制备方法 |
| WO2017026950A1 (en) * | 2015-08-07 | 2017-02-16 | Santa Farma Ilac San. A. S. | Controlled release propiverine formulations |
| WO2017055935A1 (en) * | 2015-09-30 | 2017-04-06 | Symed Labs Limited | Amorphous co-precipitates of flibanserin |
| CN106866546A (zh) * | 2015-12-10 | 2017-06-20 | 常州爱诺新睿医药技术有限公司 | 氟班色林或其药学上可接受的盐与药用辅料的固体分散体及其制备方法 |
| CN110251475B (zh) * | 2019-07-25 | 2021-07-16 | 沈阳信康药物研究有限公司 | 一种帕利哌酮片剂及其制备方法 |
| KR102816429B1 (ko) * | 2020-12-31 | 2025-06-04 | 서울대학교 산학협력단 | 퇴행성 신경질환 치료용 조성물 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1251144B (it) | 1991-07-30 | 1995-05-04 | Boehringer Ingelheim Italia | Derivati del benzimidazolone |
| DE19961334A1 (de) * | 1999-12-17 | 2001-06-21 | Roehm Gmbh | Spritzgußverfahren für neutrale und säuregruppenhaltige (Meth)acrylat-Copolymere |
| AU2002331361B2 (en) | 2001-08-02 | 2008-06-05 | Sprout Pharmaceuticals, Inc. | Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments |
| DE10209982A1 (de) * | 2002-03-07 | 2003-09-25 | Boehringer Ingelheim Pharma | Oral zu applizierende Darreichungsform für schwerlösliche basische Wirkstoffe |
| RS51718B (sr) * | 2002-05-22 | 2011-10-31 | Boehringer Ingelheim Pharma Gmbh. & Co.Kg. | Nove farmaceutske kompozicije koje sadrže flibanserin polimorf a |
| WO2006010640A1 (en) * | 2004-07-29 | 2006-02-02 | Sanofi-Aventis | Pharmaceutical multilayer tablet for controlled release of active ingredients with highly ph-dependent solubility |
| EP1896002A4 (en) * | 2005-06-27 | 2009-11-25 | Biovail Lab Int Srl | BUPROPIONAL SALT FORMULATIONS WITH MODIFIED RELEASE |
| FR2887455B1 (fr) * | 2005-06-28 | 2007-08-10 | Sanofi Aventis Sa | Formulation a liberation prolongee de principes actifs de medicaments |
| US20080275082A1 (en) * | 2005-09-30 | 2008-11-06 | Jeffrey Brum | Pharmaceutical Composition |
| AU2007211091B8 (en) * | 2006-01-27 | 2013-08-29 | Adare Pharmaceuticals, Inc. | Drug delivery systems comprising weakly basic selective serotonin 5-HT3 blocking agent and organic acids |
| KR20090042967A (ko) * | 2006-08-14 | 2009-05-04 | 베링거 인겔하임 인터내셔날 게엠베하 | 플리반세린 제형 및 이의 제조방법 |
| CN104721168A (zh) * | 2006-08-25 | 2015-06-24 | 贝林格尔·英格海姆国际有限公司 | 控制释放系统及其制造方法 |
| US8486452B2 (en) * | 2007-07-20 | 2013-07-16 | Mylan Pharmaceuticals Inc. | Stabilized tolterodine tartrate formulations |
-
2008
- 2008-02-13 EP EP08101599A patent/EP2090297A1/en not_active Withdrawn
-
2009
- 2009-02-11 JP JP2010546257A patent/JP2011511818A/ja active Pending
- 2009-02-11 EP EP09709701A patent/EP2252270A2/en not_active Withdrawn
- 2009-02-11 MX MX2010008852A patent/MX2010008852A/es not_active Application Discontinuation
- 2009-02-11 US US12/867,097 patent/US20110045090A1/en not_active Abandoned
- 2009-02-11 CN CN2009801052034A patent/CN101951894A/zh active Pending
- 2009-02-11 CA CA2714542A patent/CA2714542A1/en not_active Abandoned
- 2009-02-11 BR BRPI0908455A patent/BRPI0908455A2/pt not_active IP Right Cessation
- 2009-02-11 WO PCT/EP2009/000941 patent/WO2009100886A2/en not_active Ceased
- 2009-02-11 PE PE2009000195A patent/PE20091418A1/es not_active Application Discontinuation
- 2009-02-12 TW TW098104529A patent/TW200940057A/zh unknown
- 2009-02-12 AR ARP090100504A patent/AR070367A1/es unknown
- 2009-02-12 CL CL2009000322A patent/CL2009000322A1/es unknown
-
2010
- 2010-06-23 IL IL206577A patent/IL206577A0/en unknown
-
2012
- 2012-10-22 US US13/657,147 patent/US20130209519A1/en not_active Abandoned
-
2014
- 2014-12-15 US US14/570,467 patent/US20150224058A1/en not_active Abandoned
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