CA2652300A1 - Pharmaceutical formulations of pimavanserin - Google Patents
Pharmaceutical formulations of pimavanserin Download PDFInfo
- Publication number
- CA2652300A1 CA2652300A1 CA002652300A CA2652300A CA2652300A1 CA 2652300 A1 CA2652300 A1 CA 2652300A1 CA 002652300 A CA002652300 A CA 002652300A CA 2652300 A CA2652300 A CA 2652300A CA 2652300 A1 CA2652300 A1 CA 2652300A1
- Authority
- CA
- Canada
- Prior art keywords
- composition
- weight
- pimavanserin
- pharmaceutical composition
- magnesium stearate
- 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.)
- Abandoned
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 62
- RKEWSXXUOLRFBX-UHFFFAOYSA-N pimavanserin Chemical compound C1=CC(OCC(C)C)=CC=C1CNC(=O)N(C1CCN(C)CC1)CC1=CC=C(F)C=C1 RKEWSXXUOLRFBX-UHFFFAOYSA-N 0.000 title claims abstract description 53
- 229960003300 pimavanserin Drugs 0.000 title claims abstract description 51
- 239000000203 mixture Substances 0.000 claims description 217
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 155
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 115
- 235000019359 magnesium stearate Nutrition 0.000 claims description 77
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 76
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 74
- RGSULKHNAKTFIZ-CEAXSRTFSA-N pimavanserin tartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(OCC(C)C)=CC=C1CNC(=O)N(C1CCN(C)CC1)CC1=CC=C(F)C=C1.C1=CC(OCC(C)C)=CC=C1CNC(=O)N(C1CCN(C)CC1)CC1=CC=C(F)C=C1 RGSULKHNAKTFIZ-CEAXSRTFSA-N 0.000 claims description 66
- 238000009472 formulation Methods 0.000 claims description 62
- 229940081770 pimavanserin tartrate Drugs 0.000 claims description 53
- 238000000034 method Methods 0.000 claims description 46
- 229920000881 Modified starch Polymers 0.000 claims description 45
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims description 38
- 150000001875 compounds Chemical class 0.000 claims description 38
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 36
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 36
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 35
- 239000008101 lactose Substances 0.000 claims description 35
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 32
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- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 25
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- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 21
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- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 15
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- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 15
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- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 13
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 13
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- RGCVKNLCSQQDEP-UHFFFAOYSA-N Perphenazine Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 RGCVKNLCSQQDEP-UHFFFAOYSA-N 0.000 claims description 7
- RMEDXOLNCUSCGS-UHFFFAOYSA-N droperidol Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CC=C(N2C(NC3=CC=CC=C32)=O)CC1 RMEDXOLNCUSCGS-UHFFFAOYSA-N 0.000 claims description 7
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- YVUQSNJEYSNKRX-UHFFFAOYSA-N pimozide Chemical compound C1=CC(F)=CC=C1C(C=1C=CC(F)=CC=1)CCCN1CCC(N2C(NC3=CC=CC=C32)=O)CC1 YVUQSNJEYSNKRX-UHFFFAOYSA-N 0.000 claims description 4
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80086406P | 2006-05-15 | 2006-05-15 | |
| US60/800,864 | 2006-05-15 | ||
| US85466506P | 2006-10-26 | 2006-10-26 | |
| US60/854,665 | 2006-10-26 | ||
| PCT/US2007/011720 WO2007133802A2 (en) | 2006-05-15 | 2007-05-15 | Pharmaceutical formulations of pimavanserin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2652300A1 true CA2652300A1 (en) | 2007-11-22 |
Family
ID=38669082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002652300A Abandoned CA2652300A1 (en) | 2006-05-15 | 2007-05-15 | Pharmaceutical formulations of pimavanserin |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20070264330A1 (OSRAM) |
| EP (1) | EP2037918A2 (OSRAM) |
| JP (1) | JP2009537538A (OSRAM) |
| CA (1) | CA2652300A1 (OSRAM) |
| WO (1) | WO2007133802A2 (OSRAM) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7790899B2 (en) * | 2004-09-27 | 2010-09-07 | Acadia Pharmaceuticals, Inc. | Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms |
| EP2134330B1 (en) * | 2007-03-19 | 2013-05-08 | Acadia Pharmaceuticals Inc. | Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics |
| AU2008254669A1 (en) * | 2007-05-18 | 2008-11-27 | Acadia Pharmaceuticals Inc. | Use of pimavanserin in the treatment of parkinson and symptoms thereof |
| WO2012060847A1 (en) * | 2010-11-07 | 2012-05-10 | Targegen, Inc. | Compositions and methods for treating myelofibrosis |
| CN102600146B (zh) * | 2012-04-11 | 2014-10-08 | 兆科药业（合肥）有限公司 | 一种盐酸乐卡地平和氯沙坦钾复方制剂及其制备方法 |
| NZ707033A (en) * | 2012-11-19 | 2016-11-25 | Azanta As | Dispersible nimorazole tablet |
| US9446037B2 (en) * | 2012-11-27 | 2016-09-20 | Acadia Pharmaceuticals Inc. | Methods for the treatment of parkinson's disease psychosis using pimavanserin |
| EP3325444B1 (en) | 2015-07-20 | 2021-07-07 | Acadia Pharmaceuticals Inc. | Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c |
| CN105929030B (zh) * | 2015-12-18 | 2018-08-21 | 重庆两江药物研发中心有限公司 | 一种哌马色林中有机杂质的检测方法 |
| US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
| WO2017165635A1 (en) | 2016-03-25 | 2017-09-28 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome p450 modulators |
| EP3436010B1 (en) * | 2016-03-29 | 2021-03-10 | Acadia Pharmaceuticals Inc. | 5-ht2a serotonin receptor inverse agonists or antagonists for use in reducing amyloid-beta peptides and accumulation of amyloid plaques |
| US11464768B2 (en) | 2016-12-20 | 2022-10-11 | Acadia Pharmaceuticals Inc. | Pimavanserin alone or in combination for use in the treatment of Alzheimer's disease psychosis |
| US11135211B2 (en) | 2017-04-28 | 2021-10-05 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating impulse control disorder |
| US20210077479A1 (en) * | 2017-08-30 | 2021-03-18 | Acadia Pharmaceuticals Inc. | Formulations of pimavanserin |
| US10377708B2 (en) | 2017-12-05 | 2019-08-13 | Sunovion Pharmaceuticals Inc. | Crystal forms and production methods thereof |
| CN118593482A (zh) | 2017-12-05 | 2024-09-06 | 赛诺维信制药公司 | 非外消旋混合物及其用途 |
| CN109908097A (zh) * | 2017-12-13 | 2019-06-21 | 北京万全德众医药生物技术有限公司 | 匹莫范色林口崩缓释片 |
| IT201800003736A1 (it) | 2018-03-19 | 2019-09-19 | Lundbeck Pharmaceuticals Italy S P A | Processo per la produzione di Pimavanserin |
| IT201800009690A1 (it) | 2018-10-23 | 2020-04-23 | Lundbeck Pharmaceuticals Italy Spa | Processo per la produzione di pimavanserina |
| WO2020092618A1 (en) | 2018-10-30 | 2020-05-07 | Acadia Pharmaceuticals Inc. | Methods of treating depression, anxiety and sexual dysfunction using the compound primavanserin |
| CN109613164B (zh) * | 2019-01-08 | 2021-02-09 | 丽珠集团新北江制药股份有限公司 | 一种酒石酸匹莫范色林的检测方法 |
| CN109613163B (zh) * | 2019-01-08 | 2021-01-26 | 丽珠集团新北江制药股份有限公司 | 一种酒石酸匹莫范色林及其杂质的检测方法 |
| JP2022535893A (ja) | 2019-06-04 | 2022-08-10 | サノビオン ファーマシューティカルズ インク | 放出調節製剤およびその使用 |
| US20220288048A1 (en) | 2019-07-22 | 2022-09-15 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating schizophrenia or for treating psychosis secondary to neurodegenerative disorders or depressive disorder |
| US20220323429A1 (en) | 2019-08-15 | 2022-10-13 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating neurodegenerative diseases |
| CA3159716A1 (en) * | 2019-12-05 | 2021-06-10 | Fresenius Kabi Usa, Llc | Method for analyzing degarelix and associated products |
| US11648242B2 (en) * | 2019-12-12 | 2023-05-16 | Aurobindo Pharma Ltd | Pharmaceutical composition comprising pimavanserin, process of preparation and use thereof |
| WO2022094230A1 (en) | 2020-11-02 | 2022-05-05 | Acadia Pharmaceuticals Inc. | Compounds for treating psychosis or depression |
| WO2023128900A1 (en) * | 2021-12-30 | 2023-07-06 | Pharmactive Ilac Sanayi Ve Ticaret A.S. | Pharmaceutical compositions comprising pimavanserin as active ingredient and relevant excipients |
| CN117074579B (zh) * | 2023-10-16 | 2023-12-22 | 江苏东科康德药业有限公司 | 一种氨磺必利口服溶液有关物质的分析方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8628475D0 (en) * | 1986-11-28 | 1987-01-07 | Glaxo Group Ltd | Medicaments |
| US6419956B1 (en) * | 1999-12-30 | 2002-07-16 | Ancile Pharmaceuticals | Odor-masking coating for a pharmaceutical preparation |
| ATE407117T1 (de) * | 2003-01-16 | 2008-09-15 | Acadia Pharm Inc | Selektive serotonin 2a/2c inverse rezeptoragonisten als therapeutika für neurodegenerative erkrankungen |
| US20050065183A1 (en) * | 2003-07-31 | 2005-03-24 | Indranil Nandi | Fexofenadine composition and process for preparing |
| ATE426405T1 (de) * | 2003-12-22 | 2009-04-15 | Acadia Pharm Inc | Amino-substituierte diarylaa,ducyclohepten- analoga als muscarinische agonisten und verfahren zur behandlung von neuropsychiatrischen erkrankungen |
| US20070172524A1 (en) * | 2004-03-29 | 2007-07-26 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Process for preparing a solid pharmaceutical composition |
| BRPI0510074A (pt) * | 2004-04-22 | 2007-10-16 | Boehringer Ingelheim Int | composições farmacêuticas para o tratamento de distúrbios sexuais ii |
| US20050261278A1 (en) * | 2004-05-21 | 2005-11-24 | Weiner David M | Selective serotonin receptor inverse agonists as therapeutics for disease |
| US7820695B2 (en) * | 2004-05-21 | 2010-10-26 | Acadia Pharmaceuticals, Inc. | Selective serotonin receptor inverse agonists as therapeutics for disease |
| US7868176B2 (en) * | 2004-09-27 | 2011-01-11 | Acadia Pharmaceuticals, Inc. | Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-y1)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation |
| EP2283811A1 (en) * | 2004-10-19 | 2011-02-16 | Krka Tovarna Zdravil, D.D., Novo Mesto | Solid pharmaceutical composition comprising donepezil hydrochloride |
-
2007
- 2007-05-15 EP EP07794929A patent/EP2037918A2/en not_active Withdrawn
- 2007-05-15 WO PCT/US2007/011720 patent/WO2007133802A2/en not_active Ceased
- 2007-05-15 CA CA002652300A patent/CA2652300A1/en not_active Abandoned
- 2007-05-15 US US11/749,110 patent/US20070264330A1/en not_active Abandoned
- 2007-05-15 JP JP2009511049A patent/JP2009537538A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007133802A2 (en) | 2007-11-22 |
| JP2009537538A (ja) | 2009-10-29 |
| US20070264330A1 (en) | 2007-11-15 |
| EP2037918A2 (en) | 2009-03-25 |
| WO2007133802A3 (en) | 2008-01-24 |
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| FZDE | Discontinued | ||
| FZDE | Discontinued |
Effective date: 20120515 |