ZA200109775B - Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions. - Google Patents
Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions. Download PDFInfo
- Publication number
- ZA200109775B ZA200109775B ZA200109775A ZA200109775A ZA200109775B ZA 200109775 B ZA200109775 B ZA 200109775B ZA 200109775 A ZA200109775 A ZA 200109775A ZA 200109775 A ZA200109775 A ZA 200109775A ZA 200109775 B ZA200109775 B ZA 200109775B
- Authority
- ZA
- South Africa
- Prior art keywords
- polymorphic form
- crystalline
- citrate monohydrate
- hours
- citrate
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 6
- WCQNEVLYWBFPSQ-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;octan-3-amine Chemical compound CCCCCC(N)CC.OC(=O)CC(O)(C(O)=O)CC(O)=O WCQNEVLYWBFPSQ-UHFFFAOYSA-N 0.000 title claims description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 16
- YASYEJJMZJALEJ-UHFFFAOYSA-N Citric acid monohydrate Chemical compound O.OC(=O)CC(O)(C(O)=O)CC(O)=O YASYEJJMZJALEJ-UHFFFAOYSA-N 0.000 claims description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- 206010047700 Vomiting Diseases 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 5
- ZAFNJMIOTHYJRJ-UHFFFAOYSA-N Diisopropyl ether Chemical compound CC(C)OC(C)C ZAFNJMIOTHYJRJ-UHFFFAOYSA-N 0.000 claims description 4
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 claims description 4
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 238000001914 filtration Methods 0.000 claims description 4
- 239000012458 free base Substances 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 239000002464 receptor antagonist Substances 0.000 claims description 4
- 229940044551 receptor antagonist Drugs 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000007787 solid Substances 0.000 claims description 4
- PEGOJNFMPFGHLY-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;octan-3-amine;hydrate Chemical compound O.CCCCCC(N)CC.OC(=O)CC(O)(C(O)=O)CC(O)=O PEGOJNFMPFGHLY-UHFFFAOYSA-N 0.000 claims description 3
- 238000002425 crystallisation Methods 0.000 claims description 3
- 230000008025 crystallization Effects 0.000 claims description 3
- 229910052757 nitrogen Inorganic materials 0.000 claims description 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 3
- 238000010926 purge Methods 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 238000003756 stirring Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 238000005469 granulation Methods 0.000 claims 1
- 230000003179 granulation Effects 0.000 claims 1
- 150000004682 monohydrates Chemical class 0.000 description 5
- 239000002002 slurry Substances 0.000 description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 229960004106 citric acid Drugs 0.000 description 2
- 238000000921 elemental analysis Methods 0.000 description 2
- 239000000155 melt Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 101100114828 Drosophila melanogaster Orai gene Proteins 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical group CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 229960004543 anhydrous citric acid Drugs 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 238000000113 differential scanning calorimetry Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000002895 emetic Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- JASMWYNKLTULAN-UHFFFAOYSA-N octan-3-amine Chemical compound CCCCCC(N)CC JASMWYNKLTULAN-UHFFFAOYSA-N 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 238000001907 polarising light microscopy Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13699299P | 1999-06-01 | 1999-06-01 |
Publications (1)
Publication Number | Publication Date |
---|---|
ZA200109775B true ZA200109775B (en) | 2002-11-28 |
Family
ID=22475338
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ZA200109775A ZA200109775B (en) | 1999-06-01 | 2001-11-28 | Polymorphs of a crystalline azabicyclo (2,2,2) octan-3-amine citrate and their pharmaceutical compositions. |
Country Status (49)
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5021318B2 (ja) * | 2004-01-30 | 2012-09-05 | ファイザー・プロダクツ・インク | β−シクロデキストリンを液体投薬形態に用いて多用量製剤を達成するための抗菌性防腐剤 |
JP2007519702A (ja) * | 2004-01-30 | 2007-07-19 | ファイザー・プロダクツ・インク | ニューロキニン受容体拮抗薬及びシクロデキストリンからなる医薬組成物、ならびに注射部位の耐容性を改善するための方法 |
AU2005216706B2 (en) | 2004-01-30 | 2007-11-29 | Pfizer Products Inc. | NK-1 receptor antagonists anesthesia recovery |
CN1914202A (zh) * | 2004-02-02 | 2007-02-14 | 辉瑞产品有限公司 | 1-(2s,3s)-2-二苯甲基-n-(5-叔丁基-2-甲氧基苄基)奎宁环-3-胺的制备方法 |
JP6454323B2 (ja) * | 2013-03-15 | 2019-01-16 | パール セラピューティクス,インコーポレイテッド | 粒子状結晶性材料のコンディショニングのための方法及びシステム |
CN110577522B (zh) * | 2018-06-07 | 2022-12-27 | 东莞市东阳光动物保健药品有限公司 | 马罗匹坦柠檬酸盐新晶型及其制备方法 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE9290063U1 (de) * | 1991-05-31 | 1994-02-24 | Pfizer Inc., New York, N.Y. | Chinuclidin-Derivate |
US5393762A (en) * | 1993-06-04 | 1995-02-28 | Pfizer Inc. | Pharmaceutical agents for treatment of emesis |
US5576317A (en) * | 1994-12-09 | 1996-11-19 | Pfizer Inc. | NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis |
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2000
- 2000-05-08 US US09/566,307 patent/US6255320B1/en not_active Expired - Lifetime
- 2000-05-17 HN HN2000000077A patent/HN2000000077A/es unknown
- 2000-05-18 PL PL00352716A patent/PL196046B1/pl not_active IP Right Cessation
- 2000-05-18 CZ CZ20014269A patent/CZ295819B6/cs not_active IP Right Cessation
- 2000-05-18 IL IL14640600A patent/IL146406A0/xx not_active IP Right Cessation
- 2000-05-18 KR KR10-2001-7015494A patent/KR100476606B1/ko not_active IP Right Cessation
- 2000-05-18 DK DK00925528T patent/DK1181290T3/da active
- 2000-05-18 EA EA200101108A patent/EA003731B1/ru active Protection Beyond IP Right Term
- 2000-05-18 HU HU0201301A patent/HUP0201301A3/hu unknown
- 2000-05-18 AT AT00925528T patent/ATE244239T1/de not_active IP Right Cessation
- 2000-05-18 SI SI200030161T patent/SI1181290T1/xx unknown
- 2000-05-18 WO PCT/IB2000/000665 patent/WO2000073304A1/en active IP Right Grant
- 2000-05-18 JP JP2001500629A patent/JP3830816B2/ja not_active Expired - Lifetime
- 2000-05-18 ES ES00925528T patent/ES2199825T3/es not_active Expired - Lifetime
- 2000-05-18 TR TR2001/03473T patent/TR200103473T2/xx unknown
- 2000-05-18 PT PT00925528T patent/PT1181290E/pt unknown
- 2000-05-18 EE EEP200100656A patent/EE200100656A/xx unknown
- 2000-05-18 YU YU81101A patent/YU81101A/sh unknown
- 2000-05-18 SK SK1733-2001A patent/SK285820B6/sk not_active IP Right Cessation
- 2000-05-18 OA OA1200100318A patent/OA11956A/en unknown
- 2000-05-18 BR BR0011094-9A patent/BR0011094A/pt not_active Application Discontinuation
- 2000-05-18 MX MXPA01012325A patent/MXPA01012325A/es unknown
- 2000-05-18 UA UA2001118214A patent/UA66925C2/uk unknown
- 2000-05-18 AU AU44248/00A patent/AU767334B2/en not_active Expired
- 2000-05-18 AP APAP/P/2001/002349A patent/AP2001002349A0/en unknown
- 2000-05-18 DE DE60003679T patent/DE60003679T2/de not_active Expired - Lifetime
- 2000-05-18 NZ NZ515349A patent/NZ515349A/xx unknown
- 2000-05-18 CA CA002372238A patent/CA2372238C/en not_active Expired - Lifetime
- 2000-05-18 EP EP00925528A patent/EP1181290B1/en not_active Expired - Lifetime
- 2000-05-18 CN CNB008082782A patent/CN1146565C/zh not_active Expired - Lifetime
- 2000-05-23 PA PA20008496101A patent/PA8496101A1/es unknown
- 2000-05-26 CO CO00039195A patent/CO5170463A1/es not_active Application Discontinuation
- 2000-05-26 TW TW089110206A patent/TWI285204B/zh not_active IP Right Cessation
- 2000-05-29 UY UY26176A patent/UY26176A1/es not_active Application Discontinuation
- 2000-05-30 PE PE2000000520A patent/PE20010209A1/es not_active Application Discontinuation
- 2000-05-30 MY MYPI20002409A patent/MY133508A/en unknown
- 2000-05-30 AR ARP000102663A patent/AR033331A1/es active IP Right Grant
- 2000-05-31 TN TNTNSN00120A patent/TNSN00120A1/fr unknown
- 2000-05-31 SV SV2000000093A patent/SV2001000093A/es unknown
- 2000-05-31 DZ DZ000101A patent/DZ3050A1/xx active
- 2000-05-31 MA MA25997A patent/MA26742A1/fr unknown
- 2000-05-31 GT GT200000087A patent/GT200000087A/es unknown
- 2000-06-01 EC EC2000003508A patent/ECSP003508A/es unknown
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2001
- 2001-11-28 ZA ZA200109775A patent/ZA200109775B/en unknown
- 2001-11-30 NO NO20015848A patent/NO20015848L/no not_active Application Discontinuation
- 2001-12-04 HR HR20010904A patent/HRP20010904A2/hr not_active Application Discontinuation
- 2001-12-10 BG BG106204A patent/BG65240B1/bg unknown
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2002
- 2002-10-30 HK HK02107879A patent/HK1046284A1/xx not_active IP Right Cessation
-
2007
- 2007-03-27 CY CY2007011C patent/CY2007011I2/el unknown
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