JP2005120105A5 - - Google Patents
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- Publication number
- JP2005120105A5 JP2005120105A5 JP2004349020A JP2004349020A JP2005120105A5 JP 2005120105 A5 JP2005120105 A5 JP 2005120105A5 JP 2004349020 A JP2004349020 A JP 2004349020A JP 2004349020 A JP2004349020 A JP 2004349020A JP 2005120105 A5 JP2005120105 A5 JP 2005120105A5
- Authority
- JP
- Japan
- Prior art keywords
- pravastatin sodium
- pravastatin
- crystalline
- aprotic solvent
- solution
- 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
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims 138
- 238000000034 method Methods 0.000 claims 126
- 229960001495 pravastatin sodium Drugs 0.000 claims 97
- 239000000243 solution Substances 0.000 claims 43
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical group CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 27
- 239000000010 aprotic solvent Substances 0.000 claims 23
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 22
- 239000008194 pharmaceutical composition Substances 0.000 claims 22
- 238000000634 powder X-ray diffraction Methods 0.000 claims 20
- 239000003586 protic polar solvent Substances 0.000 claims 18
- 238000001816 cooling Methods 0.000 claims 17
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 15
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 15
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims 14
- 239000003880 polar aprotic solvent Substances 0.000 claims 14
- 229960002965 pravastatin Drugs 0.000 claims 14
- 201000001320 Atherosclerosis Diseases 0.000 claims 11
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 11
- 239000003937 drug carrier Substances 0.000 claims 11
- 239000012454 non-polar solvent Substances 0.000 claims 11
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 10
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 claims 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 8
- 238000010521 absorption reaction Methods 0.000 claims 8
- 238000010438 heat treatment Methods 0.000 claims 8
- 238000002329 infrared spectrum Methods 0.000 claims 8
- 238000007865 diluting Methods 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 239000007787 solid Substances 0.000 claims 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 7
- 239000002904 solvent Substances 0.000 claims 6
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 5
- 238000002425 crystallisation Methods 0.000 claims 5
- 230000008025 crystallization Effects 0.000 claims 5
- 238000010790 dilution Methods 0.000 claims 5
- 239000012895 dilution Substances 0.000 claims 5
- 239000003208 petroleum Substances 0.000 claims 5
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 238000011534 incubation Methods 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17068599P | 1999-12-14 | 1999-12-14 | |
| US19064900P | 2000-03-20 | 2000-03-20 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001544662A Division JP2003516959A (ja) | 1999-12-14 | 2000-12-14 | プラバスタチンナトリウムの新規フォーム |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005120105A JP2005120105A (ja) | 2005-05-12 |
| JP2005120105A5 true JP2005120105A5 (enExample) | 2005-10-06 |
Family
ID=26866349
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001544662A Pending JP2003516959A (ja) | 1999-12-14 | 2000-12-14 | プラバスタチンナトリウムの新規フォーム |
| JP2004349020A Pending JP2005120105A (ja) | 1999-12-14 | 2004-12-01 | プラバスタチンナトリウムの新規フォーム |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001544662A Pending JP2003516959A (ja) | 1999-12-14 | 2000-12-14 | プラバスタチンナトリウムの新規フォーム |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US7001919B2 (enExample) |
| EP (1) | EP1242051A4 (enExample) |
| JP (2) | JP2003516959A (enExample) |
| KR (1) | KR20020062340A (enExample) |
| CN (1) | CN1434702A (enExample) |
| AU (1) | AU779306B2 (enExample) |
| CA (1) | CA2394200C (enExample) |
| CZ (1) | CZ20021998A3 (enExample) |
| HK (1) | HK1049441A1 (enExample) |
| HU (1) | HUP0204005A3 (enExample) |
| IL (1) | IL150187A0 (enExample) |
| PL (1) | PL364929A1 (enExample) |
| SK (1) | SK8312002A3 (enExample) |
| WO (1) | WO2001043723A1 (enExample) |
| YU (1) | YU45202A (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK8312002A3 (en) * | 1999-12-14 | 2003-05-02 | Biogal Gyogyszergyar | Novel forms of pravastatin sodium |
| CA2441798C (en) * | 2001-03-27 | 2009-10-20 | Sumitomo Pharmaceuticals Company, Limited | Crystalline isoxazole derivative and medical preparation thereof |
| WO2005084669A1 (en) * | 2004-03-01 | 2005-09-15 | Lek Pharmaceuticals D.D. | Pharmaceutical composition |
| KR20070038553A (ko) | 2004-08-06 | 2007-04-10 | 트렌스폼 파마수티컬스 인코퍼레이티드 | 신규한 스타틴 약제학적 조성물 및 관련된 치료방법 |
| MX2007009229A (es) * | 2005-02-09 | 2007-09-25 | Teva Gyogyszergyar Zartkoruen | Metodos para realizar pravastatina de sodio. |
| JP4813841B2 (ja) * | 2005-07-25 | 2011-11-09 | キユーピー株式会社 | プラバスタチンナトリウムの製造方法 |
| CN101648867B (zh) * | 2009-09-04 | 2012-07-11 | 天津大学 | 一种普伐他汀钠晶型及其制备方法和应用 |
| EP2343054A1 (en) | 2010-01-04 | 2011-07-13 | LEK Pharmaceuticals d.d. | Pellets and microparticles of pravastatin sodium and a process of making them |
| WO2012085191A1 (en) | 2010-12-23 | 2012-06-28 | Dsm Sinochem Pharmaceuticals Netherlands B.V. | Crystalline form of pravastatine and process for the preparation thereof |
| SG10202012791TA (en) | 2013-11-15 | 2021-01-28 | Akebia Therapeutics Inc | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof |
| CN105949062B (zh) * | 2016-06-24 | 2017-06-13 | 广东蓝宝制药有限公司 | 一种规模化制备普伐他汀钠d型晶体的工艺 |
| CN111018714B (zh) * | 2019-12-27 | 2020-09-04 | 广东蓝宝制药有限公司 | 一种获得高纯a晶型普伐他汀钠的制备方法 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4319039A (en) | 1979-06-15 | 1982-03-09 | Merck & Co., Inc. | Preparation of ammonium salt of hypocholesteremic fermentation product |
| MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
| EP0215665B1 (en) | 1985-09-13 | 1991-11-21 | Sankyo Company Limited | Hydroxy-ml-236b derivatives, their preparation and use |
| US4857547A (en) * | 1988-01-07 | 1989-08-15 | Merck & Co., Inc. | Novel HMG-CoA reductase inhibitors |
| US4857522A (en) | 1988-03-21 | 1989-08-15 | E. R. Squibb & Sons, Inc. | Derivatives of pravastatin for inhibiting cholesterol biosynthesis |
| US5180589A (en) | 1988-03-31 | 1993-01-19 | E. R. Squibb & Sons, Inc. | Pravastatin pharmaceuatical compositions having good stability |
| US5099035A (en) * | 1989-02-27 | 1992-03-24 | E. R. Squibb & Sons, Inc. | Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same |
| US5140012A (en) * | 1990-05-31 | 1992-08-18 | E. R. Squibb & Sons, Inc. | Method for preventing onset of restenosis after angioplasty employing pravastatin |
| US5202029A (en) * | 1991-03-13 | 1993-04-13 | Caron Kabushiki Kaisha | Process for purification of hmg-coa reductase inhibitors |
| US5157025A (en) | 1991-04-01 | 1992-10-20 | E. R. Squibb & Sons, Inc. | Method for lowering serum cholesterol employing a phosphorus containing ace inhibitor alone or in combination with a cholesterol lowering drug |
| US5225202A (en) * | 1991-09-30 | 1993-07-06 | E. R. Squibb & Sons, Inc. | Enteric coated pharmaceutical compositions |
| NZ250609A (en) | 1992-12-28 | 1995-07-26 | Sankyo Co | Hexahydronaphthalene esters and ring closed lactones; preparation and medicaments |
| SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
| IL112639A0 (en) | 1994-03-11 | 1995-05-26 | Bristol Myers Squibb Co | A pharmaceutical composition containing pravastin |
| US5942423A (en) | 1995-06-07 | 1999-08-24 | Massachusetts Institute Of Technology | Conversion of compactin to pravastatin by actinomadura |
| US5616595A (en) | 1995-06-07 | 1997-04-01 | Abbott Laboratories | Process for recovering water insoluble compounds from a fermentation broth |
| US5883109A (en) | 1996-07-24 | 1999-03-16 | Bristol-Myers Squibb Company | Method for lowering serum lipid levels employing an MTP inhibitor in combination with another cholesterol lowering drug |
| US6165757A (en) | 1997-02-20 | 2000-12-26 | Dsm N.V. | Nitrogen feed in statin fermentation |
| KR100210482B1 (ko) * | 1997-04-10 | 1999-07-15 | 김종인 | 스트렙토마이세스엑스포리아투스(streptomycesexfoliatus)yj-118과이를이용한프라바스타틴나트륨의제조방법 |
| AU9264598A (en) | 1997-08-22 | 1999-03-16 | Gist-Brocades B.V. | Statin production by fermentation |
| SI9800046A (sl) | 1998-02-18 | 1999-08-31 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Postopek za pridobivanje inhibitorjev HMG-CoA reduktaze visoke čistosti |
| SI20305A (sl) * | 1999-08-06 | 2001-02-28 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Kristali natrijeve soli pravastatina |
| SI20072A (sl) | 1998-09-18 | 2000-04-30 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Postopek za pridobivanje inhibitorjev HMG-CoA reduktaze |
| WO2000033821A1 (en) * | 1998-12-07 | 2000-06-15 | Bristol-Myers Squibb Company | Enteric coated pravastatin bead formulation |
| CN1260344C (zh) | 1999-02-03 | 2006-06-21 | 药物研究所有限公司 | 培养物 |
| US6682913B1 (en) * | 1999-02-03 | 2004-01-27 | Institute For Drug Research Ltd. | Microbial process for preparing pravastatin |
| HUP9902352A1 (hu) | 1999-07-12 | 2000-09-28 | Gyógyszerkutató Intézet Kft. | Eljárás pravasztatin mikrobiológiai előállítására |
| DE60037687D1 (de) | 1999-11-30 | 2008-02-14 | Biogal Gyogyszergyar | Verfahren zur Rückgewinnung von Statinverbindungen aus einer Fermentationsbrühe |
| SK8312002A3 (en) * | 1999-12-14 | 2003-05-02 | Biogal Gyogyszergyar | Novel forms of pravastatin sodium |
| PL361230A1 (en) | 2000-10-05 | 2004-10-04 | Biogal Gyogyszergyar Rt. | Pravastatin sodium substantially free of pravastatin lactone and epi-pravastatin, and compositions containing same |
| DE10209305A1 (de) | 2001-04-30 | 2002-10-31 | Basf Ag | Thermische Spaltung von Allophanaten |
-
2000
- 2000-12-14 SK SK831-2002A patent/SK8312002A3/sk unknown
- 2000-12-14 PL PL00364929A patent/PL364929A1/xx unknown
- 2000-12-14 JP JP2001544662A patent/JP2003516959A/ja active Pending
- 2000-12-14 US US09/736,796 patent/US7001919B2/en not_active Expired - Fee Related
- 2000-12-14 WO PCT/US2000/033867 patent/WO2001043723A1/en not_active Ceased
- 2000-12-14 HK HK03101565.0A patent/HK1049441A1/zh unknown
- 2000-12-14 AU AU20987/01A patent/AU779306B2/en not_active Ceased
- 2000-12-14 CN CN00818961A patent/CN1434702A/zh active Pending
- 2000-12-14 HU HU0204005A patent/HUP0204005A3/hu unknown
- 2000-12-14 CZ CZ20021998A patent/CZ20021998A3/cs unknown
- 2000-12-14 EP EP00984355A patent/EP1242051A4/en not_active Withdrawn
- 2000-12-14 CA CA002394200A patent/CA2394200C/en not_active Expired - Fee Related
- 2000-12-14 IL IL15018700A patent/IL150187A0/xx unknown
- 2000-12-14 KR KR1020027007610A patent/KR20020062340A/ko not_active Abandoned
- 2000-12-14 YU YU45202A patent/YU45202A/sh unknown
-
2004
- 2004-12-01 JP JP2004349020A patent/JP2005120105A/ja active Pending
-
2005
- 2005-08-09 US US11/200,794 patent/US7262218B2/en not_active Expired - Fee Related
-
2007
- 2007-04-03 US US11/730,639 patent/US20070197633A1/en not_active Abandoned
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