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 (https=) | 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 (https=) |
| EP (1) | EP1242051A4 (https=) |
| JP (2) | JP2003516959A (https=) |
| KR (1) | KR20020062340A (https=) |
| CN (1) | CN1434702A (https=) |
| AU (1) | AU779306B2 (https=) |
| CA (1) | CA2394200C (https=) |
| CZ (1) | CZ20021998A3 (https=) |
| HK (1) | HK1049441A1 (https=) |
| HU (1) | HUP0204005A3 (https=) |
| IL (1) | IL150187A0 (https=) |
| PL (1) | PL364929A1 (https=) |
| SK (1) | SK8312002A3 (https=) |
| WO (1) | WO2001043723A1 (https=) |
| YU (1) | YU45202A (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL150187A0 (en) * | 1999-12-14 | 2002-12-01 | Biogal Pharmaceutical Co Ltd | Novel forms of pravastatin sodium |
| WO2002092094A1 (en) * | 2001-03-27 | 2002-11-21 | Sumitomo Pharmaceuticals Co., Ltd. | Crystalline isoxazole derivative and medical preparation thereof |
| WO2005084669A1 (en) * | 2004-03-01 | 2005-09-15 | Lek Pharmaceuticals D.D. | Pharmaceutical composition |
| JP2008509154A (ja) | 2004-08-06 | 2008-03-27 | トランスフオーム・フアーマシユーチカルズ・インコーポレーテツド | 新規なスタチン薬剤組成物および関連治療方法 |
| CN101115706A (zh) * | 2005-02-09 | 2008-01-30 | 特瓦药厂私人有限公司 | 制备普伐他汀钠的方法 |
| 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 |
| MY180626A (en) | 2013-11-15 | 2020-12-03 | 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 |
| DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
| ATE69602T1 (de) | 1985-09-13 | 1991-12-15 | Sankyo Co | Hydroxy-ml-236b-derivate, deren herstellung und anwendung. |
| 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 |
| EP0975789A1 (en) | 1997-02-20 | 2000-02-02 | 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 |
| US6682913B1 (en) * | 1999-02-03 | 2004-01-27 | Institute For Drug Research Ltd. | Microbial process for preparing pravastatin |
| CN1260344C (zh) | 1999-02-03 | 2006-06-21 | 药物研究所有限公司 | 培养物 |
| HUP9902352A1 (hu) | 1999-07-12 | 2000-09-28 | Gyógyszerkutató Intézet Kft. | Eljárás pravasztatin mikrobiológiai előállítására |
| YU39102A (sh) * | 1999-11-30 | 2006-01-16 | Biogal Gyogyszergyar Rt | Postupak dobijanja statina iz fermentacione smeše |
| IL150187A0 (en) * | 1999-12-14 | 2002-12-01 | Biogal Pharmaceutical Co Ltd | Novel forms of pravastatin sodium |
| CN1468098A (zh) | 2000-10-05 | 2004-01-14 | �ݰ¸Ƕ�ҩ������˾ | 基本上无普伐他汀内酯和表普伐他汀的普伐他汀钠和包含普伐他汀钠的组合物 |
| DE10209305A1 (de) | 2001-04-30 | 2002-10-31 | Basf Ag | Thermische Spaltung von Allophanaten |
-
2000
- 2000-12-14 IL IL15018700A patent/IL150187A0/xx unknown
- 2000-12-14 PL PL00364929A patent/PL364929A1/xx unknown
- 2000-12-14 CZ CZ20021998A patent/CZ20021998A3/cs unknown
- 2000-12-14 SK SK831-2002A patent/SK8312002A3/sk unknown
- 2000-12-14 WO PCT/US2000/033867 patent/WO2001043723A1/en not_active Ceased
- 2000-12-14 US US09/736,796 patent/US7001919B2/en not_active Expired - Fee Related
- 2000-12-14 KR KR1020027007610A patent/KR20020062340A/ko not_active Abandoned
- 2000-12-14 JP JP2001544662A patent/JP2003516959A/ja active Pending
- 2000-12-14 CA CA002394200A patent/CA2394200C/en not_active Expired - Fee Related
- 2000-12-14 HU HU0204005A patent/HUP0204005A3/hu unknown
- 2000-12-14 YU YU45202A patent/YU45202A/sh unknown
- 2000-12-14 AU AU20987/01A patent/AU779306B2/en not_active Ceased
- 2000-12-14 EP EP00984355A patent/EP1242051A4/en not_active Withdrawn
- 2000-12-14 HK HK03101565.0A patent/HK1049441A1/zh unknown
- 2000-12-14 CN CN00818961A patent/CN1434702A/zh active Pending
-
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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