MY131878A - Eplerenone crystalline form exhibiting enhanced dissolution rate - Google Patents
Eplerenone crystalline form exhibiting enhanced dissolution rateInfo
- Publication number
- MY131878A MY131878A MYPI20005734A MYPI20005734A MY131878A MY 131878 A MY131878 A MY 131878A MY PI20005734 A MYPI20005734 A MY PI20005734A MY PI20005734 A MYPI20005734 A MY PI20005734A MY 131878 A MY131878 A MY 131878A
- Authority
- MY
- Malaysia
- Prior art keywords
- eplerenone
- dissolution rate
- crystalline form
- preparing
- exhibiting enhanced
- Prior art date
Links
- 229960001208 eplerenone Drugs 0.000 title abstract 11
- JUKPWJGBANNWMW-VWBFHTRKSA-N eplerenone Chemical compound C([C@@H]1[C@]2(C)C[C@H]3O[C@]33[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)C(=O)OC)C[C@@]21CCC(=O)O1 JUKPWJGBANNWMW-VWBFHTRKSA-N 0.000 title abstract 11
- 238000004090 dissolution Methods 0.000 title abstract 2
- 230000001747 exhibiting effect Effects 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 abstract 1
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 abstract 1
- 239000012736 aqueous medium Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
- C07J71/0015—Oxiranes at position 9(11)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
Abstract
A NOVEL CRYSTALLINE FORM (FORM H) OF THE ALDOSTERONE RECEPTOR ANTAGONIST DRUG EPLERENONE IS PROVIDED HAVING A RELATIVELY RAPID DISSOLUTION RATE IN AQUEOUS MEDIA. ALSO PROVIDED ARE NOVEL SOLVATED CRYSTALLINE FORMS OF EPLERENONE THAT, WHEN DESOLVATED, CAN YIELD FORM H EPLERENONE. ALSO PROVIDED IS AMORPHOUS EPLERENONE. PHARMACEUTICAL COMPOSITIONS ARE PROVIDED COMPRISING FORM H EPLERENONE, OPTIONALLY ACCOMPINED BY ONE OR MORE OTHER SOLID STATE OF EPLERENONE, IN A TOTAL UNIT DOSAGE AMOUNT OF EPLERERIONE OF ABOUT 10 TO 100 MG, AND FURTHER COMPRISING ONE OR MORE PHARMACEUTICALLY ACCEPTABLE EXCIPIENTS.PROCESS ARE PROVIDED FOR PREPARING FORM H EPLERENONE AND FOR PREPARING COMPRISING FORM H EPLERENONE. A METHOD FOR PROPHYLAXIS AND/OR TREATMENT OF AN ALDOSTERONE-MEDIATED CONDITION OR DISORDER IS ALSO PROVIDE COMPRISING ADMINISTERING TO A SUBJECT A THERAPEUTICALLY EFFECTIVE AMOUNT OF EPLERENONE WHEREIN AT LEAST A FRACTION OF THE EPLERENONE PRESENT IS FORM H ELPERENONE.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16968299P | 1999-12-08 | 1999-12-08 | |
| US16960899P | 1999-12-08 | 1999-12-08 | |
| US16980799P | 1999-12-08 | 1999-12-08 | |
| US16963999P | 1999-12-08 | 1999-12-08 | |
| US16969099P | 1999-12-08 | 1999-12-08 | |
| US16955699P | 1999-12-08 | 1999-12-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MY131878A true MY131878A (en) | 2007-09-28 |
Family
ID=27558585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MYPI20005734A MY131878A (en) | 1999-12-08 | 2000-12-06 | Eplerenone crystalline form exhibiting enhanced dissolution rate |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP1177204A2 (en) |
| JP (1) | JP2003516414A (en) |
| KR (1) | KR100607923B1 (en) |
| CN (2) | CN1152886C (en) |
| AU (1) | AU784946B2 (en) |
| BR (1) | BR0008057A (en) |
| CA (1) | CA2362669A1 (en) |
| CO (1) | CO5280211A1 (en) |
| EA (1) | EA007934B1 (en) |
| HU (1) | HUP0203032A3 (en) |
| IL (3) | IL144764A0 (en) |
| MX (1) | MXPA01008056A (en) |
| MY (1) | MY131878A (en) |
| NO (1) | NO20013856L (en) |
| NZ (2) | NZ530028A (en) |
| PE (1) | PE20010917A1 (en) |
| WO (1) | WO2001042272A2 (en) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA04009037A (en) * | 2002-03-20 | 2005-01-25 | Pharmacia Corp | Storage stable eplerenone formulation. |
| US7235655B2 (en) | 2002-03-22 | 2007-06-26 | Pharmacia & Upjohn Company | Processes to prepare eplerenone |
| CA2582496A1 (en) | 2007-03-20 | 2008-09-20 | Apotex Pharmachem Inc. | Improved process for the preparation and purification of eplerenone |
| CA2796307A1 (en) | 2010-05-10 | 2011-11-17 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and compositions for the treatment of fluid accumulation in and/ or under the retina |
| JP6180930B2 (en) | 2010-06-16 | 2017-08-16 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | Methods and compositions for stimulating reepithelialization during wound healing processes |
| US20180280414A1 (en) | 2015-10-13 | 2018-10-04 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of choroidal neovascularisation |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| EP3490606B8 (en) | 2016-07-26 | 2024-04-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| CN108059648A (en) * | 2017-12-30 | 2018-05-22 | 合肥久诺医药科技有限公司 | A kind of eplerenone solvate and preparation method thereof |
| WO2023031277A1 (en) | 2021-08-31 | 2023-03-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of ocular rosacea |
| WO2023204729A1 (en) * | 2022-04-19 | 2023-10-26 | Общество с ограниченной ответственностью "Гелеспон" | Pharmaceutical compositions based on a novel substance of 4-[2-(1н-imidazol-4-yl)-ethylcarbamoyl]-butanoic acid and method for producing said substance |
| CN120189420B (en) * | 2025-05-23 | 2025-09-09 | 远大医药（中国）有限公司 | Eplerenone-containing composition, pharmaceutical preparation, preparation method and use thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4559332A (en) * | 1983-04-13 | 1985-12-17 | Ciba Geigy Corporation | 20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof |
| DK0944644T3 (en) * | 1996-12-11 | 2003-02-03 | Searle & Co | Process for Preparation of 3-Keto-7-Alpha-Alkoxycarbonyl-Delta-4,5-Steroids and Intermediates |
| HK1042252B (en) * | 1999-03-05 | 2004-04-23 | G.D. Searle Llc | Combination therapy of angiotensin converting enzyme inhibitor and epoxy-steroidal aldosterone antagonist for treatment of cardiovascular disease |
-
2000
- 2000-12-04 BR BR0008057-8A patent/BR0008057A/en not_active IP Right Cessation
- 2000-12-04 KR KR1020017010043A patent/KR100607923B1/en not_active Expired - Fee Related
- 2000-12-04 EP EP00983781A patent/EP1177204A2/en not_active Withdrawn
- 2000-12-04 WO PCT/US2000/032416 patent/WO2001042272A2/en not_active Ceased
- 2000-12-04 MX MXPA01008056A patent/MXPA01008056A/en not_active Application Discontinuation
- 2000-12-04 NZ NZ530028A patent/NZ530028A/en not_active IP Right Cessation
- 2000-12-04 CA CA002362669A patent/CA2362669A1/en not_active Abandoned
- 2000-12-04 HU HU0203032A patent/HUP0203032A3/en unknown
- 2000-12-04 AU AU20492/01A patent/AU784946B2/en not_active Ceased
- 2000-12-04 IL IL14476400A patent/IL144764A0/en active IP Right Grant
- 2000-12-04 JP JP2001543569A patent/JP2003516414A/en not_active Withdrawn
- 2000-12-04 NZ NZ513961A patent/NZ513961A/en not_active IP Right Cessation
- 2000-12-04 CN CNB008057788A patent/CN1152886C/en not_active Expired - Fee Related
- 2000-12-04 EA EA200100871A patent/EA007934B1/en not_active IP Right Cessation
- 2000-12-04 CN CNA2004100368081A patent/CN1557833A/en active Pending
- 2000-12-06 PE PE2000001300A patent/PE20010917A1/en not_active Application Discontinuation
- 2000-12-06 MY MYPI20005734A patent/MY131878A/en unknown
- 2000-12-11 CO CO00094075A patent/CO5280211A1/en not_active Application Discontinuation
-
2001
- 2001-08-06 IL IL144764A patent/IL144764A/en not_active IP Right Cessation
- 2001-08-08 NO NO20013856A patent/NO20013856L/en not_active Application Discontinuation
-
2006
- 2006-06-22 IL IL176511A patent/IL176511A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2001042272A3 (en) | 2001-11-29 |
| KR100607923B1 (en) | 2006-08-04 |
| MXPA01008056A (en) | 2003-07-21 |
| CA2362669A1 (en) | 2001-06-14 |
| NZ530028A (en) | 2005-08-26 |
| AU2049201A (en) | 2001-06-18 |
| PE20010917A1 (en) | 2001-09-10 |
| WO2001042272A9 (en) | 2002-12-12 |
| KR20010112261A (en) | 2001-12-20 |
| HUP0203032A3 (en) | 2003-04-28 |
| IL144764A (en) | 2007-08-19 |
| JP2003516414A (en) | 2003-05-13 |
| IL144764A0 (en) | 2002-06-30 |
| WO2001042272A2 (en) | 2001-06-14 |
| EA200100871A1 (en) | 2002-04-25 |
| NO20013856D0 (en) | 2001-08-08 |
| CN1557833A (en) | 2004-12-29 |
| IL176511A (en) | 2007-08-19 |
| HUP0203032A2 (en) | 2002-12-28 |
| AU784946B2 (en) | 2006-08-03 |
| CN1152886C (en) | 2004-06-09 |
| HK1050536A1 (en) | 2003-06-27 |
| CO5280211A1 (en) | 2003-05-30 |
| CN1377365A (en) | 2002-10-30 |
| NO20013856L (en) | 2001-10-08 |
| NZ513961A (en) | 2004-02-27 |
| EP1177204A2 (en) | 2002-02-06 |
| BR0008057A (en) | 2002-04-23 |
| EA007934B1 (en) | 2007-02-27 |
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