MY131878A - Eplerenone crystalline form exhibiting enhanced dissolution rate - Google Patents

Eplerenone crystalline form exhibiting enhanced dissolution rate

Info

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
Application number
MYPI20005734A
Inventor
Kathleen P Barton
Mark A Pietz
Daniel R Pilipauskas
Yuen-Lung L Sing
Glenn L Stahl
Joseph J Wieczorek
Chris Y Yan
Thomas B Borchardt
Marlon V Carlos
Subbash Desai
Leonard J Ferro
Henry T Gaud
Scott Ganser
Clay R Little
Partha S Mudipalli
Original Assignee
Pharmacia Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Pharmacia Corp filed Critical Pharmacia Corp
Publication of MY131878A publication Critical patent/MY131878A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • C07J71/0015Oxiranes at position 9(11)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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.
MYPI20005734A 1999-12-08 2000-12-06 Eplerenone crystalline form exhibiting enhanced dissolution rate MY131878A (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US16963999P 1999-12-08 1999-12-08
US16960899P 1999-12-08 1999-12-08
US16955699P 1999-12-08 1999-12-08
US16968299P 1999-12-08 1999-12-08
US16969099P 1999-12-08 1999-12-08
US16980799P 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 (18)

Country Link
EP (1) EP1177204A2 (en)
JP (1) JP2003516414A (en)
KR (1) KR100607923B1 (en)
CN (2) CN1557833A (en)
AU (1) AU784946B2 (en)
BR (1) BR0008057A (en)
CA (1) CA2362669A1 (en)
CO (1) CO5280211A1 (en)
EA (1) EA007934B1 (en)
HK (1) HK1050536A1 (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 (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0308475A (en) * 2002-03-20 2005-01-11 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
WO2017064121A1 (en) 2015-10-13 2017-04-20 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
US20190262363A1 (en) 2016-07-26 2019-08-29 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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
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
CN100369927C (en) * 1996-12-11 2008-02-20 G·D·瑟尔公司 Processes for preparation of 9,11-epoxy steroids and intermediates useful therein
MXPA01009035A (en) * 1999-03-05 2004-08-12 Searle Llc Combination therapy of angiotensin converting enzyme inhibitor and epoxy-steroidal aldosterone antagonist for treatment of cardiovascular disease.

Also Published As

Publication number Publication date
NZ513961A (en) 2004-02-27
KR100607923B1 (en) 2006-08-04
EA200100871A1 (en) 2002-04-25
CN1557833A (en) 2004-12-29
AU2049201A (en) 2001-06-18
HUP0203032A2 (en) 2002-12-28
NO20013856L (en) 2001-10-08
CO5280211A1 (en) 2003-05-30
HUP0203032A3 (en) 2003-04-28
NZ530028A (en) 2005-08-26
IL144764A (en) 2007-08-19
IL144764A0 (en) 2002-06-30
WO2001042272A2 (en) 2001-06-14
IL176511A (en) 2007-08-19
NO20013856D0 (en) 2001-08-08
AU784946B2 (en) 2006-08-03
WO2001042272A9 (en) 2002-12-12
PE20010917A1 (en) 2001-09-10
WO2001042272A3 (en) 2001-11-29
CN1152886C (en) 2004-06-09
MXPA01008056A (en) 2003-07-21
JP2003516414A (en) 2003-05-13
EA007934B1 (en) 2007-02-27
CA2362669A1 (en) 2001-06-14
HK1050536A1 (en) 2003-06-27
CN1377365A (en) 2002-10-30
KR20010112261A (en) 2001-12-20
EP1177204A2 (en) 2002-02-06
BR0008057A (en) 2002-04-23

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