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PE20010917A1 - CRYSTALLINE FORM OF EPLERENONE SHOWING AN INCREASE IN DISSOLUTION RATE - Google Patents

CRYSTALLINE FORM OF EPLERENONE SHOWING AN INCREASE IN DISSOLUTION RATE

Info

Publication number
PE20010917A1
PE20010917A1 PE2000001300A PE0013002000A PE20010917A1 PE 20010917 A1 PE20010917 A1 PE 20010917A1 PE 2000001300 A PE2000001300 A PE 2000001300A PE 0013002000 A PE0013002000 A PE 0013002000A PE 20010917 A1 PE20010917 A1 PE 20010917A1
Authority
PE
Peru
Prior art keywords
eplerenone
refers
crystal
dicarboxylate
crystaline
Prior art date
Application number
PE2000001300A
Other languages
Spanish (es)
Inventor
Kathleen P Barton
Chris Y Yan
Marlon V Carlos
Subhash Desai
Leonard J Ferro
Scott Ganser
Henry T Gaud
Clay R Little
Martha S Mudipalli
Mark A Pietz
Daniel R Pilipauskas
Yuen-Lung L Sing
Glenn L Stahl
Joseph J Wieczorek
Thomas B Borchardt
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 PE20010917A1 publication Critical patent/PE20010917A1/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)
  • Gastroenterology & Hepatology (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (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

SE REFIERE A LA FORMA H DE EPLERENONA (METIL HIDROGENO 9,11-EPOXI-17-HIDROXI-3-OXOPREGN-4-ENE-7,21-DICARBOXILATO, g-LACTONA) QUE TIENE UNA DISOLUCION RAPIDA EN MEDIO ACUOSO Y SE CARACTERIZA POR PRESENTARSE EN FORMA DE CRISTAL ORTOROMBICO; PATRON DE DIFRACCION DE RAYOS X; PUNTO DE FUSION DE 247°C A 251°C; TAMANO DE PARTICULAS D90 INFERIOR A 400µm; TAMBIEN SE REFIERE A UNA DROGA QUE COMPRENDE DE 90% A 100% DE LA FORMA H Y EL RESTO CONSISTE DE EPLERENONA CRISTALINA FORMA L CON UN SISTEMA DE CRISTALES MONOCLINICOS; FORMA SOLVATADA DE EPLERENONA CRISTALINA, EPLERENONA AMORFA; UTILIZANDOSE DE 10mg A 1000mg. TAMBIEN SE REFIERE A i)UN METODO PARA PREPARAR LA FORMA H; ii)EPLERENONA AMORFA LIBRE DE LA FORMA CRISTALINA; iii)METODO PARA PROMOVER LA CRISTALIZACION DE LA FORMA H DE EPLERENONA QUE COMPRENDE BANAR LA SOLUCION ANTES DE LA CRISTALIZACION CON COMPUESTOS DE BANADO QUE EN FORMA SUSTANCIAL SON CRISTALOGRAFICAMENTE ISOESTRUCTURAL CON LA EPLERENONA FORMA H COMO 7-METILHIDROGENO 4O,5O,9O; 11O-DIEPOXIDO-17-HIDROXI-3-OXO-17O-PREGNAN-7O,21-DICARBOXILATO. LA EPLERENONA ES UN ANTAGONISTA DEL RECEPTOR DE ALDOSTERONAIT REFERS TO THE H FORM OF EPLERENONE (METHYL HYDROGEN 9,11-EPOXY-17-HYDROXY-3-OXOPREGN-4-ENE-7,21-DICARBOXYLATE, g-LACTONE) WHICH HAS A RAPID DISSOLUTION IN A WATERY MEDIUM AND IS CHARACTERIZED FOR PRESENTING IN THE FORM OF ORTHOROMBIC CRYSTAL; X-RAY DIFFRACTION PATTERN; MELTING POINT OF 247 ° C TO 251 ° C; PARTICLE SIZE D90 LESS THAN 400µm; IT ALSO REFERS TO A DRUG THAT INCLUDES 90% TO 100% OF FORM H AND THE REST CONSISTS OF EPLERENONE CRYSTALINE FORM L WITH A MONOCLINIC CRYSTAL SYSTEM; SOLVATED FORM OF EPLERENONE CRYSTALINE, EPLERENONE AMORPHOUS; USING FROM 10mg TO 1000mg. IT ALSO REFERS TO i) A METHOD FOR PREPARING FORM H; ii) EPLERENONE AMORPHOUS FREE OF THE CRYSTAL FORM; iii) METHOD TO PROMOTE THE CRYSTALLIZATION OF THE FORM H OF EPLERENONE THAT INCLUDES BANAR THE SOLUTION BEFORE CRYSTALLIZATION WITH BATTERY COMPOUNDS THAT IN A SUBSTANTIAL FORM ARE CRYSTALOGRAPHICALLY ISOESTRUCTURAL WITH THE EPLERENONE FORM HIDROEN, 5-METHYLHYL 9; 11O-DIEPOXIDO-17-HYDROXY-3-OXO-17O-PREGNAN-7O, 21-DICARBOXYLATE. EPLERENONE IS AN ALDOSTERONE RECEPTOR ANTAGONIST

PE2000001300A 1999-12-08 2000-12-06 CRYSTALLINE FORM OF EPLERENONE SHOWING AN INCREASE IN DISSOLUTION RATE PE20010917A1 (en)

Applications Claiming Priority (6)

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

Publications (1)

Publication Number Publication Date
PE20010917A1 true PE20010917A1 (en) 2001-09-10

Family

ID=27558585

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001300A PE20010917A1 (en) 1999-12-08 2000-12-06 CRYSTALLINE FORM OF EPLERENONE SHOWING AN INCREASE IN 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) NZ513961A (en)
PE (1) PE20010917A1 (en)
WO (1) WO2001042272A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2479383A1 (en) * 2002-03-20 2003-10-02 Pharmacia Corporation 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
EP2582365B1 (en) 2010-06-16 2019-03-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Compositions for stimulating reepithelialisation during wound healing
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
EP4395785A1 (en) 2021-08-31 2024-07-10 Inserm (Institut National de la Santé et de la Recherche Scientifique) 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
CN120754115A (en) * 2025-05-23 2025-10-10 远大医药(中国)有限公司 Eplerenone-containing composition, pharmaceutical preparation, preparation method and use thereof

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
BR9714510A (en) * 1996-12-11 2000-11-28 Searle & Co Process and preparation of 9,11-epoxy steroids and useful intermediates
DK1382351T3 (en) * 1999-03-05 2006-01-23 Searle Llc Combination therapy with angiotensin converting enzyme inhibitor and epoxy steroidal aldosterone antagonist to treat cardiovascular disease

Also Published As

Publication number Publication date
HUP0203032A2 (en) 2002-12-28
IL176511A (en) 2007-08-19
BR0008057A (en) 2002-04-23
HUP0203032A3 (en) 2003-04-28
NZ530028A (en) 2005-08-26
JP2003516414A (en) 2003-05-13
CA2362669A1 (en) 2001-06-14
NO20013856D0 (en) 2001-08-08
HK1050536A1 (en) 2003-06-27
AU784946B2 (en) 2006-08-03
CN1377365A (en) 2002-10-30
NZ513961A (en) 2004-02-27
MXPA01008056A (en) 2003-07-21
KR100607923B1 (en) 2006-08-04
CN1557833A (en) 2004-12-29
IL144764A0 (en) 2002-06-30
WO2001042272A2 (en) 2001-06-14
EA007934B1 (en) 2007-02-27
EP1177204A2 (en) 2002-02-06
EA200100871A1 (en) 2002-04-25
MY131878A (en) 2007-09-28
NO20013856L (en) 2001-10-08
KR20010112261A (en) 2001-12-20
AU2049201A (en) 2001-06-18
CN1152886C (en) 2004-06-09
CO5280211A1 (en) 2003-05-30
IL144764A (en) 2007-08-19
WO2001042272A3 (en) 2001-11-29
WO2001042272A9 (en) 2002-12-12

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