CO5280211A1 - EPLERENONE CRYSTAL FORM EXHIBITING IMPROVED DISSOLUTION RAT - Google Patents

EPLERENONE CRYSTAL FORM EXHIBITING IMPROVED DISSOLUTION RAT

Info

Publication number
CO5280211A1
CO5280211A1 CO00094075A CO00094075A CO5280211A1 CO 5280211 A1 CO5280211 A1 CO 5280211A1 CO 00094075 A CO00094075 A CO 00094075A CO 00094075 A CO00094075 A CO 00094075A CO 5280211 A1 CO5280211 A1 CO 5280211A1
Authority
CO
Colombia
Prior art keywords
eplerenone
crystalline
rat
crystal form
exhibiting improved
Prior art date
Application number
CO00094075A
Other languages
Spanish (es)
Inventor
P Barton Kathleen
Thomas B Borehardt
V Carlos Marlon
Desai Subhash
Leonard J Ferro
Henry T Gaud
Scott Ganser
Clay R Little
S Mudipalli Partha
Mark A Pietz
Daniel R Pilipauskas
L Sing Yuen-Lung
Glen L Stahl
Joseph J Wieczoreck
Y Chris Yan
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 CO5280211A1 publication Critical patent/CO5280211A1/en

Links

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)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Una Forma H cristalina de eplerenona que tiene un sistema de cristal ortorhómbico y un patrón de difracción en polvo de rayos X con un pico a 12,0 ± 0,2 grados 2 ? La eplerenona cristalina de la Reivindicación 1 que tiene un punto de fusión en un rango de desde alrededor de 247°C hasta alrededor de 251°C. La eplerenona cristalina de la Reivindicación 1 en la forma de partículas que tiene un tamaño de partículas D90 de menos de alrededor de 400 µm.La eplerenona cristalina de la Reivindicación 1 en la forma de partículas que tiene un tamaño de partículas D90 de alrededor de 25 hasta alrededor de 400 µm.La eplerenona cristalina de la Reivindicación 1 en la forma de partículas que tiene un tamaño de partículas D90 de alrededor de 0,01 hasta alrededor de 15 µm. Una sustancia de droga de eplerenona que comprenden eplerenona cristalina de Forma H en una cantidad detectable.La sustancia de droga de eplerenona de la Reivindicación 6 que comprende alrededor de 90% hasta alrededor de 100% de eplerenona cristalina de Forma H.La sustancia de droga de eplerenona de la Reivindicación 6 que es sustancialmente eplerenona cristalina de Forma H de fase pura.A crystalline H-form of eplerenone that has an orthorhombic crystal system and an X-ray powder diffraction pattern with a peak at 12.0 ± 0.2 degrees 2? The crystalline eplerenone of Claim 1 having a melting point in a range of from about 247 ° C to about 251 ° C. The crystalline eplerenone of Claim 1 in the form of particles having a D90 particle size of less than about 400 µm. The crystalline eplerenone of Claim 1 in the form of particles having a D90 particle size of about 25 up to about 400 µm. The crystalline eplerenone of Claim 1 in the form of particles having a particle size D90 from about 0.01 to about 15 µm. An eplerenone drug substance comprising crystalline eplerenone of Form H in a detectable amount. The eplerenone drug substance of Claim 6 comprising about 90% to about 100% crystalline eplerenone of Form H. The drug substance of eplerenone of Claim 6 which is substantially pure phase Form H crystalline eplerenone.

CO00094075A 1999-12-08 2000-12-11 EPLERENONE CRYSTAL FORM EXHIBITING IMPROVED DISSOLUTION RAT CO5280211A1 (en)

Applications Claiming Priority (6)

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

Publications (1)

Publication Number Publication Date
CO5280211A1 true CO5280211A1 (en) 2003-05-30

Family

ID=27558585

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00094075A CO5280211A1 (en) 1999-12-08 2000-12-11 EPLERENONE CRYSTAL FORM EXHIBITING IMPROVED DISSOLUTION RAT

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
WO2003080181A2 (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
WO2011141456A1 (en) 2010-05-10 2011-11-17 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
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
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

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
SI1165136T1 (en) * 1999-03-05 2004-02-29 G.D. 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
BR0008057A (en) 2002-04-23
IL176511A (en) 2007-08-19
CN1152886C (en) 2004-06-09
WO2001042272A2 (en) 2001-06-14
IL144764A (en) 2007-08-19
EP1177204A2 (en) 2002-02-06
MXPA01008056A (en) 2003-07-21
AU2049201A (en) 2001-06-18
KR20010112261A (en) 2001-12-20
IL144764A0 (en) 2002-06-30
CN1557833A (en) 2004-12-29
CA2362669A1 (en) 2001-06-14
PE20010917A1 (en) 2001-09-10
NZ530028A (en) 2005-08-26
EA200100871A1 (en) 2002-04-25
MY131878A (en) 2007-09-28
NO20013856D0 (en) 2001-08-08
JP2003516414A (en) 2003-05-13
NO20013856L (en) 2001-10-08
CN1377365A (en) 2002-10-30
AU784946B2 (en) 2006-08-03
HK1050536A1 (en) 2003-06-27
HUP0203032A2 (en) 2002-12-28
NZ513961A (en) 2004-02-27
KR100607923B1 (en) 2006-08-04
EA007934B1 (en) 2007-02-27
HUP0203032A3 (en) 2003-04-28
WO2001042272A9 (en) 2002-12-12
WO2001042272A3 (en) 2001-11-29

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