WO2006048261A3 - Oral solid dosage forms containing a low dose of estradiol - Google Patents

Oral solid dosage forms containing a low dose of estradiol Download PDF

Info

Publication number
WO2006048261A3
WO2006048261A3 PCT/EP2005/011726 EP2005011726W WO2006048261A3 WO 2006048261 A3 WO2006048261 A3 WO 2006048261A3 EP 2005011726 W EP2005011726 W EP 2005011726W WO 2006048261 A3 WO2006048261 A3 WO 2006048261A3
Authority
WO
WIPO (PCT)
Prior art keywords
estradiol
dosage forms
low dose
oral solid
solid dosage
Prior art date
Application number
PCT/EP2005/011726
Other languages
French (fr)
Other versions
WO2006048261A2 (en
Inventor
Adrian Funke
Kristina Mueller
Torsten Wagner
Christian Zurth
Original Assignee
Schering Ag
Adrian Funke
Kristina Mueller
Torsten Wagner
Christian Zurth
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 Schering Ag, Adrian Funke, Kristina Mueller, Torsten Wagner, Christian Zurth filed Critical Schering Ag
Priority to MX2007005281A priority Critical patent/MX2007005281A/en
Priority to AU2005300658A priority patent/AU2005300658A1/en
Priority to CA002585095A priority patent/CA2585095A1/en
Priority to EA200700979A priority patent/EA013262B1/en
Priority to EP05800512A priority patent/EP1814526A2/en
Priority to BRPI0517940-8A priority patent/BRPI0517940A/en
Priority to JP2007538360A priority patent/JP2008518895A/en
Publication of WO2006048261A2 publication Critical patent/WO2006048261A2/en
Publication of WO2006048261A3 publication Critical patent/WO2006048261A3/en
Priority to IL182635A priority patent/IL182635A0/en
Priority to NO20072704A priority patent/NO20072704L/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens

Abstract

The present invention relates to oral solid dosage forms containing a very low dose of estradiol. The dosage forms are formulated in a manner so as to avoid degradation of the estradiol and to minimise the content of polyvinylpyrrolidone, while still achieving similar fast dissolution of the estradiol. The dosage forms are useful in preventing or treating a physical condition in a woman caused by insufficient endogenous levels of estradiol.
PCT/EP2005/011726 2004-11-02 2005-11-01 Oral solid dosage forms containing a low dose of estradiol WO2006048261A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
MX2007005281A MX2007005281A (en) 2004-11-02 2005-11-01 Oral solid dosage forms containing a low dose of estradiol.
AU2005300658A AU2005300658A1 (en) 2004-11-02 2005-11-01 Oral solid dosage forms containing a low dose of estradiol
CA002585095A CA2585095A1 (en) 2004-11-02 2005-11-01 Oral solid dosage forms containing a low dose of estradiol
EA200700979A EA013262B1 (en) 2004-11-02 2005-11-01 Oral sold dosage forms containing a low dose of estradiol
EP05800512A EP1814526A2 (en) 2004-11-02 2005-11-01 Oral solid dosage forms containing a low dose of estradiol
BRPI0517940-8A BRPI0517940A (en) 2004-11-02 2005-11-01 oral solid dosage forms containing a low dose of estradiol as well as a process for the manufacture and use thereof
JP2007538360A JP2008518895A (en) 2004-11-02 2005-11-01 Oral solid formulation containing low dose of estradiol
IL182635A IL182635A0 (en) 2004-11-02 2007-04-18 Oral solid dosage forms containing a low dose of estradiol
NO20072704A NO20072704L (en) 2004-11-02 2007-05-29 Oral solid dosage forms containing a low oestradiol dose

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04078014 2004-11-02
EP04078014.0 2004-11-02

Publications (2)

Publication Number Publication Date
WO2006048261A2 WO2006048261A2 (en) 2006-05-11
WO2006048261A3 true WO2006048261A3 (en) 2006-09-21

Family

ID=34928627

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2005/011726 WO2006048261A2 (en) 2004-11-02 2005-11-01 Oral solid dosage forms containing a low dose of estradiol

Country Status (21)

Country Link
EP (1) EP1814526A2 (en)
JP (1) JP2008518895A (en)
KR (1) KR20070085558A (en)
CN (1) CN101094656A (en)
AR (1) AR053650A1 (en)
AU (1) AU2005300658A1 (en)
BR (1) BRPI0517940A (en)
CA (1) CA2585095A1 (en)
CR (1) CR9112A (en)
CU (1) CU20070094A7 (en)
EA (1) EA013262B1 (en)
GT (1) GT200500315A (en)
IL (1) IL182635A0 (en)
MX (1) MX2007005281A (en)
NO (1) NO20072704L (en)
PA (1) PA8651401A1 (en)
PE (1) PE20061126A1 (en)
TW (1) TW200621312A (en)
UY (1) UY29185A1 (en)
WO (1) WO2006048261A2 (en)
ZA (1) ZA200705012B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8022053B2 (en) 2004-11-02 2011-09-20 Bayer Schering Pharma Aktiengesellschaft Oral solid dosage forms containing a low dose of estradiol
KR20080047957A (en) * 2006-11-27 2008-05-30 주식회사 엠디바이오알파 Pharmaceutical composition for treatment and prevention of hypertension
DE102009007771B4 (en) 2009-02-05 2012-02-16 Bayer Schering Pharma Aktiengesellschaft Buccal administration system containing 17α-estradiol
AU2011240102B2 (en) 2010-04-15 2015-07-23 Bayer Intellectual Property Gmbh Very low-dosed solid oral dosage forms for HRT
ES2533584T3 (en) 2010-04-15 2015-04-13 Bayer Intellectual Property Gmbh Solid low dose oral dosage forms for TSH
CN112516149B (en) * 2020-07-21 2023-07-18 南方医科大学 Application of estradiol benzoate or pharmaceutically acceptable salt thereof in preparation of anti-coronavirus drugs

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3318925A (en) * 1963-12-24 1967-05-09 Ciba Geigy Corp Methylated estrones
WO1987004342A1 (en) * 1986-01-22 1987-07-30 Key Pharmaceuticals, Inc. Buccal formulation
EP0371466A1 (en) * 1988-11-30 1990-06-06 Schering Corporation Fast buccal tablet
WO1997012600A1 (en) * 1995-10-05 1997-04-10 Laboratoire Innothera, S.A. Unit galenical form for local hormonotherapy of vaginal dryness
US6326366B1 (en) * 2000-08-22 2001-12-04 Protein Technologies International Hormone replacement therapy
WO2002047692A1 (en) * 2000-12-15 2002-06-20 Novo Nordisk A/S Use of an oestrogen in the manufacture of a composition containing oestrogen for the treatment of atrophic vaginitis
FR2823976A1 (en) * 2001-04-25 2002-10-31 Theramex NOVEL HORMONAL COMPOSITION AND ITS USE
WO2003055495A1 (en) * 2001-12-21 2003-07-10 Galen (Chemicals) Limited ORAL PHARMACEUTICAL PRODUCTS CONTAINING 17β-ESTRADIOL-3-LOWER ALKANOATE, METHOD OF ADMINISTERING THE SAME AND PROCESS OF PREPARATION

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2754179B1 (en) * 1996-10-08 1998-12-24 Theramex NOVEL HORMONONAL COMPOSITION AND ITS USE
AU2001295359A1 (en) * 2000-10-30 2002-05-15 University Of Zurich GnRH analogues for treatment of urinary incontinence
US20030018018A1 (en) * 2001-07-10 2003-01-23 Medical College Of Hampton Roads Ultra low dose oral contraceptives with sustained efficacy and induced amenorrhea
JP2004155779A (en) * 2002-10-16 2004-06-03 Taisho Pharmaceut Co Ltd Peroral composition for preventing and treating climacteric symptom

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3318925A (en) * 1963-12-24 1967-05-09 Ciba Geigy Corp Methylated estrones
WO1987004342A1 (en) * 1986-01-22 1987-07-30 Key Pharmaceuticals, Inc. Buccal formulation
EP0371466A1 (en) * 1988-11-30 1990-06-06 Schering Corporation Fast buccal tablet
WO1997012600A1 (en) * 1995-10-05 1997-04-10 Laboratoire Innothera, S.A. Unit galenical form for local hormonotherapy of vaginal dryness
US6326366B1 (en) * 2000-08-22 2001-12-04 Protein Technologies International Hormone replacement therapy
WO2002047692A1 (en) * 2000-12-15 2002-06-20 Novo Nordisk A/S Use of an oestrogen in the manufacture of a composition containing oestrogen for the treatment of atrophic vaginitis
FR2823976A1 (en) * 2001-04-25 2002-10-31 Theramex NOVEL HORMONAL COMPOSITION AND ITS USE
WO2003055495A1 (en) * 2001-12-21 2003-07-10 Galen (Chemicals) Limited ORAL PHARMACEUTICAL PRODUCTS CONTAINING 17β-ESTRADIOL-3-LOWER ALKANOATE, METHOD OF ADMINISTERING THE SAME AND PROCESS OF PREPARATION

Also Published As

Publication number Publication date
GT200500315A (en) 2006-06-06
EA200700979A1 (en) 2007-10-26
CR9112A (en) 2007-11-23
PE20061126A1 (en) 2006-11-11
CU20070094A7 (en) 2009-09-08
JP2008518895A (en) 2008-06-05
PA8651401A1 (en) 2006-12-07
KR20070085558A (en) 2007-08-27
ZA200705012B (en) 2008-10-29
BRPI0517940A (en) 2008-10-21
TW200621312A (en) 2006-07-01
CN101094656A (en) 2007-12-26
IL182635A0 (en) 2007-07-24
AU2005300658A1 (en) 2006-05-11
AR053650A1 (en) 2007-05-16
NO20072704L (en) 2007-05-29
UY29185A1 (en) 2006-05-31
EP1814526A2 (en) 2007-08-08
MX2007005281A (en) 2008-03-11
EA013262B1 (en) 2010-04-30
CA2585095A1 (en) 2006-05-11
WO2006048261A2 (en) 2006-05-11

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