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
Priority to EP04078014.0 priority Critical
Priority to EP04078014 priority
Application filed by Schering Ag, Adrian Funke, Kristina Mueller, Torsten Wagner, Christian Zurth filed Critical Schering Ag
Publication of WO2006048261A2 publication Critical patent/WO2006048261A2/en
Publication of WO2006048261A3 publication Critical patent/WO2006048261A3/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens

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 (2)

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

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CA002585095A CA2585095A1 (en) 2004-11-02 2005-11-01 Oral solid 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
MX2007005281A MX2007005281A (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
AU2005300658A AU2005300658A1 (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
JP2007538360A JP2008518895A (en) 2004-11-02 2005-11-01 Oral solid formulation containing low dose of estradiol
IL182635A IL182635D0 (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 dose of ostradiol

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) IL182635D0 (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 (5)

* 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
JP5852639B2 (en) 2010-04-15 2016-02-03 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH Low dose solid oral dosage form for HRT
BR112012026115B1 (en) 2010-04-15 2019-12-24 Bayer Ip Gmbh solid oral dosage form, its use, and packaging unit

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
JP2004512369A (en) * 2000-10-30 2004-04-22 ユニバーシティ・オブ・チューリッヒ GNRH analogs for the 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
CA2585095A1 (en) 2006-05-11
JP2008518895A (en) 2008-06-05
WO2006048261A2 (en) 2006-05-11
EA200700979A1 (en) 2007-10-26
AR053650A1 (en) 2007-05-16
GT200500315A (en) 2006-06-06
NO20072704L (en) 2007-05-29
PE20061126A1 (en) 2006-11-11
EA013262B1 (en) 2010-04-30
AU2005300658A1 (en) 2006-05-11
CN101094656A (en) 2007-12-26
TW200621312A (en) 2006-07-01
BRPI0517940A (en) 2008-10-21
IL182635D0 (en) 2007-07-24
MX2007005281A (en) 2008-03-11
CU20070094A7 (en) 2009-09-08
UY29185A1 (en) 2006-05-31
ZA200705012B (en) 2008-10-29
EP1814526A2 (en) 2007-08-08
CR9112A (en) 2007-11-23
PA8651401A1 (en) 2006-12-07
KR20070085558A (en) 2007-08-27

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