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PE20061126A1 - SOLID ORAL DOSAGE FORMS CONTAINING A LOW DOSE OF ESTRADIOL - Google Patents

SOLID ORAL DOSAGE FORMS CONTAINING A LOW DOSE OF ESTRADIOL

Info

Publication number
PE20061126A1
PE20061126A1 PE2005001279A PE2005001279A PE20061126A1 PE 20061126 A1 PE20061126 A1 PE 20061126A1 PE 2005001279 A PE2005001279 A PE 2005001279A PE 2005001279 A PE2005001279 A PE 2005001279A PE 20061126 A1 PE20061126 A1 PE 20061126A1
Authority
PE
Peru
Prior art keywords
estradiol
oral dosage
dosage form
solid oral
dosage forms
Prior art date
Application number
PE2005001279A
Other languages
Spanish (es)
Inventor
Kristina Muller
Torsten Wagner
Christian Zurth
Adrian Funke
Original Assignee
Bayer Schering Pharma Ag
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 Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of PE20061126A1 publication Critical patent/PE20061126A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY 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 TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY 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 TOILETRY 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 TOILETRY 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)

Abstract

SE REFIERE A UNA FORMA DE DOSIFICACION ORAL SOLIDA QUE COMPRENDE ESTRADIOL, UN HIDRATO, UNA SAL O UN DERIVADO DEL MISMO EN UNA CANTIDAD EQUIVALENTE ENTRE 0,01mg Y 0,5mg DE HEMIHIDRATO DE ESTRADIOL Y AL MENOS UN EXCIPIENTE FARMACEUTICAMENTE ACEPTABLE TENIENDO EN CUENTA QUE CUANDO HAY POLIVINILPIRROLIDONA LA RELACION DE PESO ENTRE LA POLIVILPIRROLIDONA Y EL ESTRADIOL ES MENOR QUE 10:1. EL DERIVADO DE ESTRADIOL ES SELECCIONADO DE VALERATO DE ESTRADIOL, ACETATO DE ESTRADIOL, PROPIONATO DE ESTRADIOL, BENZOATO DE ESTRADIOL, ENTRE OTROS. SE REFIERE TAMBIEN A LA FORMA DE DOSIFICACION CARACTERIZADA PORQUE MAS DE 70%, 80% o 90% DE ESTRADIOL SE DISUELVE EN 30 MINUTOS DONDE LA DETERMINACION SE REALIZA MEDIANTE EL SISTEMA DE PALETAS USANDO 900 ml DE AGUA A 37°C COMO MEDIO DE DISOLUCION Y 50 rpm COMO VELOCIDAD DE ROTACION. LA FORMA DE DOSIFICACION ORAL COMPRENDE UNA CANTIDAD DE HEMIHIDRATO DE ESTRADIOL ENTRE 0,05mg Y 0,4mg SIENDO UTIL EN EL TRATAMIENTO DE UNA CONDICION FISICA PROVOCADA POR LOS NIVELES ENDOGENOS INSUFICIENTES DE ESTRADIOLREFERS TO A SOLID ORAL DOSAGE FORM THAT INCLUDES ESTRADIOL, A HYDRATE, A SALT OR A DERIVATIVE OF THE SAME IN AN EQUIVALENT QUANTITY BETWEEN 0.01mg AND 0.5mg OF ESTRADIOL HEMIHYDRATE AND AT LEAST ONE EXCIPIENT STRADIOLLY ACCEPTED BY PHARMACEUTICALLY ACCEPTABLE WHEN THERE IS POLYVINYLPYRROLIDONE, THE WEIGHT RATIO BETWEEN POLYVYLPYRROLIDONE AND ESTRADIOL IS LESS THAN 10: 1. THE ESTRADIOL DERIVATIVE IS SELECTED FROM ESTRADIOL VALERATE, ESTRADIOL ACETATE, ESTRADIOL PROPIONATE, ESTRADIOL BENZOATE, AMONG OTHERS. IT ALSO REFERS TO THE CHARACTERIZED DOSAGE FORM BECAUSE MORE THAN 70%, 80% or 90% OF ESTRADIOL IS DISSOLVED IN 30 MINUTES WHERE THE DETERMINATION IS PERFORMED BY THE PADDLE SYSTEM USING 900 ml OF WATER AT 37 ° C AS A DISSOLUTION MEANS AND 50 rpm AS ROTATION SPEED. THE ORAL DOSAGE FORM INCLUDES AN AMOUNT OF ESTRADIOL HEMIHYDRATE BETWEEN 0.05mg AND 0.4mg BEING USEFUL IN THE TREATMENT OF A PHYSICAL CONDITION CAUSED BY INSUFFICIENT ENDOGENE LEVELS OF ESTRADIOL

PE2005001279A 2004-11-02 2005-11-02 SOLID ORAL DOSAGE FORMS CONTAINING A LOW DOSE OF ESTRADIOL PE20061126A1 (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20061126A1 true PE20061126A1 (en) 2006-11-11

Family

ID=34928627

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001279A PE20061126A1 (en) 2004-11-02 2005-11-02 SOLID ORAL 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 the 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
CN102985070A (en) * 2010-04-15 2013-03-20 拜耳知识产权有限责任公司 Very low-dosed solid oral dosage forms for HRT
CN112516149B (en) * 2020-07-21 2023-07-18 南方医科大学 Application of estradiol benzoate or its pharmaceutically acceptable salt in the preparation of anti-coronavirus medicine

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL125071C (en) * 1963-12-24
US4755386A (en) * 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5073374A (en) * 1988-11-30 1991-12-17 Schering Corporation Fast dissolving buccal tablet
FR2739558B1 (en) * 1995-10-05 1997-11-28 Innothera Lab Sa UNITAL GALENIC FORM FOR LOCAL HORMONOTHERAPY OF VAGINAL DROUGHT
FR2754179B1 (en) * 1996-10-08 1998-12-24 Theramex NOVEL HORMONONAL COMPOSITION AND ITS USE
US6326366B1 (en) * 2000-08-22 2001-12-04 Protein Technologies International Hormone replacement therapy
EP1330257B1 (en) * 2000-10-30 2005-08-31 University Of Zurich Gnrh analogues for treatment of urinary incontinence
ES2376649T3 (en) * 2000-12-15 2012-03-15 Novo Nordisk Femcare Ag USE OF A ESTRÓGEN IN THE PRODUCTION OF A COMPOSITION CONTAINING ESTRÓGENO FOR THE TREATMENT OF THE ATRÓFICA VAGINITIS.
FR2823976A1 (en) * 2001-04-25 2002-10-31 Theramex NOVEL HORMONAL COMPOSITION AND ITS USE
US20030018018A1 (en) * 2001-07-10 2003-01-23 Medical College Of Hampton Roads Ultra low dose oral contraceptives with sustained efficacy and induced amenorrhea
US6962908B2 (en) * 2001-12-21 2005-11-08 Warner Chilcott Company Inc. Oral pharmaceutical products containing 17 β-estradiol-3-lower alkanoate, method of administering the same and process of preparation
JP2004155779A (en) * 2002-10-16 2004-06-03 Taisho Pharmaceut Co Ltd Oral composition for prevention and treatment of menopause

Also Published As

Publication number Publication date
BRPI0517940A (en) 2008-10-21
NO20072704L (en) 2007-05-29
UY29185A1 (en) 2006-05-31
EA013262B1 (en) 2010-04-30
ZA200705012B (en) 2008-10-29
CA2585095A1 (en) 2006-05-11
AR053650A1 (en) 2007-05-16
EA200700979A1 (en) 2007-10-26
WO2006048261A2 (en) 2006-05-11
PA8651401A1 (en) 2006-12-07
CR9112A (en) 2007-11-23
GT200500315A (en) 2006-06-06
AU2005300658A1 (en) 2006-05-11
EP1814526A2 (en) 2007-08-08
JP2008518895A (en) 2008-06-05
IL182635A0 (en) 2007-07-24
CU20070094A7 (en) 2009-09-08
WO2006048261A3 (en) 2006-09-21
KR20070085558A (en) 2007-08-27
MX2007005281A (en) 2008-03-11
CN101094656A (en) 2007-12-26
TW200621312A (en) 2006-07-01

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