WO2008083192A3 - Methods and formulations for improved bioavailability of antiprogestins - Google Patents

Methods and formulations for improved bioavailability of antiprogestins Download PDF

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Publication number
WO2008083192A3
WO2008083192A3 PCT/US2007/088891 US2007088891W WO2008083192A3 WO 2008083192 A3 WO2008083192 A3 WO 2008083192A3 US 2007088891 W US2007088891 W US 2007088891W WO 2008083192 A3 WO2008083192 A3 WO 2008083192A3
Authority
WO
WIPO (PCT)
Prior art keywords
improved bioavailability
antiprogestins
formulations
methods
antiprogestin
Prior art date
Application number
PCT/US2007/088891
Other languages
French (fr)
Other versions
WO2008083192A2 (en
WO2008083192A8 (en
Inventor
Joseph Podolski
Original Assignee
Repros Therapeutics Inc
Joseph Podolski
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 Repros Therapeutics Inc, Joseph Podolski filed Critical Repros Therapeutics Inc
Priority to EP07869940A priority Critical patent/EP2094275A2/en
Priority to MX2009006912A priority patent/MX2009006912A/en
Priority to AU2007339820A priority patent/AU2007339820A1/en
Priority to CA002672888A priority patent/CA2672888A1/en
Priority to EA200970646A priority patent/EA200970646A1/en
Priority to JP2009544257A priority patent/JP2010514793A/en
Publication of WO2008083192A2 publication Critical patent/WO2008083192A2/en
Publication of WO2008083192A3 publication Critical patent/WO2008083192A3/en
Priority to NO20092271A priority patent/NO20092271L/en
Publication of WO2008083192A8 publication Critical patent/WO2008083192A8/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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • 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
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Abstract

Compositions comprising an antiprogestin and having improved bioavailability are provided. In one aspect, compositions comprising particles of an antiprogestin deposited on a carrier substrate are provided. In another aspect, compositions comprising a micronized antiprogestin are provided. Also provided is the use of compositions comprising an antiprogestin and having improved bioavailability for the treatment of endometriosis, uterine fibroids, dysmenorrhea, and meningiomas.
PCT/US2007/088891 2006-12-28 2007-12-27 Methods and formulations for improved bioavailability of antiprogestins WO2008083192A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
EP07869940A EP2094275A2 (en) 2006-12-28 2007-12-27 Methods and formulations for improved bioavailability of antiprogestins
MX2009006912A MX2009006912A (en) 2006-12-28 2007-12-27 Methods and formulations for improved bioavalability of antiprogestins.
AU2007339820A AU2007339820A1 (en) 2006-12-28 2007-12-27 Methods and formulations for improved bioavailability of antiprogestins
CA002672888A CA2672888A1 (en) 2006-12-28 2007-12-27 Methods and formulations for improved bioavailability of antiprogestins
EA200970646A EA200970646A1 (en) 2006-12-28 2007-12-27 METHODS AND COMPOSITIONS FOR IMPROVING ANTI-PROGESTIN BIO-ACCESSIBILITY
JP2009544257A JP2010514793A (en) 2006-12-28 2007-12-27 Methods and formulations for improving the bioavailability of antiprogestins
NO20092271A NO20092271L (en) 2006-12-28 2009-06-12 Methods and formulations for improved bioavailability of antiprogestins

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US88242306P 2006-12-28 2006-12-28
US60/882,423 2006-12-28
US88537207P 2007-01-17 2007-01-17
US60/885,372 2007-01-17

Publications (3)

Publication Number Publication Date
WO2008083192A2 WO2008083192A2 (en) 2008-07-10
WO2008083192A3 true WO2008083192A3 (en) 2008-11-27
WO2008083192A8 WO2008083192A8 (en) 2009-07-09

Family

ID=39589194

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/088891 WO2008083192A2 (en) 2006-12-28 2007-12-27 Methods and formulations for improved bioavailability of antiprogestins

Country Status (14)

Country Link
EP (1) EP2094275A2 (en)
JP (1) JP2010514793A (en)
KR (1) KR20090086470A (en)
AR (1) AR064697A1 (en)
AU (1) AU2007339820A1 (en)
CA (1) CA2672888A1 (en)
CL (1) CL2007003855A1 (en)
CO (1) CO6190605A2 (en)
EA (1) EA200970646A1 (en)
EC (1) ECSP099536A (en)
MX (1) MX2009006912A (en)
NO (1) NO20092271L (en)
TW (1) TW200831110A (en)
WO (1) WO2008083192A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8299050B2 (en) * 2008-01-29 2012-10-30 Laboratoire Hra-Pharma Method for treating uterine fibroids
US8512745B2 (en) 2008-12-08 2013-08-20 Laboratoire Hra Pharma Ulipristal acetate tablets
NZ595790A (en) 2009-04-14 2013-11-29 Hra Pharma Lab Method for on-demand contraception
EP2471537A1 (en) * 2010-12-30 2012-07-04 PregLem S.A. Treatment of pain associated with dislocation of basal endometrium
EP2545922A1 (en) 2011-07-12 2013-01-16 PregLem S.A. Treatment of excessive menstrual bleeding associated with uterine fibroids
WO2013059664A1 (en) * 2011-10-21 2013-04-25 Seachaid Pharmaceuticals, Inc. Pharmaceutical compositions and uses thereof
FR2997627B1 (en) * 2012-11-08 2015-01-16 Hra Pharma Lab CO-MICRONIZATION PRODUCT COMPRISING ULIPRISTAL ACETATE
FR2997628B1 (en) * 2012-11-08 2015-01-16 Hra Pharma Lab CO-MICRONIZATION PRODUCT COMPRISING A SELECTIVE MODULATOR OF PROGESTERONE RECEPTORS
FR2999081B1 (en) * 2012-12-06 2015-02-27 Hra Pharma Lab SOLID DISPERSION OF A SELECTIVE PROGESTERONE RECEPTOR MODULATOR
SG11201507260QA (en) 2013-04-10 2015-10-29 Preglem Sa Progesteron receptor modulators for use in the therapy of uterine fibroids
US20200069702A1 (en) * 2016-12-09 2020-03-05 Repros Therapeutics Inc. Oral pharmaceutical compositions comprising an unmicronized selective progesterone receptor as active agent
WO2017216637A2 (en) 2017-08-04 2017-12-21 Alvogen Malta Operations (Row) Ltd Tablet form including ulipristal acetate and the methods for its preparation
WO2023033900A1 (en) 2021-09-06 2023-03-09 Slayback Pharma Llc Pharmaceutical compositions of mifepristone

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997041145A1 (en) * 1996-05-01 1997-11-06 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents
WO2001037808A1 (en) * 1999-11-23 2001-05-31 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
WO2002069978A1 (en) * 2001-03-01 2002-09-12 Laboratoires Besins International Progestin co-micronized with a surfactant, pharmaceutical composition comprising same, methods for making same and uses thereof
US20050220825A1 (en) * 2004-03-10 2005-10-06 Adrian Funke Molecular dispersions of drospirenone
WO2007038796A1 (en) * 2005-09-29 2007-04-05 Repros Therapeutics Inc. Formulations with improved bioavailability, comprising a steroid derivative and a polyglycolysed glyceride

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997041145A1 (en) * 1996-05-01 1997-11-06 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents
WO2001037808A1 (en) * 1999-11-23 2001-05-31 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
WO2002069978A1 (en) * 2001-03-01 2002-09-12 Laboratoires Besins International Progestin co-micronized with a surfactant, pharmaceutical composition comprising same, methods for making same and uses thereof
US20050220825A1 (en) * 2004-03-10 2005-10-06 Adrian Funke Molecular dispersions of drospirenone
WO2007038796A1 (en) * 2005-09-29 2007-04-05 Repros Therapeutics Inc. Formulations with improved bioavailability, comprising a steroid derivative and a polyglycolysed glyceride

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ATTARDI BARBARA J ET AL: "CDB-4124 and its putative monodemethylated metabolite, CDB-4453, are potent antiprogestins with reduced antiglucocorticoid activity: In vitro comparison to mifepristone and CDB-2914", MOLECULAR AND CELLULAR ENDOCRINOLOGY, vol. 188, no. 1-2, 25 February 2002 (2002-02-25), pages 111 - 123, XP002496575, ISSN: 0303-7207 *
CHAMBIN O ET AL: "INTEREST OF MULTIFUNCTIONAL LIPID EXCIPIENTS: CASE OF GELUCIRE 44/14", DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, NEW YORK, NY, US, vol. 31, no. 6, 1 July 2005 (2005-07-01), pages 527 - 534, XP009059038, ISSN: 0363-9045 *

Also Published As

Publication number Publication date
AR064697A1 (en) 2009-04-22
CL2007003855A1 (en) 2008-03-14
EP2094275A2 (en) 2009-09-02
AU2007339820A1 (en) 2008-07-10
MX2009006912A (en) 2009-08-12
NO20092271L (en) 2009-08-06
ECSP099536A (en) 2009-08-28
CA2672888A1 (en) 2008-07-10
WO2008083192A2 (en) 2008-07-10
EA200970646A1 (en) 2009-12-30
WO2008083192A8 (en) 2009-07-09
KR20090086470A (en) 2009-08-12
JP2010514793A (en) 2010-05-06
CO6190605A2 (en) 2010-08-19
TW200831110A (en) 2008-08-01

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