AU2015276321B2 - Stable formulations of testosterone undecanoate - Google Patents

Stable formulations of testosterone undecanoate Download PDF

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Publication number
AU2015276321B2
AU2015276321B2 AU2015276321A AU2015276321A AU2015276321B2 AU 2015276321 B2 AU2015276321 B2 AU 2015276321B2 AU 2015276321 A AU2015276321 A AU 2015276321A AU 2015276321 A AU2015276321 A AU 2015276321A AU 2015276321 B2 AU2015276321 B2 AU 2015276321B2
Authority
AU
Australia
Prior art keywords
formulation
testosterone undecanoate
propylene glycol
formulations
pharmaceutical formulation
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2015276321A
Other languages
English (en)
Other versions
AU2015276321A1 (en
Inventor
Gerritdina G. SCHOONUS-GERRITSMA
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme BV
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp & Dohme BV
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 Merck Sharp and Dohme Ltd, Merck Sharp & Dohme BV filed Critical Merck Sharp and Dohme Ltd
Publication of AU2015276321A1 publication Critical patent/AU2015276321A1/en
Application granted granted Critical
Publication of AU2015276321B2 publication Critical patent/AU2015276321B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • 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
    • A61P5/26—Androgens

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dispersion Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2015276321A 2014-06-17 2015-06-15 Stable formulations of testosterone undecanoate Ceased AU2015276321B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14172805.5 2014-06-17
EP14172805 2014-06-17
PCT/EP2015/063292 WO2015193224A1 (en) 2014-06-17 2015-06-15 Stable formulations of testosterone undecanoate

Publications (2)

Publication Number Publication Date
AU2015276321A1 AU2015276321A1 (en) 2016-11-10
AU2015276321B2 true AU2015276321B2 (en) 2019-10-24

Family

ID=50980940

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015276321A Ceased AU2015276321B2 (en) 2014-06-17 2015-06-15 Stable formulations of testosterone undecanoate

Country Status (12)

Country Link
US (1) US9925200B2 (enExample)
EP (1) EP3157505B1 (enExample)
JP (1) JP6618488B2 (enExample)
KR (1) KR20170020779A (enExample)
CN (1) CN106456782B (enExample)
AU (1) AU2015276321B2 (enExample)
BR (1) BR112016028192A2 (enExample)
CA (1) CA2950670A1 (enExample)
ES (1) ES2749008T3 (enExample)
MX (1) MX373197B (enExample)
RU (1) RU2708238C2 (enExample)
WO (1) WO2015193224A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110160168A1 (en) 2009-12-31 2011-06-30 Differential Drug Development Associates, Llc Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
WO2014143127A1 (en) 2013-03-15 2014-09-18 Differential Drug Development Associates Llc Emulsion formulations
UA128186C2 (uk) 2017-11-27 2024-05-01 Умекрайн Когнішн Аб ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ 3<font face="Symbol">a</font>-ЕТИНІЛ-3<font face="Symbol">b</font>-ГІДРОКСІАНДРОСТАН-17-ОНУ ОКСИМУ
EP3824296B1 (en) 2018-07-20 2026-04-01 Lipocine Inc. Oral pharmaceutical composition comprising testosterone tridecanoate and/or testosterone dodecanoate for treating liver diseases
US12403146B2 (en) 2019-10-30 2025-09-02 Marius Pharmaceuticals, Inc. Preferred oral testosterone undecanoate therapy to achieve testosterone replacement treatment

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997040823A1 (en) * 1996-04-26 1997-11-06 R.P. Scherer Limited Oral pharmaceutical compositions containing sex hormones
WO2000059482A1 (en) * 1999-04-01 2000-10-12 R.P. Scherer Corporation Oral pharmaceutical compositions containing long-chain triglycerides and lipophilic surfactants
US20080317844A1 (en) * 2005-04-15 2008-12-25 Clarus Therapeutics, Inc. Pharmaceutical Delivery Systems for Hydrophobic Drugs and Compositions Compositions Comprising Same
US20120135074A1 (en) * 2010-11-30 2012-05-31 Chandrashekar Giliyar High-Strength Testosterone Undecanoate Compositions
US20120244215A1 (en) * 2010-11-30 2012-09-27 Lipocine Inc. High-strength testosterone undecanoate compositions
US20130303495A1 (en) * 2009-12-31 2013-11-14 Sov Therapeutics Emulsion formulations

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4098802A (en) 1975-02-18 1978-07-04 Akzona Incorporated Oral pharmaceutical preparation having androgenic activity
US4147783A (en) 1974-02-28 1979-04-03 Akzona Incorporated Oral pharmaceutical preparation
NL189235C (nl) 1974-02-28 1993-02-16 Akzo Nv Werkwijze voor de bereiding van een oraal toe te dienen farmaceutisch preparaat met androgene werking.
NL7510104A (nl) 1975-08-27 1977-03-01 Akzo Nv Werkwijze ter bereiding van een oraal werkzaam farmaceutisch preparaat.
US5532002A (en) 1989-08-17 1996-07-02 Cortecs Limited Gelatin pharmaceutical formulations
CA2063791C (en) 1989-08-17 2000-12-19 Michael John Story Hard gelatine capsule containing fat-soluble nutrients.
CN1102095A (zh) 1993-10-30 1995-05-03 浙江医科大学 长效雄激素类制剂——十一酸睾丸注射液
GB9405304D0 (en) 1994-03-16 1994-04-27 Scherer Ltd R P Delivery systems for hydrophobic drugs
SE9700642D0 (sv) 1997-02-24 1997-02-24 Kronvall Stefan Med Ab Medel och sätt för förebyggande och behandling av det metabola syndromet
SI0999826T1 (en) 1997-07-29 2004-12-31 Pharmacia & Upjohn Company Self-emulsifying formulation for lipophilic compounds
US7396526B1 (en) * 1998-11-12 2008-07-08 Johnson & Johnson Consumer Companies, Inc. Skin care composition
US6652880B1 (en) * 1999-04-01 2003-11-25 R.P. Scherer Technologies, Inc. Oral pharmaceutical compositions containing long-chain triglycerides and liphophilic surfactants
JP2002541111A (ja) 1999-04-01 2002-12-03 アクゾ・ノベル・エヌ・ベー ウンデカン酸テストステロンとヒマシ油を含む調合物
RU2303981C2 (ru) * 2000-11-01 2007-08-10 Юнимед Фармасьютикалс, Инк. Способ лечения эректильной дисфункции и повышения либидо у мужчин
AU2005309808A1 (en) * 2004-11-24 2006-06-01 Merck & Co., Inc. Liquid and semi-solid pharmaceutical formulations for oral administration of a substituted amide
US8492369B2 (en) 2010-04-12 2013-07-23 Clarus Therapeutics Inc Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same
US20110160168A1 (en) * 2009-12-31 2011-06-30 Differential Drug Development Associates, Llc Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
WO2011129812A1 (en) * 2010-04-12 2011-10-20 Clarus Therapeutics, Inc. Oral testosterone ester formulations and methods of treating testoterone deficiency comprising same
EP4234015A3 (en) 2013-03-15 2023-11-22 Tolmar, Inc. Methods of treating testosterone deficiency
US10245273B2 (en) 2013-12-26 2019-04-02 Clarus Therapeutics, Inc. Oral pharmaceutical products and methods of use combining testosterone esters with hypolipidemic agents

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997040823A1 (en) * 1996-04-26 1997-11-06 R.P. Scherer Limited Oral pharmaceutical compositions containing sex hormones
WO2000059482A1 (en) * 1999-04-01 2000-10-12 R.P. Scherer Corporation Oral pharmaceutical compositions containing long-chain triglycerides and lipophilic surfactants
US20080317844A1 (en) * 2005-04-15 2008-12-25 Clarus Therapeutics, Inc. Pharmaceutical Delivery Systems for Hydrophobic Drugs and Compositions Compositions Comprising Same
US20130303495A1 (en) * 2009-12-31 2013-11-14 Sov Therapeutics Emulsion formulations
US20120135074A1 (en) * 2010-11-30 2012-05-31 Chandrashekar Giliyar High-Strength Testosterone Undecanoate Compositions
US20120244215A1 (en) * 2010-11-30 2012-09-27 Lipocine Inc. High-strength testosterone undecanoate compositions

Also Published As

Publication number Publication date
MX373197B (es) 2020-05-12
JP2017522283A (ja) 2017-08-10
AU2015276321A1 (en) 2016-11-10
RU2017101240A (ru) 2018-07-17
CA2950670A1 (en) 2015-12-23
MX2016016612A (es) 2017-03-20
CN106456782B (zh) 2020-02-18
EP3157505A1 (en) 2017-04-26
WO2015193224A1 (en) 2015-12-23
BR112016028192A2 (pt) 2017-08-22
CN106456782A (zh) 2017-02-22
RU2017101240A3 (enExample) 2019-02-22
EP3157505B1 (en) 2019-07-24
KR20170020779A (ko) 2017-02-24
ES2749008T3 (es) 2020-03-18
RU2708238C2 (ru) 2019-12-05
US20170136033A1 (en) 2017-05-18
US9925200B2 (en) 2018-03-27
JP6618488B2 (ja) 2019-12-11

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired