CA2950670A1 - Stable formulations of testosterone undecanoate - Google Patents

Stable formulations of testosterone undecanoate Download PDF

Info

Publication number
CA2950670A1
CA2950670A1 CA2950670A CA2950670A CA2950670A1 CA 2950670 A1 CA2950670 A1 CA 2950670A1 CA 2950670 A CA2950670 A CA 2950670A CA 2950670 A CA2950670 A CA 2950670A CA 2950670 A1 CA2950670 A1 CA 2950670A1
Authority
CA
Canada
Prior art keywords
formulation
surfactant
pharmaceutical formulation
formulations
propylene glycol
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.)
Abandoned
Application number
CA2950670A
Other languages
English (en)
French (fr)
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 and Dohme BV
Original Assignee
Merck Sharp and 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 BV filed Critical Merck Sharp and Dohme BV
Publication of CA2950670A1 publication Critical patent/CA2950670A1/en
Abandoned legal-status Critical Current

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)
CA2950670A 2014-06-17 2015-06-15 Stable formulations of testosterone undecanoate Abandoned CA2950670A1 (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 (1)

Publication Number Publication Date
CA2950670A1 true CA2950670A1 (en) 2015-12-23

Family

ID=50980940

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2950670A Abandoned CA2950670A1 (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
PL2519230T3 (pl) 2009-12-31 2019-05-31 Marius Pharmaceuticals Llc Modulacja rozpuszczalności, stabilności, absorpcji, metabolizmu i profilu farmakokinetycznego leków lipofilowych przez sterole
CN105188670B (zh) 2013-03-15 2018-11-02 马留斯医药有限责任公司 乳液制剂
CN111432805B (zh) 2017-11-27 2023-02-17 梅克里内科尼蒂翁公司 3α-乙炔基-3β-羟基雄甾烷-17-酮肟的药物制剂
US12150945B2 (en) 2018-07-20 2024-11-26 Lipocine Inc. Liver disease
US12403146B2 (en) 2019-10-30 2025-09-02 Marius Pharmaceuticals, Inc. Preferred oral testosterone undecanoate therapy to achieve testosterone replacement treatment

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4147783A (en) 1974-02-28 1979-04-03 Akzona Incorporated Oral pharmaceutical preparation
US4098802A (en) 1975-02-18 1978-07-04 Akzona Incorporated Oral pharmaceutical preparation having androgenic activity
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
ATE113471T1 (de) 1989-08-17 1994-11-15 Cortecs Ltd Arzneiformulierungen.
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
GB9608719D0 (en) * 1996-04-26 1996-07-03 Scherer Ltd R P Pharmaceutical compositions
SE9700642D0 (sv) 1997-02-24 1997-02-24 Kronvall Stefan Med Ab Medel och sätt för förebyggande och behandling av det metabola syndromet
CN1208047C (zh) 1997-07-29 2005-06-29 法玛西雅厄普约翰美国公司 亲脂性化合物的自体乳化剂
US7396526B1 (en) * 1998-11-12 2008-07-08 Johnson & Johnson Consumer Companies, Inc. Skin care composition
GB9907715D0 (en) 1999-04-01 1999-05-26 Scherer Corp R P Pharmaceutical compositions
US6652880B1 (en) * 1999-04-01 2003-11-25 R.P. Scherer Technologies, Inc. Oral pharmaceutical compositions containing long-chain triglycerides and liphophilic surfactants
RU2246296C2 (ru) 1999-04-01 2005-02-20 Акцо Нобель Н.В. Композиция, включающая ундеканоат тестостерона и касторовое масло
RU2303981C2 (ru) * 2000-11-01 2007-08-10 Юнимед Фармасьютикалс, Инк. Способ лечения эректильной дисфункции и повышения либидо у мужчин
KR20070084531A (ko) * 2004-11-24 2007-08-24 머크 앤드 캄파니 인코포레이티드 치환된 아미드의 경구 투여용 액체 및 반고체 약제학적제형
US8492369B2 (en) 2010-04-12 2013-07-23 Clarus Therapeutics Inc Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same
WO2006113505A2 (en) 2005-04-15 2006-10-26 Clarus Therapeutics, Inc. Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same
US20130303495A1 (en) * 2009-12-31 2013-11-14 Sov Therapeutics Emulsion formulations
PL2519230T3 (pl) * 2009-12-31 2019-05-31 Marius Pharmaceuticals Llc Modulacja rozpuszczalności, stabilności, absorpcji, metabolizmu i profilu farmakokinetycznego leków lipofilowych przez sterole
SG184540A1 (en) 2010-04-12 2012-11-29 Clarus Therapeutics Inc Oral testosterone ester formulations and methods of treating testoterone deficiency comprising same
US9034858B2 (en) * 2010-11-30 2015-05-19 Lipocine Inc. High-strength testosterone undecanoate compositions
US20120135074A1 (en) * 2010-11-30 2012-05-31 Chandrashekar Giliyar High-Strength Testosterone Undecanoate Compositions
CA2905703A1 (en) 2013-03-15 2014-09-18 Clarus Therapeutics, 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

Also Published As

Publication number Publication date
JP2017522283A (ja) 2017-08-10
RU2708238C2 (ru) 2019-12-05
EP3157505B1 (en) 2019-07-24
KR20170020779A (ko) 2017-02-24
ES2749008T3 (es) 2020-03-18
MX2016016612A (es) 2017-03-20
CN106456782B (zh) 2020-02-18
RU2017101240A3 (enExample) 2019-02-22
US9925200B2 (en) 2018-03-27
AU2015276321B2 (en) 2019-10-24
AU2015276321A1 (en) 2016-11-10
US20170136033A1 (en) 2017-05-18
MX373197B (es) 2020-05-12
EP3157505A1 (en) 2017-04-26
CN106456782A (zh) 2017-02-22
WO2015193224A1 (en) 2015-12-23
BR112016028192A2 (pt) 2017-08-22
JP6618488B2 (ja) 2019-12-11
RU2017101240A (ru) 2018-07-17

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20200527

FZDE Discontinued

Effective date: 20221107