CA2722408C - Lipid composition for enhancing steroid solubility - Google Patents

Lipid composition for enhancing steroid solubility Download PDF

Info

Publication number
CA2722408C
CA2722408C CA2722408A CA2722408A CA2722408C CA 2722408 C CA2722408 C CA 2722408C CA 2722408 A CA2722408 A CA 2722408A CA 2722408 A CA2722408 A CA 2722408A CA 2722408 C CA2722408 C CA 2722408C
Authority
CA
Canada
Prior art keywords
composition according
testosterone
oil
fatty acid
composition
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.)
Active
Application number
CA2722408A
Other languages
English (en)
French (fr)
Other versions
CA2722408A1 (en
Inventor
Hiep Huatan
Richard Ross
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.)
Neurocrine UK Ltd
Original Assignee
Diurnal Ltd
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 Diurnal Ltd filed Critical Diurnal Ltd
Publication of CA2722408A1 publication Critical patent/CA2722408A1/en
Application granted granted Critical
Publication of CA2722408C publication Critical patent/CA2722408C/en
Active 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
    • 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
    • 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
    • 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
    • A61K9/48—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
    • 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
    • A61P5/26—Androgens
    • 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
    • A61P5/30—Oestrogens
    • 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
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2722408A 2008-04-28 2009-04-27 Lipid composition for enhancing steroid solubility Active CA2722408C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0807605.1A GB0807605D0 (en) 2008-04-28 2008-04-28 Lipid composition
GB0807605.1 2008-04-28
PCT/GB2009/001068 WO2009133352A2 (en) 2008-04-28 2009-04-27 Lipid composition

Publications (2)

Publication Number Publication Date
CA2722408A1 CA2722408A1 (en) 2009-11-05
CA2722408C true CA2722408C (en) 2018-01-30

Family

ID=39522593

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2722408A Active CA2722408C (en) 2008-04-28 2009-04-27 Lipid composition for enhancing steroid solubility

Country Status (15)

Country Link
US (2) US9012436B2 (enExample)
EP (2) EP2722038A3 (enExample)
JP (1) JP5727925B2 (enExample)
KR (1) KR101617811B1 (enExample)
CN (1) CN102083421B (enExample)
AU (1) AU2009241910B2 (enExample)
CA (1) CA2722408C (enExample)
DK (1) DK2273984T3 (enExample)
ES (1) ES2502242T3 (enExample)
GB (1) GB0807605D0 (enExample)
IL (2) IL208612A (enExample)
PL (1) PL2273984T3 (enExample)
PT (1) PT2273984E (enExample)
WO (1) WO2009133352A2 (enExample)
ZA (1) ZA201007612B (enExample)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6248363B1 (en) * 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US20030236236A1 (en) * 1999-06-30 2003-12-25 Feng-Jing Chen Pharmaceutical compositions and dosage forms for administration of hydrophobic drugs
US20040115287A1 (en) * 2002-12-17 2004-06-17 Lipocine, Inc. Hydrophobic active agent compositions and methods
US20060003002A1 (en) * 2003-11-03 2006-01-05 Lipocine, Inc. Pharmaceutical compositions with synchronized solubilizer release
ES2930658T3 (es) 2005-04-15 2022-12-20 Tolmar Inc Sistemas de administración farmacéutica para medicamentos hidrofóbicos y composiciones que comprenden los mismos
US8492369B2 (en) 2010-04-12 2013-07-23 Clarus Therapeutics Inc Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same
WO2009114365A2 (en) * 2008-03-13 2009-09-17 Mallinckrodt Inc. Multi-function, foot-activated controller for imaging system
US11304960B2 (en) * 2009-01-08 2022-04-19 Chandrashekar Giliyar Steroidal compositions
US9034858B2 (en) 2010-11-30 2015-05-19 Lipocine Inc. High-strength testosterone undecanoate compositions
US20180153904A1 (en) 2010-11-30 2018-06-07 Lipocine Inc. High-strength testosterone undecanoate compositions
US9358241B2 (en) 2010-11-30 2016-06-07 Lipocine Inc. High-strength testosterone undecanoate compositions
US20120148675A1 (en) 2010-12-10 2012-06-14 Basawaraj Chickmath Testosterone undecanoate compositions
US20130040923A1 (en) 2011-05-13 2013-02-14 Trimel Pharmaceuticals Corporation Intranasal lower dosage strength testosterone gel formulations and use thereof for treating anorgasmia or hypoactive sexual desire disorder
US20130045958A1 (en) 2011-05-13 2013-02-21 Trimel Pharmaceuticals Corporation Intranasal 0.15% and 0.24% testosterone gel formulations and use thereof for treating anorgasmia or hypoactive sexual desire disorder
US9757388B2 (en) 2011-05-13 2017-09-12 Acerus Pharmaceuticals Srl Intranasal methods of treating women for anorgasmia with 0.6% and 0.72% testosterone gels
MX363561B (es) * 2011-05-15 2019-03-27 Trimel Biopharma Srl Geles nasales de liberacion controlada de testosterona, metodos y sistemas aplicadores multidosis pre cargados para administracion pernasal.
CA2856520C (en) 2011-11-23 2021-04-06 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US9486433B2 (en) 2012-10-12 2016-11-08 Mochida Pharmaceuticals Co. Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
US20140179655A1 (en) 2012-12-20 2014-06-26 Solural Pharma ApS Solid oral dosage form of testosterone derivative
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11744838B2 (en) 2013-03-15 2023-09-05 Acerus Biopharma Inc. Methods of treating hypogonadism with transnasal testosterone bio-adhesive gel formulations in male with allergic rhinitis, and methods for preventing an allergic rhinitis event
US9889108B2 (en) 2013-03-15 2018-02-13 Mochida Pharmaceutical Co., Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
US10441560B2 (en) 2013-03-15 2019-10-15 Mochida Pharmaceutical Co., Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
KR101440726B1 (ko) * 2013-04-16 2014-09-18 중앙대학교 산학협력단 가용화제를 포함하는 림프계 약물전달 시스템용 조성물
EP3054940B1 (en) * 2013-10-07 2020-09-23 Mochida Pharmaceutical Co., Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
AR100562A1 (es) 2014-05-22 2016-10-12 Therapeuticsmd Inc Composición farmacéutica de estradiol y progesterona para terapia de reemplazo hormonal
US11197828B2 (en) 2014-06-19 2021-12-14 Solural Pharma ApS Solid oral dosage form of lipophilic compounds
AU2015296609A1 (en) 2014-07-29 2016-12-22 Therapeuticsmd, Inc. Transdermal cream
EP3185872B1 (en) * 2014-08-28 2021-03-31 Board of Regents, The University of Texas System Formulations of testosterone and methods of treatment therewith
WO2016033556A1 (en) 2014-08-28 2016-03-03 Lipocine Inc. BIOAVAILABLE SOLID STATE (17-β)-HYDROXY-4-ANDROSTEN-3-ONE ESTERS
US20170246187A1 (en) 2014-08-28 2017-08-31 Lipocine Inc. (17-ß)-3-OXOANDROST-4-EN-17-YL TRIDECANOATE COMPOSITIONS AND METHODS OF THEIR PREPARATION AND USE
US20160361322A1 (en) 2015-06-15 2016-12-15 Lipocine Inc. Composition and method for oral delivery of androgen prodrugs
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
KR101679380B1 (ko) * 2015-09-10 2016-11-25 주식회사 유유제약 두타스테리드를 포함하는 약학적 조성물 및 이를 포함하는 캡슐 제형
CN106562949A (zh) * 2015-10-10 2017-04-19 浙江旭晨医药科技有限公司 甘油三酯类化合物在制备治疗多囊卵巢综合征药物中的应用
KR102351762B1 (ko) * 2016-03-02 2022-01-18 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 테스토스테론 제형 및 이를 이용한 치료 방법
AU2017239645A1 (en) 2016-04-01 2018-10-18 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
US11559530B2 (en) 2016-11-28 2023-01-24 Lipocine Inc. Oral testosterone undecanoate therapy
WO2019046582A1 (en) * 2017-08-30 2019-03-07 Antares Pharma, Inc. TESTOSTERONE ESTER TRIGLYCERIDE FORMULATIONS
US11311554B2 (en) * 2018-04-04 2022-04-26 Slayback Pharma Llc Pharmaceutical compositions of testosterone
CA3107214A1 (en) 2018-07-20 2020-01-23 Lipocine Inc. Liver disease
CN114617968B (zh) * 2019-04-09 2023-10-03 北京五和博澳药业股份有限公司 黄酮多酚类药物自乳化组合物、其制备方法、药物组合物及用途
AU2021216630A1 (en) 2020-02-05 2022-09-22 Neurocrine UK Limited Testosterone containing pharmaceutical composition
WO2024014958A2 (en) * 2022-07-15 2024-01-18 Seranovo Holding B.V. Lides formulation platform
WO2024014959A2 (en) * 2022-07-15 2024-01-18 Seranovo Holding B.V. Micelle-generating formulations with improved hydrophobicity

Family Cites Families (12)

* 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
GB1567515A (en) 1976-05-28 1980-05-14 Akzo Nv Esters of testo-sterone and 5 -dihydro-testosterone
NL7711916A (nl) 1977-10-29 1979-05-02 Akzo Nv Werkwijze ter bereiding van sterk geconcen- treerde farmaceutische preparaten van steroiden.
GB9608719D0 (en) * 1996-04-26 1996-07-03 Scherer Ltd R P Pharmaceutical compositions
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
US6541025B1 (en) 1999-12-30 2003-04-01 Shear/Kershman Laboratories, Inc. Method for preparing solid delivery system for encapsulated and non-encapsulated pharmaceuticals
GB0000313D0 (en) * 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
EP1260225A1 (en) * 2001-05-18 2002-11-27 Pantarhei Bioscience B.V. A pharmaceutical composition for use in hormone replacement therapy
JO2505B1 (en) * 2003-03-14 2009-10-05 باير شيرنغ فارما اكتنجيسيلشافت Pharmacy methods and formulations for obtaining acceptable serum testosterone levels
US7138389B2 (en) * 2004-02-09 2006-11-21 University Of Washington Oral androgen therapy using modulators of testosterone bioavailability
ES2930658T3 (es) 2005-04-15 2022-12-20 Tolmar Inc Sistemas de administración farmacéutica para medicamentos hidrofóbicos y composiciones que comprenden los mismos

Also Published As

Publication number Publication date
EP2722038A3 (en) 2014-06-18
EP2273984B1 (en) 2014-07-30
PT2273984E (pt) 2014-11-03
ZA201007612B (en) 2011-07-27
EP2722038A2 (en) 2014-04-23
PL2273984T3 (pl) 2015-04-30
WO2009133352A3 (en) 2010-10-28
ES2502242T3 (es) 2014-10-03
WO2009133352A2 (en) 2009-11-05
CN102083421B (zh) 2012-12-12
KR20110007169A (ko) 2011-01-21
US9012436B2 (en) 2015-04-21
US20150133417A1 (en) 2015-05-14
EP2273984A2 (en) 2011-01-19
US20110039814A1 (en) 2011-02-17
IL236400A0 (en) 2015-01-29
IL236400A (en) 2016-06-30
GB0807605D0 (en) 2008-06-04
KR101617811B1 (ko) 2016-05-03
IL208612A (en) 2015-03-31
DK2273984T3 (da) 2014-08-25
JP2011519846A (ja) 2011-07-14
CN102083421A (zh) 2011-06-01
IL208612A0 (en) 2010-12-30
CA2722408A1 (en) 2009-11-05
JP5727925B2 (ja) 2015-06-03
AU2009241910A1 (en) 2009-11-05
AU2009241910B2 (en) 2013-10-24

Similar Documents

Publication Publication Date Title
CA2722408C (en) Lipid composition for enhancing steroid solubility
KR100511133B1 (ko) 성호르몬을함유하는경구용약제학적조성물
CA2795908C (en) Oral testosterone ester formulations and methods of treating testoterone deficiency comprising same
RU2429850C2 (ru) Фармацевтические системы доставки для гидрофобных лекарственных средств и композиций, их содержащих
US10286077B2 (en) Steroid hormone compositions in medium chain oils
ES2967709T3 (es) Formulaciones y terapias naturales de reemplazo hormonal combinadas
JPS6245845B2 (enExample)
US11433083B2 (en) High-strength testosterone undecanoate compositions
AU2014200332B2 (en) Lipid composition
HK1194006A (en) Lipid composition
US20250319101A1 (en) Oral pharmaceutical compositions of progesterone and estradiol
CN103705462A (zh) 口服睾酮酯制剂以及包含其的治疗睾酮缺乏症的方法
RU2642244C2 (ru) Оральные фармацевтические композиции сложных эфиров тестостерона и способы лечения недостатка тестостерона с их использованием
TW200306197A (en) Medicament for treating climacteric post-menopausal complaints
CN103830245A (zh) 口服睾酮酯制剂及其在制备治疗睾酮缺乏症药物中的应用

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20140428