RU2722592C2 - Длинноцепочечные липосбалансированные сложные эфиры тестостерона для пероральной доставки - Google Patents

Длинноцепочечные липосбалансированные сложные эфиры тестостерона для пероральной доставки Download PDF

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Publication number
RU2722592C2
RU2722592C2 RU2015128028A RU2015128028A RU2722592C2 RU 2722592 C2 RU2722592 C2 RU 2722592C2 RU 2015128028 A RU2015128028 A RU 2015128028A RU 2015128028 A RU2015128028 A RU 2015128028A RU 2722592 C2 RU2722592 C2 RU 2722592C2
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Russia
Prior art keywords
testosterone
composition
ester
compositions
serum
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RU2015128028A
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English (en)
Russian (ru)
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RU2015128028A3 (enExample
RU2015128028A (ru
Inventor
Сатиш Кумар НАЧАЕГАРИ
Чандрашекар ГИЛИЯР
Радж ПАТЕЛ
Чидамбарам НАЧИАППАН
Сринивансан ВЕНКАТЕШВАРАН
Махеш В. ПАТЕЛ
Original Assignee
Липосин Инк.
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Priority claimed from US13/843,403 external-priority patent/US20130225544A1/en
Application filed by Липосин Инк. filed Critical Липосин Инк.
Publication of RU2015128028A publication Critical patent/RU2015128028A/ru
Publication of RU2015128028A3 publication Critical patent/RU2015128028A3/ru
Application granted granted Critical
Publication of RU2722592C2 publication Critical patent/RU2722592C2/ru

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    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • 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
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • 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

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  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Reproductive Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pregnancy & Childbirth (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
RU2015128028A 2013-03-15 2014-03-17 Длинноцепочечные липосбалансированные сложные эфиры тестостерона для пероральной доставки RU2722592C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13/843,403 2013-03-15
US13/843,403 US20130225544A1 (en) 2009-01-08 2013-03-15 Lipobalanced long chain testosterone esters for oral delivery
PCT/US2014/030604 WO2014145781A1 (en) 2013-03-15 2014-03-17 Lipobalanced long chain testosterone esters for oral delivery

Publications (3)

Publication Number Publication Date
RU2015128028A RU2015128028A (ru) 2017-04-21
RU2015128028A3 RU2015128028A3 (enExample) 2018-02-13
RU2722592C2 true RU2722592C2 (ru) 2020-06-02

Family

ID=51538095

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2015128028A RU2722592C2 (ru) 2013-03-15 2014-03-17 Длинноцепочечные липосбалансированные сложные эфиры тестостерона для пероральной доставки

Country Status (16)

Country Link
US (2) US20160193228A1 (enExample)
EP (2) EP2968363B1 (enExample)
JP (1) JP6307711B2 (enExample)
KR (1) KR102238478B1 (enExample)
CN (1) CN105073118A (enExample)
AR (1) AR095538A1 (enExample)
AU (2) AU2014232475A1 (enExample)
BR (1) BR112015020849A2 (enExample)
CA (1) CA2942005C (enExample)
IL (1) IL240958B (enExample)
MX (1) MX2015010594A (enExample)
RU (1) RU2722592C2 (enExample)
TW (1) TW201521731A (enExample)
UY (1) UY35445A (enExample)
WO (1) WO2014145781A1 (enExample)
ZA (1) ZA201507700B (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018102618A1 (en) 2016-11-30 2018-06-07 Lipocine Inc. Oral testosterone tridecanoate therapy
EP3824296B1 (en) * 2018-07-20 2026-04-01 Lipocine Inc. Oral pharmaceutical composition comprising testosterone tridecanoate and/or testosterone dodecanoate for treating liver diseases
JP6945874B2 (ja) * 2019-12-24 2021-10-06 一般財団法人バイオダイナミックス研究所 経口投与用医薬組成物
CN115869321A (zh) * 2021-09-28 2023-03-31 杭州中美华东制药有限公司 一种芦可替尼组合物及其制备方法
AU2022467882B2 (en) * 2022-06-22 2026-02-12 Lipocine, Inc. (17-)-3-oxoandrost-4-en-17-yl dodecanoate compositions and methods of preparation and use

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006113505A2 (en) * 2005-04-15 2006-10-26 Clarus Therapeutics, Inc. Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same
RU2354381C2 (ru) * 2003-03-14 2009-05-10 Шеринг Акциенгезельшафт Способы и фармацевтические композиции для достоверного достижения приемлемых уровней тестостерона в сыворотке
US20110251167A1 (en) * 2010-04-12 2011-10-13 Clarus Therapeutics, Inc. Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same

Family Cites Families (8)

* 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
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.
GB1567515A (en) * 1976-05-28 1980-05-14 Akzo Nv Esters of testo-sterone and 5 -dihydro-testosterone
MXPA03001147A (es) * 2000-08-23 2003-10-06 Akzo Nobel Nv Nueva formulacion de ester de testosterona para uso humano.
US20030022875A1 (en) * 2001-07-27 2003-01-30 Wilson Leland F. As-needed administration of orally active androgenic agents to enhance female sexual desire and responsiveness
US7138389B2 (en) 2004-02-09 2006-11-21 University Of Washington Oral androgen therapy using modulators of testosterone bioavailability
CN101217963A (zh) * 2005-04-15 2008-07-09 克劳拉斯医疗有限公司 疏水性药物给药系统及含有疏水性药物的组合物
US9034858B2 (en) * 2010-11-30 2015-05-19 Lipocine Inc. High-strength testosterone undecanoate compositions

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2354381C2 (ru) * 2003-03-14 2009-05-10 Шеринг Акциенгезельшафт Способы и фармацевтические композиции для достоверного достижения приемлемых уровней тестостерона в сыворотке
WO2006113505A2 (en) * 2005-04-15 2006-10-26 Clarus Therapeutics, Inc. Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same
US20110251167A1 (en) * 2010-04-12 2011-10-13 Clarus Therapeutics, Inc. Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same

Also Published As

Publication number Publication date
TW201521731A (zh) 2015-06-16
US20160193228A1 (en) 2016-07-07
AU2014232475A1 (en) 2015-08-06
MX2015010594A (es) 2015-12-16
JP6307711B2 (ja) 2018-04-11
EP2968363A4 (en) 2016-08-17
EP2968363B1 (en) 2020-08-19
US20160193227A1 (en) 2016-07-07
AU2019200097A1 (en) 2019-01-31
RU2015128028A (ru) 2017-04-21
JP2016514706A (ja) 2016-05-23
BR112015020849A2 (pt) 2017-07-18
UY35445A (es) 2014-10-31
CA2942005A1 (en) 2014-09-18
AR095538A1 (es) 2015-10-21
KR102238478B1 (ko) 2021-04-09
EP3797762A1 (en) 2021-03-31
ZA201507700B (en) 2017-02-22
IL240958B (en) 2019-07-31
WO2014145781A1 (en) 2014-09-18
AU2019200097B2 (en) 2021-02-04
IL240958A0 (en) 2015-11-30
KR20150129671A (ko) 2015-11-20
CA2942005C (en) 2022-02-01
EP2968363A1 (en) 2016-01-20
CN105073118A (zh) 2015-11-18

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