RU2016141135A - Трансдермальный крем - Google Patents
Трансдермальный крем Download PDFInfo
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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
- A61K31/57—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
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- 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
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- 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
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- 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
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Claims (127)
1. Трансдермальная фармацевтическая композиция, содержащая
прогестерон,
среднецепочечное масло и
d-лимонен,
где фармацевтическая композиция находится в виде крема для местного введения.
2. Трансдермальная фармацевтическая композиция по п.1, содержащая прогестерон в количестве, варьирующем примерно от 1,5% (мас./мас.) до 3,5% (мас./мас.).
3. Трансдермальная фармацевтическая композиция по п.2, содержащая прогестерон в количестве, варьирующем примерно от 2% (мас./мас.) до 3% (мас./мас.).
4. Трансдермальная фармацевтическая композиция по п.1, где среднецепочечное масло содержит среднецепочечные триглицериды, а среднецепочечные триглицериды, в свою очередь, в основном содержат триглицерид каприловой кислоты и триглицерид каприновой кислоты.
5. Трансдермальная фармацевтическая композиция по п.1, содержащая d-лимонен в количестве, варьирующем примерно от 1% (мас./мас.) до 12% (мас./мас.).
6. Трансдермальная фармацевтическая композиция по п.5, содержащая d-лимонен в количестве, варьирующем примерно от 1,5% (мас./мас.) до 10% (мас./мас.).
7. Трансдермальная фармацевтическая композиция по п.1, содержащая
прогестерон в количестве, варьирующем примерно от 1,5% (мас./мас.) до 3,5% (мас./мас.);
среднецепочечное масло в количестве, варьирующем примерно от 10% (мас./мас.) до 30% (мас./мас.); и
d-лимонен в количестве, варьирующем примерно от 1% (мас./мас.) до 12% (мас./мас.).
8. Трансдермальная фармацевтическая композиция по п.7, содержащая
прогестерон в количестве, варьирующем примерно от 2% (мас./мас.) до 3% (мас./мас.);
среднецепочечное масло в количестве, варьирующем примерно от 15% (мас./мас.) до 25% (мас./мас.); и
d-лимонен в количестве, варьирующем примерно от 1,5% (мас./мас.) до 10% (мас./мас.).
9. Трансдермальная фармацевтическая композиция по п.7, содержащая
прогестерон в количестве, составляющем примерно 2,5% (мас./мас.);
среднецепочечное масло в количестве, составляющем примерно 15% (мас./мас.); и
d-лимонен в количестве, составляющем примерно 5% (мас./мас.).
10. Трансдермальная фармацевтическая композиция по п.1, дополнительно содержащая эстрадиол.
11. Трансдермальная фармацевтическая композиция по п.10, содержащая эстрадиол в количестве, варьирующем примерно от 0,001% (мас./мас.) до 0,5% (мас./мас.).
12. Трансдермальная фармацевтическая композиция по п.10, содержащая эстрадиол в количестве, составляющем примерно 0,005% (мас./мас.).
13. Трансдермальная фармацевтическая композиция по п.10, содержащая эстрадиол в количестве, составляющем примерно 0,05% (мас./мас.).
14. Трансдермальная фармацевтическая композиция по п.1, содержащая
прогестерон в количестве, составляющем примерно 2,5% (мас./мас.);
среднецепочечное масло в количестве, составляющем примерно 15% (мас./мас.), где среднецепочечное масло содержит среднецепочечные триглицериды, которые, в свою очередь, содержат в основном триглицерид каприловой кислоты и триглицерид каприновой кислоты;
d-лимонен в количестве, составляющем примерно 5% (мас./мас.);
моноэтиловый эфир диэтиленгликоля в количестве, составляющем примерно 3% (мас./мас.);
монолаурат пропиленгликоля в количестве, составляющем примерно 5% (мас./мас.);
смесь стеаратов в количестве, составляющем примерно 7% (мас./мас.), где смесь стеаратов содержит моностеарат глицерина и стеарат ПЭГ-75;
смесь цетиловых спиртов в количестве, составляющем примерно 3,5% (мас./мас.), где смесь цетиловых спиртов содержит цетиловый спирт, цетет-20 и стеарет-20;
карбомер в количестве, составляющем примерно 0,2% (мас./мас.);
лецитин в количестве, составляющем примерно 3% (мас./мас.);
пропиленгликоль в количестве, составляющем примерно 4% (мас./мас.);
метилпарабен в количестве, составляющем примерно 0,2% (мас./мас.);
пропилпарабен в количестве, составляющем примерно 0,02% (мас./мас.);
лимонную кислоту в количестве, составляющем примерно 0,5% (мас./мас.);
фосфат натрия в количестве, составляющем примерно 0,8% (мас./мас.); и
очищенную воду.
15. Трансдермальная фармацевтическая композиция по п.14, дополнительно содержащая эстрадиол в количестве, составляющем примерно 0,005% (мас./мас.).
16. Трансдермальная фармацевтическая композиция по п.1, содержащая
прогестерон в количестве, составляющем примерно 2,5% (мас./мас.);
среднецепочечное масло в количестве, составляющем примерно 15% (мас./мас.), где среднецепочечное масло содержит среднецепочечные триглицериды, которые, в свою очередь, содержат в основном триглицерид каприловой кислоты и триглицерид каприновой кислоты;
d-лимонен в количестве, составляющем примерно 5% (мас./мас.);
моноэтиловый эфир диэтиленгликоля в количестве, составляющем примерно 3% (мас./мас.);
монолаурат пропиленгликоля в количестве, составляющем примерно 5% (мас./мас.);
бутилированный гидрокситолуол в количестве, составляющем примерно 0,1% (мас./мас.);
смесь стеаратов в количестве, составляющем примерно 7% (мас./мас.), где смесь стеаратов содержит моностеарат глицерина и стеарат ПЭГ-75;
смесь цетиловых спиртов в количестве, составляющем примерно 3,5% (мас./мас.), где смесь цетиловых спиртов содержит цетиловый спирт, цетет-20 и стеарет-20;
карбомер в количестве, составляющем примерно 0,2% (мас./мас.);
лецитин в количестве, составляющем примерно 3% (мас./мас.);
пропиленгликоль в количестве, составляющем примерно 4% (мас./мас.);
метилпарабен в количестве, составляющем примерно 0,2% (мас./мас.);
пропилпарабен в количестве, составляющем примерно 0,02% (мас./мас.);
лимонную кислоту в количестве, составляющем примерно 0,5% (мас./мас.);
фосфат натрия в количестве, составляющем примерно 0,8% (мас./мас.); и
очищенную воду.
17. Трансдермальная фармацевтическая композиция по п.16, дополнительно содержащая эстрадиол в количестве, составляющем примерно 0,005% (мас./мас.).
18. Трансдермальная фармацевтическая композиция, содержащая
прогестерон,
солюбилизирующее средство, включающее в себя среднецепочечное масло и вещество, способствующее проникновению,
где фармацевтическая композиция находится в виде крема для местного введения.
19. Трансдермальная фармацевтическая композиция по п.18, где вещество, способствующее проникновению, включает в себя монолаурат пропиленгликоля, моноэтиловый эфир диэтиленгликоля и пропиленгликоль.
20. Трансдермальная фармацевтическая композиция по п.18, где вещество, способствующее проникновению, дополнительно содержит d-лимонен.
21. Трансдермальная фармацевтическая композиция по п.18, где композиция содержит:
прогестерон,
среднецепочечное масло,
монолаурат пропиленгликоля,
моноэтиловый эфир диэтиленгликоля и
пропиленгликоль,
где фармацевтическая композиция находится в виде крема для местного введения.
22. Трансдермальная фармацевтическая композиция по п.21, содержащая прогестерон в количестве, варьирующем примерно от 1,5% (мас./мас.) до 3,5% (мас./мас.).
23. Трансдермальная фармацевтическая композиция по п.22, содержащая прогестерон в количестве, варьирующем примерно от 2% (мас./мас.) до 3% (мас./мас.).
24. Трансдермальная фармацевтическая композиция по п.18, где среднецепочечное масло содержит среднецепочечные триглицериды, а среднецепочечные триглицериды, в свою очередь, содержат в основном триглицерид каприловой кислоты и триглицерид каприновой кислоты.
25. Трансдермальная фармацевтическая композиция по п.21, содержащая
прогестерон в количестве, варьирующем примерно от 1,5% (мас./мас.) до примерно 3,5% (мас./мас.); и
среднецепочечное масло в количестве, варьирующем примерно от 10% (мас./мас.) до 30% (мас./мас.).
26. Трансдермальная фармацевтическая композиция по п.25, содержащая
прогестерон в количестве, варьирующем примерно от 2% (мас./мас.) до 3% (мас./мас.); и
среднецепочечное масло в количестве, варьирующем примерно от 15% (мас./мас.) до 25% (мас./мас.).
27. Трансдермальная фармацевтическая композиция по п.25, содержащая
прогестерон в количестве, составляющем примерно 2,5% (мас./мас.); и
среднецепочечное масло в количестве, составляющем примерно 15% (мас./мас.).
28. Трансдермальная фармацевтическая композиция по п.21, дополнительно содержащая эстрадиол.
29. Трансдермальная фармацевтическая композиция по п.28, содержащая эстрадиол в количестве, варьирующем примерно от 0,001% (мас./мас.) до 0,5% (мас./мас.).
30. Трансдермальная фармацевтическая композиция по п.29, содержащая эстрадиол в количестве, составляющем примерно 0,005% (мас./мас.).
31. Трансдермальная фармацевтическая композиция по п.29, содержащая эстрадиол в количестве, составляющем примерно 0,05% (мас./мас.).
32. Трансдермальная фармацевтическая композиция по п.21, содержащая
прогестерон в количестве, составляющем примерно 2,5% (мас./мас.);
среднецепочечное масло в количестве, составляющем примерно 15% (мас./мас.), где среднецепочечное масло содержит среднецепочечные триглицериды, которые, в свою очередь, в основном содержат триглицерид каприловой кислоты и триглицерид каприновой кислоты;
моноэтиловый эфир диэтиленгликоля в количестве, составляющем примерно 3% (мас./мас.);
монолаурат пропиленгликоля в количестве, составляющем примерно 5% (мас./мас.);
смесь стеаратов в количестве, составляющем примерно 7% (мас./мас.), где смесь стеаратов содержит моностеарат глицерина и стеарат ПЭГ-75;
смесь цетиловых спиртов в количестве, составляющем примерно 3,5% (мас./мас.), где смесь цетиловых спиртов содержит цетиловый спирт, цетет-20 и стеарет-20;
карбомер в количестве, составляющем примерно 0,2% (мас./мас.);
лецитин в количестве, составляющем примерно 3% (мас./мас.);
пропиленгликоль в количестве, составляющем примерно 4% (мас./мас.);
метилпарабен в количестве, составляющем примерно 0,2% (мас./мас.);
пропилпарабен в количестве, составляющем примерно 0,02% (мас./мас.);
лимонную кислоту в количестве, составляющем примерно 0,5% (мас./мас.);
фосфат натрия в количестве, составляющем примерно 0,8% (мас./мас.); и
очищенную воду.
33. Трансдермальная фармацевтическая композиция по п.32, дополнительно содержащая эстрадиол в количестве, составляющем примерно 0,005% (мас./мас.).
34. Трансдермальная фармацевтическая композиция по п.32, содержащая эстрадиол в количестве, составляющем примерно 0,05% (мас./мас.).
35. Трансдермальная фармацевтическая композиция по п.21, содержащая
прогестерон в количестве, составляющем примерно 2,5% (мас./мас.);
среднецепочечное масло в количестве, составляющем примерно 15% (мас./мас.), где среднецепочечное масло содержит среднецепочечные триглицериды, которые, в свою очередь, в основном содержат триглицерид каприловой кислоты и триглицерид каприновой кислоты;
моноэтиловый эфир диэтиленгликоля в количестве, составляющем примерно 3% (мас./мас.);
монолаурат пропиленгликоля в количестве, составляющем примерно 5% (мас./мас.);
бутилированный гидрокситолуол в количестве, составляющем примерно 0,1% (мас./мас.);
смесь стеаратов в количестве, составляющем примерно 7% (мас./мас.), где смесь стеаратов содержит моностеарат глицерина и стеарат ПЭГ-75;
смесь цетиловых спиртов в количестве, составляющем примерно 3,5% (мас./мас.), где смесь цетиловых спиртов содержит цетиловый спирт, цетет-20 и стеарет-20;
карбомер в количестве, составляющем примерно 0,2% (мас./мас.);
лецитин в количестве, составляющем примерно 3% (мас./мас.);
пропиленгликоль в количестве, составляющем примерно 4% (мас./мас.);
метилпарабен в количестве, составляющем примерно 0,2% (мас./мас.);
пропилпарабен в количестве, составляющем примерно 0,02% (мас./мас.);
лимонную кислоту в количестве, составляющем примерно 0,5% (мас./мас.);
фосфат натрия в количестве, составляющем примерно 0,8% (мас./мас.); и
очищенную воду.
36. Трансдермальная фармацевтическая композиция по п.35, дополнительно содержащая эстрадиол в количестве, составляющем примерно 0,005% (мас./мас.).
37. Трансдермальная фармацевтическая композиция по п.35, дополнительно содержащая эстрадиол в количестве, составляющем примерно 0,05% (мас./мас.).
38. Способ лечения состояния, связанного с дефицитом гормона у индивидуума, где способ включает введение индивидууму трансдермальной фармацевтической композиции по п.1.
39. Способ лечения состояния, связанного с дефицитом гормона у индивидуума, где способ включает введение индивидууму трансдермальной фармацевтической композиции по п.19.
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-
2015
- 2015-07-29 BR BR112016029338A patent/BR112016029338A2/pt not_active Application Discontinuation
- 2015-07-29 EP EP15827543.8A patent/EP3174542A4/en not_active Withdrawn
- 2015-07-29 US US14/812,179 patent/US10098894B2/en active Active
- 2015-07-29 MX MX2016013693A patent/MX2016013693A/es unknown
- 2015-07-29 WO PCT/US2015/042621 patent/WO2016018993A1/en active Application Filing
- 2015-07-29 AU AU2015296609A patent/AU2015296609A1/en not_active Abandoned
- 2015-07-29 RU RU2016141135A patent/RU2016141135A/ru not_active Application Discontinuation
- 2015-07-29 KR KR1020177002451A patent/KR20170040209A/ko unknown
- 2015-07-29 CA CA2951284A patent/CA2951284A1/en not_active Abandoned
- 2015-07-29 JP JP2016571728A patent/JP2017523138A/ja active Pending
-
2016
- 2016-11-15 IL IL248984A patent/IL248984A0/en unknown
-
2018
- 2018-09-07 US US16/125,201 patent/US20190070197A1/en not_active Abandoned
Also Published As
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US20160030449A1 (en) | 2016-02-04 |
CA2951284A1 (en) | 2016-02-04 |
RU2016141135A3 (ru) | 2019-05-07 |
MX2016013693A (es) | 2017-10-31 |
KR20170040209A (ko) | 2017-04-12 |
AU2015296609A1 (en) | 2016-12-22 |
IL248984A0 (en) | 2017-01-31 |
US20190070197A1 (en) | 2019-03-07 |
WO2016018993A1 (en) | 2016-02-04 |
US10098894B2 (en) | 2018-10-16 |
JP2017523138A (ja) | 2017-08-17 |
EP3174542A4 (en) | 2018-01-03 |
BR112016029338A2 (pt) | 2017-08-22 |
EP3174542A1 (en) | 2017-06-07 |
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