RU2012133627A - Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, с улучшенными свойствами хранения и растворимости - Google Patents
Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, с улучшенными свойствами хранения и растворимости Download PDFInfo
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 30
- AURFZBICLPNKBZ-FZCSVUEKSA-N 3beta-hydroxy-5alpha-pregnan-20-one Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-FZCSVUEKSA-N 0.000 claims abstract 8
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims abstract 8
- 239000000203 mixture Substances 0.000 claims abstract 8
- 229930182558 Sterol Natural products 0.000 claims abstract 7
- 150000003432 sterols Chemical class 0.000 claims abstract 7
- 235000003702 sterols Nutrition 0.000 claims abstract 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract 5
- OILXMJHPFNGGTO-UHFFFAOYSA-N (22E)-(24xi)-24-methylcholesta-5,22-dien-3beta-ol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(C)C(C)C)C1(C)CC2 OILXMJHPFNGGTO-UHFFFAOYSA-N 0.000 claims abstract 4
- LGJMUZUPVCAVPU-UHFFFAOYSA-N beta-Sitostanol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(CC)C(C)C)C1(C)CC2 LGJMUZUPVCAVPU-UHFFFAOYSA-N 0.000 claims abstract 4
- 235000012000 cholesterol Nutrition 0.000 claims abstract 4
- 239000007787 solid Substances 0.000 claims abstract 4
- 235000015112 vegetable and seed oil Nutrition 0.000 claims abstract 4
- 239000008158 vegetable oil Substances 0.000 claims abstract 4
- 150000002148 esters Chemical class 0.000 claims abstract 3
- 238000000034 method Methods 0.000 claims abstract 3
- OSELKOCHBMDKEJ-UHFFFAOYSA-N (10R)-3c-Hydroxy-10r.13c-dimethyl-17c-((R)-1-methyl-4-isopropyl-hexen-(4c)-yl)-(8cH.9tH.14tH)-Delta5-tetradecahydro-1H-cyclopenta[a]phenanthren Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(=CC)C(C)C)C1(C)CC2 OSELKOCHBMDKEJ-UHFFFAOYSA-N 0.000 claims abstract 2
- MCWVPSBQQXUCTB-UHFFFAOYSA-N (24Z)-5alpha-Stigmasta-7,24(28)-dien-3beta-ol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)CCC(=CC)C(C)C)CCC33)C)C3=CCC21 MCWVPSBQQXUCTB-UHFFFAOYSA-N 0.000 claims abstract 2
- OQMZNAMGEHIHNN-UHFFFAOYSA-N 7-Dehydrostigmasterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CC(CC)C(C)C)CCC33)C)C3=CC=C21 OQMZNAMGEHIHNN-UHFFFAOYSA-N 0.000 claims abstract 2
- OILXMJHPFNGGTO-NRHJOKMGSA-N Brassicasterol Natural products O[C@@H]1CC=2[C@@](C)([C@@H]3[C@H]([C@H]4[C@](C)([C@H]([C@@H](/C=C/[C@H](C(C)C)C)C)CC4)CC3)CC=2)CC1 OILXMJHPFNGGTO-NRHJOKMGSA-N 0.000 claims abstract 2
- 235000019483 Peanut oil Nutrition 0.000 claims abstract 2
- OILXMJHPFNGGTO-ZRUUVFCLSA-N UNPD197407 Natural products C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)C=C[C@H](C)C(C)C)[C@@]1(C)CC2 OILXMJHPFNGGTO-ZRUUVFCLSA-N 0.000 claims abstract 2
- HZYXFRGVBOPPNZ-UHFFFAOYSA-N UNPD88870 Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)=CCC(CC)C(C)C)C1(C)CC2 HZYXFRGVBOPPNZ-UHFFFAOYSA-N 0.000 claims abstract 2
- MCWVPSBQQXUCTB-OQTIOYDCSA-N avenasterol Chemical compound C1[C@@H](O)CC[C@]2(C)[C@@H](CC[C@@]3([C@@H]([C@H](C)CC/C(=C/C)C(C)C)CC[C@H]33)C)C3=CC[C@H]21 MCWVPSBQQXUCTB-OQTIOYDCSA-N 0.000 claims abstract 2
- 229940076810 beta sitosterol Drugs 0.000 claims abstract 2
- NJKOMDUNNDKEAI-UHFFFAOYSA-N beta-sitosterol Natural products CCC(CCC(C)C1CCC2(C)C3CC=C4CC(O)CCC4C3CCC12C)C(C)C NJKOMDUNNDKEAI-UHFFFAOYSA-N 0.000 claims abstract 2
- OILXMJHPFNGGTO-ZAUYPBDWSA-N brassicasterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)/C=C/[C@H](C)C(C)C)[C@@]1(C)CC2 OILXMJHPFNGGTO-ZAUYPBDWSA-N 0.000 claims abstract 2
- 235000004420 brassicasterol Nutrition 0.000 claims abstract 2
- 239000004359 castor oil Substances 0.000 claims abstract 2
- 235000019438 castor oil Nutrition 0.000 claims abstract 2
- 229940107161 cholesterol Drugs 0.000 claims abstract 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims abstract 2
- 239000004006 olive oil Substances 0.000 claims abstract 2
- 235000008390 olive oil Nutrition 0.000 claims abstract 2
- 238000007911 parenteral administration Methods 0.000 claims abstract 2
- 239000000312 peanut oil Substances 0.000 claims abstract 2
- 239000008159 sesame oil Substances 0.000 claims abstract 2
- 235000011803 sesame oil Nutrition 0.000 claims abstract 2
- KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 claims abstract 2
- 229950005143 sitosterol Drugs 0.000 claims abstract 2
- NLQLSVXGSXCXFE-UHFFFAOYSA-N sitosterol Natural products CC=C(/CCC(C)C1CC2C3=CCC4C(C)C(O)CCC4(C)C3CCC2(C)C1)C(C)C NLQLSVXGSXCXFE-UHFFFAOYSA-N 0.000 claims abstract 2
- HCXVJBMSMIARIN-PHZDYDNGSA-N stigmasterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)/C=C/[C@@H](CC)C(C)C)[C@@]1(C)CC2 HCXVJBMSMIARIN-PHZDYDNGSA-N 0.000 claims abstract 2
- 235000016831 stigmasterol Nutrition 0.000 claims abstract 2
- 229940032091 stigmasterol Drugs 0.000 claims abstract 2
- BFDNMXAIBMJLBB-UHFFFAOYSA-N stigmasterol Natural products CCC(C=CC(C)C1CCCC2C3CC=C4CC(O)CCC4(C)C3CCC12C)C(C)C BFDNMXAIBMJLBB-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000000725 suspension Substances 0.000 claims abstract 2
- 230000027758 ovulation cycle Effects 0.000 claims 5
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 235000019441 ethanol Nutrition 0.000 claims 2
- 208000007848 Alcoholism Diseases 0.000 claims 1
- 206010002091 Anaesthesia Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010027940 Mood altered Diseases 0.000 claims 1
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- 201000007930 alcohol dependence Diseases 0.000 claims 1
- 230000037005 anaesthesia Effects 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000008020 evaporation Effects 0.000 claims 1
- 238000001704 evaporation Methods 0.000 claims 1
- 206010016256 fatigue Diseases 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 230000007510 mood change Effects 0.000 claims 1
- 229940127234 oral contraceptive Drugs 0.000 claims 1
- 239000003539 oral contraceptive agent Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
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- 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
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Abstract
1. Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, по меньшей мере, один стерин или его эфир и смесь ацилглицеролов с содержанием твердых жиров менее чем приблизительно 25% при 25°C и приблизительно 0% при 37°C.2. Фармацевтическая композиция по п.1, где стерин выбран из группы, состоящей из холестерина, бета-ситостерина, стигмастерина, брассикастерина и авенастерина.3. Фармацевтическая композиция по п.2, где стерин представляет собой холестерин.4. Фармацевтическая композиция по любому из пп.1-3, где в смеси ацилглицеролов содержится растительное масло.5. Фармацевтическая композиция по п.4, где растительное масло выбрано из группы, состоящей из кунжутного масла, арахисового масла, оливкового масла и касторового масла.6. Фармацевтическая композиция по любому из пп.1-3, где смесь ацилглицеролов представляет собой среднецепочечные ацилглицеролы.7. Фармацевтическая композиция по любому из пп.1-3, где 3-бета-гидрокси-5-альфа-прегнан-20-он по существу растворен.8. Фармацевтическая композиция по любому из пп.1-3, содержащая суспензию 3-бета-гидрокси-5-альфа-прегнан-20-она.9. Фармацевтическая композиция по любому из пп.1-3 для парентерального введения.10. Фармацевтическая композиция по любому из пп.1-3 для перорального введения.11. Фармацевтическая композиция по любому из пп.1-3 для вагинального введения.12. Фармацевтическая композиция по любому из пп.1-3 для назального введения.13. Способ получения фармацевтической композиции по п.7, включающий следующие стадии:а) растворение 3-бета-гидрокси-5-альфа-прегнан-20-она в этиловом спирте,b) добавление смеси ацилглицеролов с содержанием твердых жиров менее чем приблизительно 25% п�
Claims (17)
1. Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, по меньшей мере, один стерин или его эфир и смесь ацилглицеролов с содержанием твердых жиров менее чем приблизительно 25% при 25°C и приблизительно 0% при 37°C.
2. Фармацевтическая композиция по п.1, где стерин выбран из группы, состоящей из холестерина, бета-ситостерина, стигмастерина, брассикастерина и авенастерина.
3. Фармацевтическая композиция по п.2, где стерин представляет собой холестерин.
4. Фармацевтическая композиция по любому из пп.1-3, где в смеси ацилглицеролов содержится растительное масло.
5. Фармацевтическая композиция по п.4, где растительное масло выбрано из группы, состоящей из кунжутного масла, арахисового масла, оливкового масла и касторового масла.
6. Фармацевтическая композиция по любому из пп.1-3, где смесь ацилглицеролов представляет собой среднецепочечные ацилглицеролы.
7. Фармацевтическая композиция по любому из пп.1-3, где 3-бета-гидрокси-5-альфа-прегнан-20-он по существу растворен.
8. Фармацевтическая композиция по любому из пп.1-3, содержащая суспензию 3-бета-гидрокси-5-альфа-прегнан-20-она.
9. Фармацевтическая композиция по любому из пп.1-3 для парентерального введения.
10. Фармацевтическая композиция по любому из пп.1-3 для перорального введения.
11. Фармацевтическая композиция по любому из пп.1-3 для вагинального введения.
12. Фармацевтическая композиция по любому из пп.1-3 для назального введения.
13. Способ получения фармацевтической композиции по п.7, включающий следующие стадии:
а) растворение 3-бета-гидрокси-5-альфа-прегнан-20-она в этиловом спирте,
b) добавление смеси ацилглицеролов с содержанием твердых жиров менее чем приблизительно 25% при 25°C и приблизительно 0% при 37°C и стерина или его эфира,
c) перемешивание до получения однородной жидкости, и
d) выпаривание спирта.
14. Фармацевтическая композиция, полученная способом по п.13.
15. Применение фармацевтической композиции по любому из пп.1-12 или п.14 для лечения или профилактики нарушений центральной нервной системы.
16. Применение по п.15, где нарушение центральной нервной системы выбрано из группы, состоящей из эпилепсии, эпилепсии, зависимой от менструального цикла, депрессии, депрессии, связанной со стрессом, мигрени, повышенной утомляемости, и, в частности, повышенной утомляемости, вызванной стрессом, предменструального синдрома, предменструального дисфорического расстройства, связанных с менструальным циклом изменений настроения, вызванных стрессом нарушений памяти, связанных с менструальным циклом трудностей в концентрации внимания деменции Альцгеймера, связанных с менструальным циклом нарушения сна и утомляемости, наркотической зависимости, алкоголизма, связанного с менструальным циклом, побочных эффектов оральных контрацептивов и постменопаузальной терапии или их комбинаций.
17. Применение фармацевтической композиции по любому из пп.1-12 или п.14 для прекращения стероидиндуцированной анестезии.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
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| US61/295,027 | 2010-01-14 | ||
| PCT/SE2011/050036 WO2011087441A1 (en) | 2010-01-14 | 2011-01-14 | A pharmaceutical composition comprising 3-beta-hydroxy-5-alpha-pregnan-20-one with improved storage and solubility properties |
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| US20200281990A1 (en) * | 2016-09-27 | 2020-09-10 | Guangxi Jiufu Biotechnology Co., Ltd | Extract effective in treating drug addiction |
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| US10478505B2 (en) * | 2011-09-23 | 2019-11-19 | The Regents Of The University Of California | Edible oils to enhance delivery of orally administered steroids |
| CN106146596A (zh) * | 2016-07-05 | 2016-11-23 | 浙江海洋大学 | 一种铜藻β‑谷甾醇化合物及其提取方法、应用 |
| CN106146597A (zh) * | 2016-07-05 | 2016-11-23 | 浙江海洋大学 | 一种马尾藻甾醇化合物及其提取方法、应用 |
| SI3565528T1 (sl) * | 2017-01-09 | 2025-10-30 | Relmada Therapeutics, Inc. | Injekcijske suspenzije |
| FI3579843T3 (fi) | 2017-02-10 | 2026-01-19 | Relmada Therapeutics Inc | 3-beetahydroksi-5-alfapregnan-20-oni touretten oireyhtymän, pakko-oireisen häiriön ja uhkapeliriippuvuuden hoitoa varten |
| 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 |
| WO2020011789A1 (en) | 2018-07-09 | 2020-01-16 | Asarina Pharma Ab | Injectable suspensions |
| EP3593789A1 (fr) * | 2018-07-11 | 2020-01-15 | Beta Innov | Composition contenant un dérivé de 7beta-hydroxycholestérol et un véhicule lipidique, et son utilisation dans le traitement de pathologies néoplasiques |
| CA3136389A1 (en) * | 2019-04-05 | 2020-10-08 | The Regents Of The University Of California | Allopregnanolone compositions and uses thereof |
| CN112341511A (zh) * | 2019-08-09 | 2021-02-09 | 南京诺瑞特医药科技有限公司 | 3-羟基-5-孕烷-20-酮衍生物及其用途 |
| CN114907436A (zh) * | 2021-02-08 | 2022-08-16 | 南京诺瑞特医药科技有限公司 | 3-羟基-5-孕烷-20-酮衍生物的晶型及其制备方法和用途 |
| EP4321152A4 (en) * | 2021-04-08 | 2025-05-21 | Tionlab Therapeutics | Sustained-release lipid preconcentrate |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20200281990A1 (en) * | 2016-09-27 | 2020-09-10 | Guangxi Jiufu Biotechnology Co., Ltd | Extract effective in treating drug addiction |
| US11925665B2 (en) * | 2016-09-27 | 2024-03-12 | Guangxi Jiufu Biotechnology Co., Ltd | Extract effective in treating drug addiction |
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| BR112012017136B1 (pt) | 2021-05-25 |
| ES2566765T3 (es) | 2016-04-15 |
| US9687496B2 (en) | 2017-06-27 |
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| AU2011205821A1 (en) | 2012-07-12 |
| US20170258809A1 (en) | 2017-09-14 |
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| WO2011087441A1 (en) | 2011-07-21 |
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| US20120322781A1 (en) | 2012-12-20 |
| ZA201204574B (en) | 2013-08-28 |
| JP2013517269A (ja) | 2013-05-16 |
| CN102753181A (zh) | 2012-10-24 |
| EP2523666B1 (en) | 2016-01-13 |
| EP2523666A4 (en) | 2013-07-03 |
| EP2523666A1 (en) | 2012-11-21 |
| AU2011205821B2 (en) | 2013-07-25 |
| HUE027298T2 (en) | 2016-10-28 |
| US11534446B2 (en) | 2022-12-27 |
| DK2523666T3 (en) | 2016-04-04 |
| PL2523666T3 (pl) | 2016-06-30 |
| CA2786330C (en) | 2013-11-19 |
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