JP2008518895A5 - - Google Patents
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- Publication number
- JP2008518895A5 JP2008518895A5 JP2007538360A JP2007538360A JP2008518895A5 JP 2008518895 A5 JP2008518895 A5 JP 2008518895A5 JP 2007538360 A JP2007538360 A JP 2007538360A JP 2007538360 A JP2007538360 A JP 2007538360A JP 2008518895 A5 JP2008518895 A5 JP 2008518895A5
- Authority
- JP
- Japan
- Prior art keywords
- formulation
- estradiol
- pharmaceutically acceptable
- hydrate
- salt
- 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.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims 47
- 238000009472 formulation Methods 0.000 claims 43
- 150000002148 esters Chemical class 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 21
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims 16
- 229960005309 estradiol Drugs 0.000 claims 16
- 229930182833 estradiol Natural products 0.000 claims 16
- ZVVGLAMWAQMPDR-WVEWYJOQSA-N (8r,9s,13s,14s,17s)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol;hydrate Chemical compound O.OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1.OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 ZVVGLAMWAQMPDR-WVEWYJOQSA-N 0.000 claims 11
- 229960003851 estradiol hemihydrate Drugs 0.000 claims 11
- 239000007787 solid Substances 0.000 claims 11
- 238000002360 preparation method Methods 0.000 claims 10
- 229920002472 Starch Polymers 0.000 claims 5
- 239000001913 cellulose Substances 0.000 claims 5
- 229920002678 cellulose Polymers 0.000 claims 5
- 235000010980 cellulose Nutrition 0.000 claims 5
- 239000008184 oral solid dosage form Substances 0.000 claims 5
- 239000008107 starch Substances 0.000 claims 4
- 235000019698 starch Nutrition 0.000 claims 4
- 229920000881 Modified starch Polymers 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 239000003826 tablet Substances 0.000 claims 3
- 229920002261 Corn starch Polymers 0.000 claims 2
- 101000939135 Homo sapiens Ubiquitin carboxyl-terminal hydrolase 27 Proteins 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 2
- 102100029736 Ubiquitin carboxyl-terminal hydrolase 27 Human genes 0.000 claims 2
- 239000008120 corn starch Substances 0.000 claims 2
- 229960000913 crospovidone Drugs 0.000 claims 2
- 239000012738 dissolution medium Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940011871 estrogen Drugs 0.000 claims 2
- 239000000262 estrogen Substances 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 235000019426 modified starch Nutrition 0.000 claims 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 238000003860 storage Methods 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- LDSYPJSYQOUQMN-WAJSLEGFSA-N (8R,9S,13S,14S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol sulfuric acid Chemical compound OS(O)(=O)=O.OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)O)[C@@H]4[C@@H]3CCC2=C1 LDSYPJSYQOUQMN-WAJSLEGFSA-N 0.000 claims 1
- UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 claims 1
- 208000010392 Bone Fractures Diseases 0.000 claims 1
- GEMHYEDMDDCPKB-WAJSLEGFSA-N C(CCCCCCCCC=C)(=O)O.[C@@H]12CCC(O)[C@@]1(C)CC[C@@H]1C3=C(CC[C@@H]21)C=C(O)C=C3 Chemical compound C(CCCCCCCCC=C)(=O)O.[C@@H]12CCC(O)[C@@]1(C)CC[C@@H]1C3=C(CC[C@@H]21)C=C(O)C=C3 GEMHYEDMDDCPKB-WAJSLEGFSA-N 0.000 claims 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 1
- UOACKFBJUYNSLK-XRKIENNPSA-N Estradiol Cypionate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H](C4=CC=C(O)C=C4CC3)CC[C@@]21C)C(=O)CCC1CCCC1 UOACKFBJUYNSLK-XRKIENNPSA-N 0.000 claims 1
- JQIYNMYZKRGDFK-RUFWAXPRSA-N Estradiol dipropionate Chemical compound C1CC2=CC(OC(=O)CC)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CC)[C@@]1(C)CC2 JQIYNMYZKRGDFK-RUFWAXPRSA-N 0.000 claims 1
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 1
- 206010017076 Fracture Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000033830 Hot Flashes Diseases 0.000 claims 1
- 206010060800 Hot flush Diseases 0.000 claims 1
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims 1
- 229920002774 Maltodextrin Polymers 0.000 claims 1
- 239000005913 Maltodextrin Substances 0.000 claims 1
- 240000003183 Manihot esculenta Species 0.000 claims 1
- 235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- YXYXCSOJKUAPJI-ZBRFXRBCSA-N [(8r,9s,13s,14s,17s)-17-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl] sulfamate Chemical compound NS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 YXYXCSOJKUAPJI-ZBRFXRBCSA-N 0.000 claims 1
- 230000037182 bone density Effects 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 229960003575 estradiol acetate Drugs 0.000 claims 1
- FHXBMXJMKMWVRG-SLHNCBLASA-N estradiol acetate Chemical compound C1C[C@]2(C)[C@@H](O)CC[C@H]2[C@@H]2CCC3=CC(OC(=O)C)=CC=C3[C@H]21 FHXBMXJMKMWVRG-SLHNCBLASA-N 0.000 claims 1
- 229950002007 estradiol benzoate Drugs 0.000 claims 1
- 229960005416 estradiol cypionate Drugs 0.000 claims 1
- 229950010215 estradiol dipropionate Drugs 0.000 claims 1
- 229950004659 estradiol enanthate Drugs 0.000 claims 1
- RFWTZQAOOLFXAY-BZDYCCQFSA-N estradiol enanthate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCC)[C@@]1(C)CC2 RFWTZQAOOLFXAY-BZDYCCQFSA-N 0.000 claims 1
- 229960004766 estradiol valerate Drugs 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- 239000007897 gelcap Substances 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- CJWQYWQDLBZGPD-UHFFFAOYSA-N isoflavone Natural products C1=C(OC)C(OC)=CC(OC)=C1C1=COC2=C(C=CC(C)(C)O3)C3=C(OC)C=C2C1=O CJWQYWQDLBZGPD-UHFFFAOYSA-N 0.000 claims 1
- 150000002515 isoflavone derivatives Chemical class 0.000 claims 1
- 235000008696 isoflavones Nutrition 0.000 claims 1
- 229940035034 maltodextrin Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 230000008693 nausea Effects 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 229920001592 potato starch Polymers 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 229940100486 rice starch Drugs 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 229940100445 wheat starch Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04078014 | 2004-11-02 | ||
| PCT/EP2005/011726 WO2006048261A2 (en) | 2004-11-02 | 2005-11-01 | Oral solid dosage forms containing a low dose of estradiol |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008518895A JP2008518895A (ja) | 2008-06-05 |
| JP2008518895A5 true JP2008518895A5 (https=) | 2008-12-25 |
Family
ID=34928627
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007538360A Pending JP2008518895A (ja) | 2004-11-02 | 2005-11-01 | 低用量のエストラジオールを含む経口固形製剤 |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1814526A2 (https=) |
| JP (1) | JP2008518895A (https=) |
| KR (1) | KR20070085558A (https=) |
| CN (1) | CN101094656A (https=) |
| AR (1) | AR053650A1 (https=) |
| AU (1) | AU2005300658A1 (https=) |
| BR (1) | BRPI0517940A (https=) |
| CA (1) | CA2585095A1 (https=) |
| CR (1) | CR9112A (https=) |
| CU (1) | CU20070094A7 (https=) |
| EA (1) | EA013262B1 (https=) |
| GT (1) | GT200500315A (https=) |
| IL (1) | IL182635A0 (https=) |
| MX (1) | MX2007005281A (https=) |
| NO (1) | NO20072704L (https=) |
| PA (1) | PA8651401A1 (https=) |
| PE (1) | PE20061126A1 (https=) |
| TW (1) | TW200621312A (https=) |
| UY (1) | UY29185A1 (https=) |
| WO (1) | WO2006048261A2 (https=) |
| ZA (1) | ZA200705012B (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8022053B2 (en) | 2004-11-02 | 2011-09-20 | Bayer Schering Pharma Aktiengesellschaft | Oral solid dosage forms containing a low dose of estradiol |
| KR20080047959A (ko) * | 2006-11-27 | 2008-05-30 | 주식회사 엠디바이오알파 | 비만, 당뇨, 대사성 질환, 퇴행성 질환 및 미토콘드리아이상 질환의 치료 또는 예방을 위한 나프토퀴논계 약제조성물 |
| DE102009007771B4 (de) | 2009-02-05 | 2012-02-16 | Bayer Schering Pharma Aktiengesellschaft | Bukkales Applikationssystem, 17α-Estradiol enthaltend |
| US20130137664A1 (en) * | 2010-04-15 | 2013-05-30 | Bayer Intellectual Property Gmbh | Low-dosed solid oral dosage forms for hrt |
| ES2533584T3 (es) | 2010-04-15 | 2015-04-13 | Bayer Intellectual Property Gmbh | Formas de dosificación oral sólidas de dosis baja para TSH |
| CN112516149B (zh) * | 2020-07-21 | 2023-07-18 | 南方医科大学 | 苯甲酸雌二醇或其药物可接受盐在制备抗冠状病毒的药物中的应用 |
| JP2024000555A (ja) * | 2022-06-21 | 2024-01-09 | 東ソー株式会社 | 紫外線抑制下でのエストラジオール測定試薬の製造方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL125069C (https=) * | 1963-12-24 | |||
| US4755386A (en) * | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
| US5073374A (en) * | 1988-11-30 | 1991-12-17 | Schering Corporation | Fast dissolving buccal tablet |
| FR2739558B1 (fr) * | 1995-10-05 | 1997-11-28 | Innothera Lab Sa | Forme galenique unitaire pour hormonotherapie locale de la secheresse vaginale |
| FR2754179B1 (fr) * | 1996-10-08 | 1998-12-24 | Theramex | Nouvelle composition hormononale et son utilisation |
| US6326366B1 (en) * | 2000-08-22 | 2001-12-04 | Protein Technologies International | Hormone replacement therapy |
| WO2002036144A1 (en) * | 2000-10-30 | 2002-05-10 | University Of Zurich | Gnrh analogues for treatment of urinary incontinence |
| AU2002221567A1 (en) * | 2000-12-15 | 2002-06-24 | Novo-Nordisk A/S | Use of an oestrogen in the manufacture of a composition containing oestrogen forthe treatment of atrophic vaginitis |
| FR2823976A1 (fr) * | 2001-04-25 | 2002-10-31 | Theramex | Nouvelle composition hormonale et son utilisation |
| US20030018018A1 (en) * | 2001-07-10 | 2003-01-23 | Medical College Of Hampton Roads | Ultra low dose oral contraceptives with sustained efficacy and induced amenorrhea |
| US6962908B2 (en) * | 2001-12-21 | 2005-11-08 | Warner Chilcott Company Inc. | Oral pharmaceutical products containing 17 β-estradiol-3-lower alkanoate, method of administering the same and process of preparation |
| JP2004155779A (ja) * | 2002-10-16 | 2004-06-03 | Taisho Pharmaceut Co Ltd | 更年期症の予防・治療用経口組成物 |
-
2005
- 2005-10-31 GT GT200500315A patent/GT200500315A/es unknown
- 2005-10-31 UY UY29185A patent/UY29185A1/es not_active Application Discontinuation
- 2005-11-01 CA CA002585095A patent/CA2585095A1/en not_active Abandoned
- 2005-11-01 JP JP2007538360A patent/JP2008518895A/ja active Pending
- 2005-11-01 TW TW094138264A patent/TW200621312A/zh unknown
- 2005-11-01 CN CNA200580045694XA patent/CN101094656A/zh active Pending
- 2005-11-01 WO PCT/EP2005/011726 patent/WO2006048261A2/en not_active Ceased
- 2005-11-01 EA EA200700979A patent/EA013262B1/ru not_active IP Right Cessation
- 2005-11-01 MX MX2007005281A patent/MX2007005281A/es not_active Application Discontinuation
- 2005-11-01 EP EP05800512A patent/EP1814526A2/en not_active Withdrawn
- 2005-11-01 KR KR1020077012174A patent/KR20070085558A/ko not_active Ceased
- 2005-11-01 AU AU2005300658A patent/AU2005300658A1/en not_active Abandoned
- 2005-11-01 BR BRPI0517940-8A patent/BRPI0517940A/pt not_active IP Right Cessation
- 2005-11-02 PA PA20058651401A patent/PA8651401A1/es unknown
- 2005-11-02 PE PE2005001279A patent/PE20061126A1/es not_active Application Discontinuation
- 2005-11-02 AR ARP050104580A patent/AR053650A1/es unknown
-
2007
- 2007-04-18 IL IL182635A patent/IL182635A0/en unknown
- 2007-04-30 CU CU20070094A patent/CU20070094A7/es unknown
- 2007-05-09 CR CR9112A patent/CR9112A/es not_active Application Discontinuation
- 2007-05-29 NO NO20072704A patent/NO20072704L/no not_active Application Discontinuation
- 2007-06-01 ZA ZA200705012A patent/ZA200705012B/xx unknown
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