CA2585095A1 - Oral solid dosage forms containing a low dose of estradiol - Google Patents
Oral solid dosage forms containing a low dose of estradiol Download PDFInfo
- Publication number
- CA2585095A1 CA2585095A1 CA002585095A CA2585095A CA2585095A1 CA 2585095 A1 CA2585095 A1 CA 2585095A1 CA 002585095 A CA002585095 A CA 002585095A CA 2585095 A CA2585095 A CA 2585095A CA 2585095 A1 CA2585095 A1 CA 2585095A1
- Authority
- CA
- Canada
- Prior art keywords
- estradiol
- dosage form
- 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.)
- Abandoned
Links
- 229960005309 estradiol Drugs 0.000 title claims abstract description 174
- 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 title claims abstract description 172
- 229930182833 estradiol Natural products 0.000 title claims abstract description 171
- 239000008184 oral solid dosage form Substances 0.000 title claims abstract description 53
- 239000002552 dosage form Substances 0.000 claims abstract description 77
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 63
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 63
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 59
- 150000003839 salts Chemical class 0.000 claims description 56
- 239000011230 binding agent Substances 0.000 claims description 50
- 239000000203 mixture Substances 0.000 claims description 44
- 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 description 39
- 229960003851 estradiol hemihydrate Drugs 0.000 claims description 38
- 229920002472 Starch Polymers 0.000 claims description 37
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- 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 description 2
- 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 description 2
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- 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 description 2
- 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 description 2
- TXHUMRBWIWWBGW-UHFFFAOYSA-N Estradiol undecylate Natural products C1CC2=CC(O)=CC=C2C2C1C1CCC(OC(=O)CCCCCCCCCC)C1(C)CC2 TXHUMRBWIWWBGW-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 2
- 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 description 2
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- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
- 229960003575 estradiol acetate Drugs 0.000 claims description 2
- 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 description 2
- 229950002007 estradiol benzoate Drugs 0.000 claims description 2
- 229960005416 estradiol cypionate Drugs 0.000 claims description 2
- 229950010215 estradiol dipropionate Drugs 0.000 claims description 2
- 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 description 2
- 229950005281 estradiol undecylate Drugs 0.000 claims description 2
- TXHUMRBWIWWBGW-GVGNIZHQSA-N estradiol undecylate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCCCCCC)[C@@]1(C)CC2 TXHUMRBWIWWBGW-GVGNIZHQSA-N 0.000 claims description 2
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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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Reproductive Health (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04078014.0 | 2004-11-02 | ||
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| CA2585095A1 true CA2585095A1 (en) | 2006-05-11 |
Family
ID=34928627
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002585095A Abandoned CA2585095A1 (en) | 2004-11-02 | 2005-11-01 | Oral solid dosage forms containing a low dose of estradiol |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1814526A2 (zh) |
| JP (1) | JP2008518895A (zh) |
| KR (1) | KR20070085558A (zh) |
| CN (1) | CN101094656A (zh) |
| AR (1) | AR053650A1 (zh) |
| AU (1) | AU2005300658A1 (zh) |
| BR (1) | BRPI0517940A (zh) |
| CA (1) | CA2585095A1 (zh) |
| CR (1) | CR9112A (zh) |
| CU (1) | CU20070094A7 (zh) |
| EA (1) | EA013262B1 (zh) |
| GT (1) | GT200500315A (zh) |
| IL (1) | IL182635A0 (zh) |
| MX (1) | MX2007005281A (zh) |
| NO (1) | NO20072704L (zh) |
| PA (1) | PA8651401A1 (zh) |
| PE (1) | PE20061126A1 (zh) |
| TW (1) | TW200621312A (zh) |
| UY (1) | UY29185A1 (zh) |
| WO (1) | WO2006048261A2 (zh) |
| ZA (1) | ZA200705012B (zh) |
Families Citing this family (6)
| 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 |
| BR112012026115B1 (pt) | 2010-04-15 | 2019-12-24 | Bayer Ip Gmbh | forma de dosagem oral sólida, seu uso, e unidade de acondicionamento |
| US20130140210A1 (en) | 2010-04-15 | 2013-06-06 | Bayer Intellectual Property Gmbh | Low-dosed solid oral dosage forms for hrt |
| 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 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL125071C (zh) * | 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 |
| AU2001295359A1 (en) * | 2000-10-30 | 2002-05-15 | University Of Zurich | GnRH analogues for treatment of urinary incontinence |
| ATE532521T1 (de) * | 2000-12-15 | 2011-11-15 | Novo Nordisk Femcare Ag | Verwendung eines östrogens bei der herstellung einer östrogenhaltigen zusammensetzung zur behandlung von atrophischer 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 EA EA200700979A patent/EA013262B1/ru not_active IP Right Cessation
- 2005-11-01 KR KR1020077012174A patent/KR20070085558A/ko not_active Application Discontinuation
- 2005-11-01 CN CNA200580045694XA patent/CN101094656A/zh active Pending
- 2005-11-01 WO PCT/EP2005/011726 patent/WO2006048261A2/en active Application Filing
- 2005-11-01 JP JP2007538360A patent/JP2008518895A/ja active Pending
- 2005-11-01 BR BRPI0517940-8A patent/BRPI0517940A/pt not_active IP Right Cessation
- 2005-11-01 AU AU2005300658A patent/AU2005300658A1/en not_active Abandoned
- 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 TW TW094138264A patent/TW200621312A/zh unknown
- 2005-11-01 CA CA002585095A patent/CA2585095A1/en not_active Abandoned
- 2005-11-02 PE PE2005001279A patent/PE20061126A1/es not_active Application Discontinuation
- 2005-11-02 PA PA20058651401A patent/PA8651401A1/es unknown
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| NO20072704L (no) | 2007-05-29 |
| PA8651401A1 (es) | 2006-12-07 |
| MX2007005281A (es) | 2008-03-11 |
| WO2006048261A2 (en) | 2006-05-11 |
| CR9112A (es) | 2007-11-23 |
| EA013262B1 (ru) | 2010-04-30 |
| AU2005300658A1 (en) | 2006-05-11 |
| UY29185A1 (es) | 2006-05-31 |
| CN101094656A (zh) | 2007-12-26 |
| EA200700979A1 (ru) | 2007-10-26 |
| ZA200705012B (en) | 2008-10-29 |
| AR053650A1 (es) | 2007-05-16 |
| JP2008518895A (ja) | 2008-06-05 |
| TW200621312A (en) | 2006-07-01 |
| WO2006048261A3 (en) | 2006-09-21 |
| IL182635A0 (en) | 2007-07-24 |
| GT200500315A (es) | 2006-06-06 |
| PE20061126A1 (es) | 2006-11-11 |
| BRPI0517940A (pt) | 2008-10-21 |
| KR20070085558A (ko) | 2007-08-27 |
| EP1814526A2 (en) | 2007-08-08 |
| CU20070094A7 (es) | 2009-09-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |
Effective date: 20131007 |