CA2988485A1 - Orodispersible tablet containing estetrol - Google Patents
Orodispersible tablet containing estetrolInfo
- Publication number
- CA2988485A1 CA2988485A1 CA2988485A CA2988485A CA2988485A1 CA 2988485 A1 CA2988485 A1 CA 2988485A1 CA 2988485 A CA2988485 A CA 2988485A CA 2988485 A CA2988485 A CA 2988485A CA 2988485 A1 CA2988485 A1 CA 2988485A1
- Authority
- CA
- Canada
- Prior art keywords
- dosage unit
- estetrol
- particles
- combinations
- process according
- 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
- AJIPIJNNOJSSQC-NYLIRDPKSA-N estetrol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)[C@@H]4O)O)[C@@H]4[C@@H]3CCC2=C1 AJIPIJNNOJSSQC-NYLIRDPKSA-N 0.000 title claims abstract description 143
- 229950009589 estetrol Drugs 0.000 title claims abstract description 135
- 239000002245 particle Substances 0.000 claims abstract description 120
- 238000000034 method Methods 0.000 claims abstract description 64
- 239000007787 solid Substances 0.000 claims abstract description 55
- 230000008569 process Effects 0.000 claims abstract description 44
- 239000007788 liquid Substances 0.000 claims abstract description 43
- 238000011068 loading method Methods 0.000 claims abstract description 40
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 40
- 239000000203 mixture Substances 0.000 claims abstract description 29
- 239000003960 organic solvent Substances 0.000 claims abstract description 26
- 238000002156 mixing Methods 0.000 claims abstract description 23
- 239000004615 ingredient Substances 0.000 claims abstract description 13
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 48
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 21
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 21
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 19
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- UXYRZJKIQKRJCF-TZPFWLJSSA-N mesterolone Chemical compound C1C[C@@H]2[C@@]3(C)[C@@H](C)CC(=O)C[C@@H]3CC[C@H]2[C@@H]2CC[C@H](O)[C@]21C UXYRZJKIQKRJCF-TZPFWLJSSA-N 0.000 description 1
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- VOCBWIIFXDYGNZ-IXKNJLPQSA-N testosterone enanthate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCC)[C@@]1(C)CC2 VOCBWIIFXDYGNZ-IXKNJLPQSA-N 0.000 description 1
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Classifications
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- 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
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- 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
-
- 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
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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
- A61P15/18—Feminine contraceptives
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Zoology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15172751 | 2015-06-18 | ||
| EP15172751.8 | 2015-06-18 | ||
| PCT/EP2016/064071 WO2016203009A1 (en) | 2015-06-18 | 2016-06-17 | Orodispersible tablet containing estetrol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2988485A1 true CA2988485A1 (en) | 2016-12-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2988485A Abandoned CA2988485A1 (en) | 2015-06-18 | 2016-06-17 | Orodispersible tablet containing estetrol |
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|---|---|
| US (1) | US10894014B2 (enExample) |
| EP (1) | EP3310345B1 (enExample) |
| JP (1) | JP6866561B2 (enExample) |
| CN (1) | CN107810001A (enExample) |
| CA (1) | CA2988485A1 (enExample) |
| CY (1) | CY1124104T1 (enExample) |
| DK (1) | DK3310345T3 (enExample) |
| ES (1) | ES2877186T3 (enExample) |
| HR (1) | HRP20210668T1 (enExample) |
| HU (1) | HUE054589T2 (enExample) |
| LT (1) | LT3310345T (enExample) |
| MA (1) | MA44205B1 (enExample) |
| MD (1) | MD3310345T2 (enExample) |
| PL (1) | PL3310345T3 (enExample) |
| PT (1) | PT3310345T (enExample) |
| RS (1) | RS61812B1 (enExample) |
| SI (1) | SI3310345T1 (enExample) |
| SM (1) | SMT202100370T1 (enExample) |
| WO (1) | WO2016203009A1 (enExample) |
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| CA2835979C (en) | 2011-06-01 | 2018-05-01 | Estetra S.A. | Process for the production of estetrol intermediates |
| US11053274B2 (en) | 2011-06-01 | 2021-07-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| CN116077454A (zh) | 2015-06-18 | 2023-05-09 | 埃斯特拉有限责任公司 | 含雌四醇组分的口腔分散剂量单位 |
| US11147771B2 (en) | 2015-06-18 | 2021-10-19 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| JP6813150B2 (ja) | 2015-06-18 | 2021-01-13 | エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ | エステトロールを含有する口腔内崩壊錠 |
| ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
| CA3178291A1 (en) | 2016-08-05 | 2018-04-12 | Estetra Srl | Method for the management of dysmenorrhea and menstrual pain |
| TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
| JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
| HU231240B1 (hu) | 2019-09-03 | 2022-04-28 | Richter Gedeon Nyrt. | Ipari eljárás nagytisztaságú ösztetrol hatóanyag előállítására |
| US12427113B2 (en) | 2019-11-07 | 2025-09-30 | Asahi Kasei Kabushiki Kaisha | Cellulose composition, tablet, and orally disintegrating tablet |
| TWI893101B (zh) | 2020-04-16 | 2025-08-11 | 比利時商埃斯特拉有限責任公司 | 具有降低之副作用之避孕組成物 |
| WO2022069956A1 (en) | 2020-09-29 | 2022-04-07 | Millicent Pharma Limited | Orodispersible formulations |
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| US3138588A (en) | 1962-08-24 | 1964-06-23 | American Home Prod | 17-ketals of estrone and derivatives thereof |
| US3433785A (en) | 1966-07-11 | 1969-03-18 | Sterling Drug Inc | 15,16-disubstituted aromatic steroids,intermediates and processes |
| US5073374A (en) | 1988-11-30 | 1991-12-17 | Schering Corporation | Fast dissolving buccal tablet |
| US5340586A (en) | 1991-04-12 | 1994-08-23 | University Of Southern California | Methods and formulations for use in treating oophorectomized women |
| JPH07101977A (ja) | 1993-10-05 | 1995-04-18 | Kureha Chem Ind Co Ltd | ホルモン作用を軽減した新規なエストラジオール誘導体及びその増殖因子阻害剤 |
| DE4344405C2 (de) | 1993-12-24 | 1995-12-07 | Marika Dr Med Ehrlich | Ovulationshemmendes Mittel und Verfahren zur hormonalen Kontrazeption |
| WO1997004752A1 (en) | 1995-07-26 | 1997-02-13 | Duramed Pharmaceuticals, Inc. | Pharmaceutical compositions of conjugated estrogens and methods for their use |
| US6117446A (en) | 1999-01-26 | 2000-09-12 | Place; Virgil A. | Drug dosage unit for buccal administration of steroidal active agents |
| TW548277B (en) | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
| AU778017B2 (en) | 1999-12-02 | 2004-11-11 | N.V. Organon | 14,15-beta-methylene substituted androgens |
| US20020132801A1 (en) | 2001-01-11 | 2002-09-19 | Schering Aktiengesellschaft | Drospirenone for hormone replacement therapy |
| DE10044241A1 (de) * | 2000-09-07 | 2002-03-21 | Mahle Gmbh | Kolbenring für Kolben-Maschine |
| EP1216713A1 (en) | 2000-12-20 | 2002-06-26 | Schering Aktiengesellschaft | Compositions of estrogen-cyclodextrin complexes |
| EP1260225A1 (en) | 2001-05-18 | 2002-11-27 | Pantarhei Bioscience B.V. | A pharmaceutical composition for use in hormone replacement therapy |
| US8048869B2 (en) | 2001-05-18 | 2011-11-01 | Pantarhei Bioscience B.V. | Pharmaceutical composition for use in hormone replacement therapy |
| ES2337129T3 (es) | 2001-05-23 | 2010-04-21 | Pantarhei Bioscience B.V. | Sistema de administracion de medicamento comprendiendo un estrogeno tetrahidroxilado para el uso en la anticoncepcion hormonal. |
| DK1390042T3 (da) | 2001-05-23 | 2008-03-31 | Pantarhei Bioscience Bv | System for administration af et lægemiddel omfattende tetrahydroxyleret östrogen til anvendelse i hormonal svangerskabsforebyggelse |
| WO2003018026A1 (en) | 2001-08-31 | 2003-03-06 | Pantarhei Bioscience B.V. | Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy |
| WO2003041718A1 (en) | 2001-11-15 | 2003-05-22 | Pantarhei Bioscience B.V. | Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy |
| US6723348B2 (en) | 2001-11-16 | 2004-04-20 | Ethypharm | Orodispersible tablets containing fexofenadine |
| HU227198B1 (en) | 2001-11-27 | 2010-10-28 | Richter Gedeon Nyrt | Pharmaceutical composition for emergency contraception containing levonorgestrel |
| DK1478373T3 (da) | 2002-02-21 | 2007-01-15 | Schering Ag | Farmaceutisk præparat omfattende ét eller flere steroider, én eller flere tetrahydrofolatbestanddele og vitamin B 12 |
| US20050147670A1 (en) | 2002-05-29 | 2005-07-07 | Impax Laboratories Inc. | Oral disintegrating dosage forms |
| CN1691947B (zh) | 2002-06-11 | 2011-11-23 | 潘塔希生物科学股份有限公司 | 雌激素成分在制备用于治疗或预防免疫介导的疾病中的应用以及包含所述雌激素成分的药物组合物 |
| CN100352445C (zh) | 2002-06-11 | 2007-12-05 | 潘塔希生物科学股份有限公司 | 一种皮肤护理组合物及其用途 |
| ES2299730T3 (es) | 2002-07-12 | 2008-06-01 | Pantarhei Bioscience B.V. | Composicion farmaceutica que comprende derivados de estetrol para el uso en la terapia del cancer. |
| KR20050059092A (ko) | 2002-08-28 | 2005-06-17 | 로버트 캐스퍼 | 에스트로겐 보충 요법 |
| CA2503549C (en) | 2002-10-23 | 2012-07-10 | Pantarhei Bioscience B.V. | Pharmaceutical compositions comprising estetrol derivatives for use in cancer therapy |
| DK1558265T3 (da) | 2002-11-05 | 2010-03-15 | Bayer Schering Pharma Ag | Anvendelse af dropspirenon til behandling af hypertension |
| ATE469165T1 (de) | 2002-11-08 | 2010-06-15 | Pantarhei Bioscience Bv | Synthese von oestetrol aus von oestron abgeleiteten steroiden |
| ES2274456T3 (es) | 2003-05-22 | 2007-05-16 | Pantarhei Bioscience B.V. | Uso de composiciones que comprenden un componente estrogenico para el tratamiento y la prevencion del dolor musculoesqueletico. |
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-
2016
- 2016-06-17 ES ES16729601T patent/ES2877186T3/es active Active
- 2016-06-17 PL PL16729601T patent/PL3310345T3/pl unknown
- 2016-06-17 HU HUE16729601A patent/HUE054589T2/hu unknown
- 2016-06-17 MD MDE20180402T patent/MD3310345T2/ro unknown
- 2016-06-17 CA CA2988485A patent/CA2988485A1/en not_active Abandoned
- 2016-06-17 DK DK16729601.1T patent/DK3310345T3/da active
- 2016-06-17 SM SM20210370T patent/SMT202100370T1/it unknown
- 2016-06-17 JP JP2017564396A patent/JP6866561B2/ja not_active Expired - Fee Related
- 2016-06-17 US US15/737,233 patent/US10894014B2/en active Active
- 2016-06-17 CN CN201680035673.8A patent/CN107810001A/zh active Pending
- 2016-06-17 HR HRP20210668TT patent/HRP20210668T1/hr unknown
- 2016-06-17 WO PCT/EP2016/064071 patent/WO2016203009A1/en not_active Ceased
- 2016-06-17 SI SI201631167T patent/SI3310345T1/sl unknown
- 2016-06-17 MA MA44205A patent/MA44205B1/fr unknown
- 2016-06-17 PT PT167296011T patent/PT3310345T/pt unknown
- 2016-06-17 EP EP16729601.1A patent/EP3310345B1/en active Active
- 2016-06-17 RS RS20210512A patent/RS61812B1/sr unknown
- 2016-06-17 LT LTEP16729601.1T patent/LT3310345T/lt unknown
-
2021
- 2021-05-05 CY CY20211100379T patent/CY1124104T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2877186T3 (es) | 2021-11-16 |
| LT3310345T (lt) | 2021-06-25 |
| PL3310345T3 (pl) | 2021-10-18 |
| US10894014B2 (en) | 2021-01-19 |
| HUE054589T2 (hu) | 2021-09-28 |
| HRP20210668T1 (hr) | 2021-05-28 |
| EP3310345B1 (en) | 2021-03-31 |
| JP6866561B2 (ja) | 2021-04-28 |
| SMT202100370T1 (it) | 2021-07-12 |
| MA44205B1 (fr) | 2021-04-30 |
| CN107810001A (zh) | 2018-03-16 |
| DK3310345T3 (da) | 2021-05-25 |
| MA44205A (fr) | 2018-04-25 |
| WO2016203009A1 (en) | 2016-12-22 |
| US20180185271A1 (en) | 2018-07-05 |
| JP2018517718A (ja) | 2018-07-05 |
| EP3310345A1 (en) | 2018-04-25 |
| SI3310345T1 (sl) | 2021-05-31 |
| RS61812B1 (sr) | 2021-06-30 |
| MD3310345T2 (ro) | 2021-07-31 |
| PT3310345T (pt) | 2021-05-28 |
| CY1124104T1 (el) | 2022-05-27 |
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