HRP20180129T1 - Oralno raspadajuća čvrsta jedinica doze koja sadrži estetrol komponentu - Google Patents

Oralno raspadajuća čvrsta jedinica doze koja sadrži estetrol komponentu Download PDF

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Publication number
HRP20180129T1
HRP20180129T1 HRP20180129TT HRP20180129T HRP20180129T1 HR P20180129 T1 HRP20180129 T1 HR P20180129T1 HR P20180129T T HRP20180129T T HR P20180129TT HR P20180129 T HRP20180129 T HR P20180129T HR P20180129 T1 HRP20180129 T1 HR P20180129T1
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HR
Croatia
Prior art keywords
dosage unit
solid dosage
unit according
solid
estetrol
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Application number
HRP20180129TT
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English (en)
Inventor
Johannes Jan Platteeuw
Herman Jan Tijmen Coelingh Bennink
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Donesta Bioscience B.V.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49759137&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20180129(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Donesta Bioscience B.V. filed Critical Donesta Bioscience B.V.
Publication of HRP20180129T1 publication Critical patent/HRP20180129T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • A61K31/573Compounds 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 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Zoology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Biochemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (17)

1. Oralno raspadajuća čvrsta farmaceutska jedinica doze koja ima težinu između 50 i 1,000 mg, naznačena time što se navedena jedinica doze sastoji od: • 4-95 tež.% granula koje se sastoje od: - 3-80 tež.% estetrol komponente izabrane od estetrola, estetrol estera i njihovih kombinacija; - 20-97 tež.% C4-C12 šećernog alkohola; - 0-45 tež.% jednog ili više drugih farmaceutski prihvatljivih sastojaka; i • 5-96 tež.% jednog ili više farmaceutski prihvatljivih ekscipijensa. pri čemu čvrsta jedinica doze sadrži najmanje 0.1 mg estetrol komponente.
2. Čvrsta jedinica doze prema patentnom zahtjevu 1, naznačena time što je estetrol komponenta estetrol, poželjno anhidridan estetrol.
3. Čvrsta jedinica doze prema patentnom zahtjevu 1 ili 2, naznačena time što granule predstavljaju između 5 i 90 tež. % jedinice doze.
4. Čvrsta jedinica doze prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time što granule imaju srednju veličinu prema zapremini između 30 i 200 μm, poželjno između 40 i 150 μm.
5. Čvrsta jedinica doze prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time što je C4-C12 šećerni alkohol izabran od manitola, eritritola, izomalta i njihovih kombinacija.
6. Čvrsta jedinica doze prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time što jedan ili više farmaceutski prihvatljivih ekscipijensa sadrže najmanje 30% prema težini navedenog jednog ili više farmaceutski prihvatljivih ekscipijensa čestica koje sadrže sredstvo za raspadanje disperzirano u matriksu koji sadrži C4-C6 šećerni alkohol.
7. Čvrsta jedinica doze prema patentnom zahtjevu 6, naznačena time što čestice sadrže 10-50 tež. % sredstva za raspadanje i 40-90 tež. % C4-C6 šećernog alkohola.
8. Čvrsta jedinica doze prema patentnom zahtjevu 7, naznačena time što je sredstvo za raspadanje izabrano od krospovidona, hidroksipropil celuloze, kroskarmeloze natrija i kristalne celuloze i njihovih kombinacija.
9. Čvrsta jedinica doze prema bilo kojem od patentnih zahtjeva 6-8, naznačena time što je C4-C6 šećerni alkohol izabran od manitola, ksilitola i njihovih kombinacija.
10. Čvrsta jedinica doze prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time što jedinica doze sadrži 0.05-10 mg progestogena.
11. Čvrsta jedinica doze prema bilo kojem od prethodnih patentnih zahtjeva za upotrebu u medicinskom liječenju ili za upotrebu u zamjenskoj hormonskoj terapiji kod žena, pri čemu navedena upotreba sadrži sublingualnu, bukalnu ili sublabijalnu primjenu jedinice doze.
12. Čvrsta jedinica doze za upotrebu prema patentnom zahtjevu 11, naznačena time što navedena upotreba sadrži primjenu jednom dnevno u tijeku perioda od najmanje 1 tjedna.
13. Postupak ženske kontracepcije, naznačen time što navedeni postupak sadrži subligualnu, bukalnu ili sublabijalnu primjenu jedinice doze prema bilo kojem od patentnih zahtjeva 1-10.
14. Postupak prema patentnom zahtjevu 13, naznačen time što navedeni postupak sadrži primjenu jednom dnevno u tijeku perioda od najmanje 1 tjedna.
15. Postupak za pripremu čvrste jedinice doze prema bilo kojem od patentnih zahtjeva 1-10, naznačen time što navedeni postupak sadrži korake: • osiguravanje vrele smjese estetrol komponente koja se može pumpati, C4-C12 šećernog alkohola i izborno jednog ili više drugih farmaceutski prihvatljivih sastojaka, pri čemu navedena vrela smjesa koja se može pumpati ima temperaturu od najmanje 105°C; • hlađenje vrele smjese koja se može pumpati da bi se stvrdnuo C4-C12 šećerni alkohol i razbijanje smjese koja se može pumpati prije ili poslije navedenog hlađenja da bi se proizvele čvrste granule; • miješanje granula s jednim ili više farmaceutski prihvatljivih ekscipijensa; i • formiranje smjese u čvrstu jedinicu doze.
16. Postupak prema patentnom zahtjevu 15, naznačen time što smjesa koja se može pumpati ima temperaturu od najmanje 160°C, poželjno od 180 do 240°C.
17. Postupak prema patentnom zahtjevu 15 ili 16, naznačen time što je vrela smjesa koja se može pumpati podvrgnuta hlađenju prskanjem da bi se proizvele čvrste granule.
HRP20180129TT 2013-12-12 2018-01-23 Oralno raspadajuća čvrsta jedinica doze koja sadrži estetrol komponentu HRP20180129T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13196904 2013-12-12
PCT/EP2014/077127 WO2015086643A1 (en) 2013-12-12 2014-12-10 Orally disintegrating solid dosage unit containing an estetrol component
EP14814804.2A EP3079671B1 (en) 2013-12-12 2014-12-10 Orally disintegrating solid dosage unit containing an estetrol component

Publications (1)

Publication Number Publication Date
HRP20180129T1 true HRP20180129T1 (hr) 2018-02-23

Family

ID=49759137

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20180129TT HRP20180129T1 (hr) 2013-12-12 2018-01-23 Oralno raspadajuća čvrsta jedinica doze koja sadrži estetrol komponentu

Country Status (29)

Country Link
US (2) US9884064B2 (hr)
EP (1) EP3079671B1 (hr)
JP (1) JP6447931B2 (hr)
KR (1) KR102265150B1 (hr)
CN (1) CN105979935B (hr)
AU (1) AU2014363599B2 (hr)
BR (1) BR112016013502B1 (hr)
CA (1) CA2932855C (hr)
CL (1) CL2016001411A1 (hr)
CY (1) CY1119817T1 (hr)
DK (1) DK3079671T3 (hr)
EA (1) EA032306B1 (hr)
ES (1) ES2655076T3 (hr)
HR (1) HRP20180129T1 (hr)
HU (1) HUE035848T2 (hr)
IL (1) IL246082B (hr)
LT (1) LT3079671T (hr)
MA (1) MA39105B1 (hr)
MX (1) MX369035B (hr)
NO (1) NO3079671T3 (hr)
NZ (1) NZ720906A (hr)
PL (1) PL3079671T3 (hr)
PT (1) PT3079671T (hr)
RS (1) RS56738B1 (hr)
SG (1) SG11201604741UA (hr)
SI (1) SI3079671T1 (hr)
TN (1) TN2016000230A1 (hr)
WO (1) WO2015086643A1 (hr)
ZA (1) ZA201603903B (hr)

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UA123098C2 (uk) * 2015-06-18 2021-02-17 Естетра Спрл Диспергована у порожнині рота одиниця дозування, що містить естетрольний компонент
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Also Published As

Publication number Publication date
US20160310506A1 (en) 2016-10-27
SG11201604741UA (en) 2016-07-28
EA032306B1 (ru) 2019-05-31
DK3079671T3 (en) 2017-12-11
MA39105B1 (fr) 2018-05-31
CN105979935B (zh) 2019-07-26
NZ720906A (en) 2022-04-29
JP2016540021A (ja) 2016-12-22
EA201691226A1 (ru) 2016-10-31
AU2014363599A1 (en) 2016-06-30
WO2015086643A1 (en) 2015-06-18
CA2932855C (en) 2022-07-19
US20180117063A1 (en) 2018-05-03
CA2932855A1 (en) 2015-06-18
CN105979935A (zh) 2016-09-28
PT3079671T (pt) 2017-11-24
AU2014363599B2 (en) 2019-10-31
US9987287B2 (en) 2018-06-05
PL3079671T3 (pl) 2018-03-30
IL246082A0 (en) 2016-07-31
MX2016007595A (es) 2016-11-28
LT3079671T (lt) 2018-02-12
ES2655076T3 (es) 2018-02-16
TN2016000230A1 (en) 2017-10-06
BR112016013502A2 (pt) 2018-07-03
SI3079671T1 (en) 2018-04-30
IL246082B (en) 2018-03-29
BR112016013502B1 (pt) 2021-05-11
ZA201603903B (en) 2018-07-25
KR20160102212A (ko) 2016-08-29
HUE035848T2 (en) 2018-05-28
CL2016001411A1 (es) 2016-11-11
CY1119817T1 (el) 2018-06-27
KR102265150B1 (ko) 2021-06-16
NO3079671T3 (hr) 2018-03-24
EP3079671B1 (en) 2017-10-25
JP6447931B2 (ja) 2019-01-09
RS56738B1 (sr) 2018-03-30
MX369035B (es) 2019-10-25
MA39105A1 (fr) 2017-04-28
EP3079671A1 (en) 2016-10-19
US9884064B2 (en) 2018-02-06

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