HRP20130892T1 - Farmaceutske formulacije i njihove upotrebe u lijeäśenju ženske seksualne disfunkcije - Google Patents

Farmaceutske formulacije i njihove upotrebe u lijeäśenju ženske seksualne disfunkcije Download PDF

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HRP20130892T1
HRP20130892T1 HRP20130892TT HRP20130892T HRP20130892T1 HR P20130892 T1 HRP20130892 T1 HR P20130892T1 HR P20130892T T HRP20130892T T HR P20130892TT HR P20130892 T HRP20130892 T HR P20130892T HR P20130892 T1 HRP20130892 T1 HR P20130892T1
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testosterone
combination
dihydrotestosterone
use according
pde5
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HRP20130892TT
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Jan Johan Adriaan Tuiten
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Emotional Brain B.V.
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Publication of HRP20130892T1 publication Critical patent/HRP20130892T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61K31/568Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/716Glucans
    • A61K31/724Cyclodextrins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/40Cyclodextrins; 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
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P5/26Androgens
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16HHEALTHCARE INFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR THE HANDLING OR PROCESSING OF MEDICAL OR HEALTHCARE DATA
    • G16H20/00ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance
    • G16H20/10ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16HHEALTHCARE INFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR THE HANDLING OR PROCESSING OF MEDICAL OR HEALTHCARE DATA
    • G16H70/00ICT specially adapted for the handling or processing of medical references
    • G16H70/40ICT specially adapted for the handling or processing of medical references relating to drugs, e.g. their side effects or intended usage

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Reproductive Health (AREA)
  • Toxicology (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Business, Economics & Management (AREA)
  • Tourism & Hospitality (AREA)
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  • Child & Adolescent Psychology (AREA)
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Claims (22)

1. Kombinacija od PDE5-inhibitora i testosterona ili dihidrotestosterona, naznačena time, da se upotrebljava kao lijek za liječenje ženske seksualne disfunkcije, pri čemu se testosteron primjenjuje 3,5 do 5,5 sati prije seksualne aktivnosti ili se dihidrotestosteron primjenjuje 3 do 5 sati prije seksualne aktivnosti, dok se PDE5-inhibitor primjenjuje 1 do 2 sata prije seksualne aktivnosti, tako da se učinci tih spojeva barem djelomično preklapaju.
2. Kombinacija za uporabu prema zahtjevu 1, naznačena time, da se testosteron ili dihidrotestosteron formuliraju za dobivanje vršne vrijednosti slobodnog testosterona ili dihidrotestosterona u cirkulaciji krvi od najmanje 0,010 nmol/l kod pacijenta koji pati od seksualne disfunkcije.
3. Kombinacija za uporabu prema bilo kojem zahtjevu od 1 do 2, naznačena time, da se testosteron ili dihidrotestosteron dobavljaju u obliku podjezične recepture.
4. Kombinacija za uporabu prema zahtjevu 3, naznačena time, da spomenuta podjezična receptura sadrži ciklodekstrin, primjerice hidroksipropil-betaciklodekstrin.
5. Kombinacija za uporabu prema bilo kojem zahtjevu od 1 do 2, naznačena time, da je testosteron ili dihidrotestosteron pripremljen za oslobađanje uglavnom cjelokupnog testosterona ili dihidrotestosterona unutar vremenskog perioda od 60 sekundi nakon primjene.
6. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5, naznačena time, da spomenuti lijek obuhvaća jedan sastav koji sadrži testosteron i jedan sastav koji sadrži PDE5-inhibitor.
7. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5, naznačena time, da spomenuti lijek obuhvaća jednu kapsulu ili recepturu s različitim svojstvima otpuštanja za dva sastava.
8. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 7, naznačena time, da spomenuti lijek obuhvaća najmanje 0,3 mg testosterona i najviše 2,5 mg testosterona.
9. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 8, naznačena time, da spomenuti lijek obuhvaća najmanje 5 mg vardenafila i najviše 20 mg vardenafila.
10. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 8, naznačena time, da spomenuti lijek obuhvaća najmanje 25 mg sildenafila i najviše 100 mg sildenafila.
11. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 8, naznačena time, da spomenuti lijek obuhvaća najmanje 5 mg tadalafila i najviše 20 mg tadalafila.
12. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 11, naznačena time, da spomenuti lijek nadalje obuhvaća spoj koji se nadmeće s testosteronom ili dihidrotestosteronom u vezivanju za SHBG.
13. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 12, naznačena time, da nadalje obuhvaća agonist dopaminskog prolaza.
14. Kombinacija za uporabu prema bilo kojem zahtjevu od 1, 2 ili 5 do 13, naznačena time, da nadalje obuhvaća inhibiciju adrenergijskog tonusa u centralnom nervnom sustavu.
15. Garnitura od dijelova za uporabu u liječenju ženske seksualne disfunkcije, naznačena time, da se putem nje primjenjuje testosteron 3,5 do 5,5 sati prije seksualne aktivnosti ili se dihidrotestosteron primjenjuje 3 do 5 sati prije seksualne aktivnosti, a PDE5-inhibitor se primjenjuje 1 do 2 sata prije seksualne aktivnosti, tako da se učinci spojeva barem djelomično preklapaju, pri čemu ta garnitura od dijelova sadrži najmanje jedan farmaceutski sastav koji obuhvaća testosteron ili dihidrotestosteron i najmanje jedan farmaceutski sastav koji obuhvaća PDE5-inhibitor, gdje je spomenuti sastav koji obuhvaća testosteron ili dihidrotestosteron, pripravljen za oslobađanje cjelokupnog testosterona uglavnom odmah na ciljanom mjestu.
16. Garnitura od dijelova prema zahtjevu 15, naznačena time, da farmaceutski sastav koji obuhvaća testosteron, sadrži najmanje 0,3 mg testosterona i najviše 2,5 mg testosterona.
17. Garnitura od dijelova prema zahtjevu 15 ili 16, naznačena time, da farmaceutski sastav koji obuhvaća PDE5-inhibitor, sadrži najmanje 5 mg vardenafila i najviše 20 mg vardenafila.
18. Garnitura od dijelova prema zahtjevu 15 ili 16, naznačena time, da farmaceutski sastav koji obuhvaća PDE5-inhibitor, sadrži najmanje 25 mg sildenafila i najviše 100 mg sildenafila.
19. Garnitura od dijelova prema zahtjevu 15 ili 16, naznačena time, da farmaceutski sastav koji obuhvaća PDE5-inhibitor, sadrži najmanje 5 mg tadalafila i najviše 20 mg tadalafila.
20. Garnitura od dijelova prema bio kojem zahtjevu od 15 do 19, naznačena time, da ona nadalje obuhvaća agonist dopaminskog prolaza.
21. Garnitura od dijelova prema bio kojem zahtjevu od 15 do 19, naznačena time, da nadalje obuhvaća inhibiciju adrenergijskog tonusa u centralnom nervnom sustavu.
22. Farmaceutski sastav za uporabu u prema bilo kojem zahtjevu od 1 do 14, naznačen time, da spomenuti farmaceutski sastav obuhvaća PDE5-inhibitor i testosteron ili dihidrotestosteron zapakirane u jednoj kapsuli ili recepturi s različitim svojstvima oslobađanja za dva spoja, tako da se učinci od PDE5-inhibitora i testosterona ili dihidrotestosterona podudaraju.
HRP20130892TT 2004-05-11 2013-09-20 Farmaceutske formulacije i njihove upotrebe u lijeäśenju ženske seksualne disfunkcije HRP20130892T1 (hr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP04076402 2004-05-11
EP04078033 2004-11-04
EP04078381 2004-12-13
EP04078380 2004-12-13
EP04078455 2004-12-21
PCT/NL2005/000355 WO2005107810A2 (en) 2004-05-11 2005-05-11 Pharmaceutical formulations and uses thereof in the treatment of female sexual dysfunction

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US (5) US8227453B2 (hr)
EP (1) EP1750766B1 (hr)
JP (3) JP2007537247A (hr)
KR (1) KR101292492B1 (hr)
CN (2) CN101027061B (hr)
AU (1) AU2005239962B2 (hr)
BR (1) BRPI0511079A (hr)
CA (1) CA2566699C (hr)
CY (1) CY1114448T1 (hr)
DK (1) DK1750766T3 (hr)
ES (1) ES2429444T3 (hr)
HK (1) HK1108128A1 (hr)
HR (1) HRP20130892T1 (hr)
MX (2) MX347237B (hr)
NZ (1) NZ551356A (hr)
PL (1) PL1750766T3 (hr)
PT (1) PT1750766E (hr)
RS (1) RS52945B (hr)
RU (2) RU2436579C2 (hr)
SI (1) SI1750766T1 (hr)
WO (1) WO2005107810A2 (hr)
ZA (1) ZA200609974B (hr)

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