SI20360B - Sredstva in metode za zdravljenje motenj v zvezi z neuravnovešenostjo ter hiperaktivnih motenj v zvezi z neuravnovešenostjo s pomočjo metilfenidata - Google Patents

Sredstva in metode za zdravljenje motenj v zvezi z neuravnovešenostjo ter hiperaktivnih motenj v zvezi z neuravnovešenostjo s pomočjo metilfenidata Download PDF

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SI20360B
SI20360B SI9820083A SI9820083A SI20360B SI 20360 B SI20360 B SI 20360B SI 9820083 A SI9820083 A SI 9820083A SI 9820083 A SI9820083 A SI 9820083A SI 20360 B SI20360 B SI 20360B
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methylphenidate
agent
polymer
natural
acrylic polymer
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SI20360A (sl
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Juan Mantelle
Terese A Dixon
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Noven Pharma
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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
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A61K9/7061Polyacrylates
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4458Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7069Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

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  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Izum se nanaša na metode za zdravljenje motenj vzvezi neuravnovešenostjo (ADD) ter hiperaktivnostnih motenj v zvezi neuravnovešenostjo (ADHD) kottudi na sredstva za topično uporabo metilfenidata v farmacevtsko spremljivem gibkem končnem sistemu, kjer je metilfenidat prisoten v količini, ki pri doziranju skozi pacientovo kožo ali sluznico zadostuje za doseganje kinetike v bistvu ničtega reda v časovnem obdobju vsaj 10 ur.

Description

* V tem dokumentu so objavljeni spremenjeni zahtevki patenta 20360 A. Zahtevki so bili spremenjeni na podlagi ugotovitvene odločbe, izdane po členu 93( 1 )(b)

Claims (23)

1. Sredstvo za topično uporabo metilfenidata, obsegajoče metilfenidat v fleksibilnem končnem sistemu, pri čemer sistem obsega naraven ali sintetičen polimer, ki ga je možno prilepiti na lokacijo topične aplikacije, in pri čemer je metilfenidat prisoten v količini od 20-180 mg metilfenidata na približno 2 do približno 60 cm2 z intenziteto doziranja od 0,5 do 100 mg/24 h, bolj prednostno od
2,5 do 20 mg/24 h, kar se odraža v vsebnostih metilfenidata v krvi, ki srednje vrednosti v ustaljenem stanju doziranja skozi pacientovo kožo ali sluznico v časovnem obdobju vsaj 10 ur ne presegajo za več kot 40%, in pri čemer, kadar polimer predstavlja akrilni polimer, sredstvo obsega največ 5 ut. % funkcionalnih kislinskih monomerov glede na maso akrilnega polimera.
2. Sredstvo po zahtevku 1, pri čemer se metilfenidat nahaja v obliki baze.
3. Sredstvo po zahtevku 1, pri čemer se metilfenidat nahaja v obliki kombinacije baze/bazične soli ali estra.
4. Sredstvo po zahtevku 1, pri čemer metilfenidat obsega pretežno enantiomer ά-threo- metilfenidata.
5. Sredstvo po zahtevku 1, pri čemer je naraven ali sintetičen polimer, ki ga je možno prilepiti na vsakokratno lokacijo topične uporabe, izbran iz skupine, ki sestoji iz akrilov, naravne in sintetične gume, bioadhezijskih sredstev, polisiloksanov, poliakrilatov, polivinilpirolidonov, kopolimerov vinilpirolidonov, blok polimerov stirena ter zmesi le-teh.
6. Sredstvo po zahtevku 5, pri čemer naraven ali sintetičen polimer, ki ga je možno prilepiti na vsakokratno lokacijo topične uporabe, vključuje bioadhezijsko sredstvo, izbrano iz skupine, ki sestoji iz naravnih ali umetnih polisaharidov in polimerov poliakrilnih kislin.
7. Sredstvo po zahtevku 6, pri čemer naravni polisaharid predstavlja naravna guma.
8. Sredstvo po zahtevku 5, pri čemer naraven ali sintetičen polimer, ki ga je možno prilepiti na vsakokratno lokacijo topične uporabe, vključuje polisiloksan, ki je nasičen ali amino-kompatibilen polimer polisiloksana.
9. Sredstvo po zahtevku 5, pri čemer naraven ali sintetičen polimer, ki ga je možno prilepiti na vsakokratno lokacijo topične uporabe, vključuje akril, ki je nefunkcionalen ali hidroksi-funkcionalen ali kar najmanj kislinsko funkcionalen polimer z največ 5 ut. % kislinsko funkcionalnih monomerov glede na maso akrilnega polimera.
10. Sredstvo po zahtevku 5, pri čemer naraven ali sintetičen polimer, ki gaje možno prilepiti na vsakokratno lokacijo topične uporabe, vključuje poliakrilat, ki je polimer brez vsebnosti vinil acetata.
11. Sredstvo po zahtevku 1, pri čemer se doziranje v kožo ali sluznico vrši v časovnem obdobju od približno 12 ur do približno 20 ur.
12. Sredstvo po zahtevku 1, pri čemer se doziranje v kožo ali sluznico vrši v časovnem obdobju od približno 14 ur do približno 16 ur.
2C
13. Sredstvo po zahtevku 2, pri čemer je baza metilfenidata v spojini prisotna v količini vsaj 26,4 mg na 10 cm .
14. Uporaba metilfenidata v fleksibilnem končnem sistemu za pripravo zdravila za zdravljenje motenj v zvezi neuravnovešenostjo ter hiperaktivnostnih motenj v zvezi neuravnovešenostjo, pri čemer sistem obsega naraven ali sintetičen polimer, ki gaje možno prilepiti na lokacijo topične aplikacije, in pri čemer je metilfenidat prisoten v količini od 20-180 mg metilfenidata na približno 2 do približno 60 cm z intenziteto doziranja od 0,5 do 100 mg/24 h, bolj prednostno od 2,5 do 20 mg/24 h, kar se odraža v vsebnostih metilfenidata v krvi, ki srednje vrednosti v ustaljenem stanju doziranja skozi pacientovo kožo ali sluznico v časovnem obdobju vsaj 10 ur ne presegajo za več kot 40%, in pri čemer, kadar polimer predstavlja akrilni polimer, sredstvo obsega največ 5 ut. % funkcionalnih kislinskih monomerov glede na maso akrilnega polimera.
15. Sredstvo za topično uporabo metilfenidata, obsegajoče metilfenidat v fleksibilnem končnem sistemu, pri čemer sistem obsega naraven ali sintetičen polimer, ki ga je možno prilepiti na lokacijo topične aplikacije, in pri čemer je metilfenidat prisoten v količini, ki zadostuje za zagotavljanje terapevtsko učinkovite doze pri pacientu v celotnem obdobju 24 ur, pri čemer celotna dozirana količina metilfenidata znaša od 0,5 mg do 100 mg, in pri čemer, kadar polimer predstavlja akrilni polimer, sredstvo obsega največ 5 ut. % funkcionalnih kislinskih monomerov glede na maso akrilnega polimera.
16. Sredstvo po zahtevku 15, pri čemer celotna količina doziranja metilfenidata znaša od 2,5 mg do 20 mg.
17. Sredstvo po zahtevku 15, pri čemer terapevtsko učinkovita doza znaša od 0,05 mg/kg/dan do 1,0 mg/kg/dan.
18. Sredstvo po zahtevku 15, pri čemer terapevtsko učinkovita doza znaša od 0,075 mg/kg/dan do 0,3 mg/kg/dan.
19. Uporaba metilfenidata v fleksibilnem končnem sistemu za pripravo zdravila za zdravljenje motenj v zvezi neuravnovešenostjo ter hiperaktivnostnih motenj v zvezi neuravnovešenostjo, pri čemer sistem obsega naraven ali sintetičen polimer, ki gaje možno prilepiti na lokacijo topične aplikacije, in pri čemer je metilfenidat prisoten v količini, ki zadostuje za dovajanje terapevtsko učinkovite doze pacientu preko celotnega obdobja 24 ur, pri čemer celotna količina doziranja metilfenidata znaša od 0,5 mg do 100 mg, in pri čemer, kadar polimer predstavlja akrilni polimer, sredstvo obsega največ 5 ut. % funkcionalnih kislinskih monomerov glede na maso akrilnega polimera.
20. Sredstvo po zahtevku 16, pri čemer terapevtsko učinkovita doza znaša od 0,05 mg/kg/dan do 1,0 mg/kg/dan.
21. Sredstvo po zahtevku 16, pri čemer terapevtsko učinkovita doza znaša od 0,075 mg/kg/dan do 0,3 mg/kg/dan.
22. Sredstvo po zahtevku 1 ali po zahtevku 15, pri čemer, kadar polimer predstavlja akrilni polimer, spojina obsega največ 1 ut. % funkcionalnih kislinskih monomerov glede na maso akrilnega polimera.
£
23. Sredstvo po zahtevku 14 ali po zahtevku 19, pri čemer, kadar polimer predstavlja akrilni polimer, spojina obsega največ 1 ut. % funkcionalnih kislinskih monomerov glede na maso akrilnega polimera.
SI9820083A 1997-12-15 1998-12-14 Sredstva in metode za zdravljenje motenj v zvezi z neuravnovešenostjo ter hiperaktivnih motenj v zvezi z neuravnovešenostjo s pomočjo metilfenidata SI20360B (sl)

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US6951097P 1997-12-15 1997-12-15
US09/163,351 US6210705B1 (en) 1997-12-15 1998-09-30 Compositions and methods for treatment of attention deficit disorder and attention deficit/hyperactivity disorder with methylphenidate
PCT/US1998/026560 WO1999030694A2 (en) 1997-12-15 1998-12-14 Compositions and methods for treatment of attention deficit disorder and attention deficit/hyperactivity disorder with methylphenidate

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SI20360A SI20360A (sl) 2001-04-30
SI20360B true SI20360B (sl) 2008-06-30

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US6348211B1 (en) 2002-02-19
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JP2013056944A (ja) 2013-03-28
KR100633348B1 (ko) 2006-10-16
NO329974B1 (no) 2011-01-31
CZ305817B6 (cs) 2016-03-23
PE20000120A1 (es) 2000-02-19
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TW200406231A (en) 2004-05-01
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BR9814282A (pt) 2000-10-03
LV12558B (en) 2001-03-20
PL195315B1 (pl) 2007-08-31
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US6210705B1 (en) 2001-04-03
CA2315237A1 (en) 1999-06-24
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LV12558A (lv) 2000-11-20
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