HRP20100159T1 - Upotreba hidrofilnog matriksa koji se sastoji od derivata poliakrilne kiseline, celuloznog etera i sredstva za raspadanje u proizvodnji medikamenta za liječenje ženskih genitalnih poremećaja - Google Patents

Upotreba hidrofilnog matriksa koji se sastoji od derivata poliakrilne kiseline, celuloznog etera i sredstva za raspadanje u proizvodnji medikamenta za liječenje ženskih genitalnih poremećaja Download PDF

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HRP20100159T1
HRP20100159T1 HR20100159T HRP20100159T HRP20100159T1 HR P20100159 T1 HRP20100159 T1 HR P20100159T1 HR 20100159 T HR20100159 T HR 20100159T HR P20100159 T HRP20100159 T HR P20100159T HR P20100159 T1 HRP20100159 T1 HR P20100159T1
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use according
polyacrylic acid
starches
matrix
disintegrant
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HR20100159T
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De Luigi Bruschi Stefano
Mailland Federico
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Polichem S.A.
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    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
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    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K9/0034Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • A61K9/0039Devices retained in the uterus for a prolonged period, e.g. intrauterine devices for contraception
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • AHUMAN NECESSITIES
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    • A61P31/12Antivirals
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis

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Abstract

Upotreba hidrofilnog matriksa koji se sastoji od: a) najmanje jednog derivata poliakrilne kiseline, u količini od 0,5-40 % s obzirom na težinu matriksa; b) najmanje jednog celuloznog etera; ic) najmanje jednog sredstva za raspadanje; te od najmanje jednog farmaceutski prihvatljivog aktivnog principa, naznačena time što je navedeni hidrofilni matriks namijenjen proizvodnji formulacije za liječenje ženskih genitalnih poremećaja, gdje najmanje jedno sredstvo za raspadanje se bira između modificiranih celuloza, poput umrežene natrij-karboksimetilceluloze, umreženog polivinilpirolidona, poput krospovidona, prirodnih škrobova, poput kukuruznog škroba, krumpirovog škroba, izravno kompresibilnih škrobova, modificiranih škrobova, poput karboksimetilškrobova i natrij-karboksimetilškroba, škrobnih derivata, poput amiloze, alginske kiseline i natrijevog alginata, mikrokristalne celuloze, te gdje navedeni ženski genitalni poremećaji su hipotrofija spolnih organa, atrofija spolnih organa, gubitak elastičnosti spolnih organa, suhoća rodnice, infekcije vrata maternice i/ili rodnice uzrokovane gljivicama, bakterijama, protozoama ili virusima. Patent sadrži još 21 patentni zahtjev.

Claims (22)

1. Upotreba hidrofilnog matriksa koji se sastoji od: a) najmanje jednog derivata poliakrilne kiseline, u količini od 0,5-40 % s obzirom na težinu matriksa; b) najmanje jednog celuloznog etera; i c) najmanje jednog sredstva za raspadanje; te od najmanje jednog farmaceutski prihvatljivog aktivnog principa, naznačena time što je navedeni hidrofilni matriks namijenjen proizvodnji formulacije za liječenje ženskih genitalnih poremećaja, gdje najmanje jedno sredstvo za raspadanje se bira između modificiranih celuloza, poput umrežene natrij-karboksimetilceluloze, umreženog polivinilpirolidona, poput krospovidona, prirodnih škrobova, poput kukuruznog škroba, krumpirovog škroba, izravno kompresibilnih škrobova, modificiranih škrobova, poput karboksimetilškrobova i natrij-karboksimetilškroba, škrobnih derivata, poput amiloze, alginske kiseline i natrijevog alginata, mikrokristalne celuloze, te gdje navedeni ženski genitalni poremećaji su hipotrofija spolnih organa, atrofija spolnih organa, gubitak elastičnosti spolnih organa, suhoća rodnice, infekcije vrata maternice i/ili rodnice uzrokovane gljivicama, bakterijama, protozoama ili virusima.
2. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedeno najmanje jedno sredstvo za raspadanje je umrežena natrij-karboksimetilceluloza.
3. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedeni najmanje jedan derivat poliakrilne kiseline dolazi u količinama od 2-40 %, po mogućnosti 2-30 %, navedeni najmanje jedan celulozni eter dolazi u količinama od 30-90 %, a navedeno najmanje jedno sredstvo za raspadanje dolazi u količinama od 2-50 %, s obzirom na težinu matriksa.
4. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedeni najmanje jedan derivat poliakrilne kiseline dolazi u količinama od 1-20 %, navedeni najmanje jedan celulozni eter dolazi u količinama od 40-80 %, a navedeno najmanje jedno sredstvo za raspadanje dolazi u količinama od 5-40 %, s obzirom na težinu matriksa.
5. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedeni najmanje jedan derivat poliakrilne kiseline je poliakrilna kiselina umrežena s polialkenil-eterima šećera ili polialkohola, po mogućnost s karbomerom.
6. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedeni najmanje jedan derivat poliakrilne kiseline je poliakrilna kiselina umrežena s divinil-glikolom, po mogućnosti s polikarbofilom.
7. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedeni najmanje jedan celulozni eter se bira između hidroksilakilceluloze, alkilceluloze, karboksimetilceluloze ili njezine soli.
8. Upotreba u skladu s patentnim zahtjevom 7, naznačena time što navedenu hidroksilakilcelulozu se bira između hidroksipropilmehilceluloze, hidroksilpropilceluloze i hidroksiehilceluloze; i/ili navedenu alkilcelulozu se bira između metilceluloze i etilceluloze.
9. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što navedena formulacija je čvrsta.
10. Čvrsta formulacija u skladu s patentnim zahtjevom 9, naznačena time što navedeni matriks je prisutan u količini od otprilike 5-60 %, po mogućnosti 20-40 %, a navedeni najmanje jedan aktivni princip u količinama od otprilike 2-70 %, po mogućnosti 5-50 %, s obzirom na težinu matriksa.
11. Upotreba u skladu s patentnim zahtjevom 9, naznačena time što uključuje farmaceutski prihvatljiva punila, pomoćne tvari i/ili adjuvanse.
12. Upotreba u skladu s patentnim zahtjevom 9, naznačena time što navedeni najmanje jedan aktivni princip se bira između antimikotika, antibiotika, antivirusnih, antimikrobnih sredstava ili kemoterapeutika i hormona.
13. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što navedeni antimikotik se bira između hidroksi-2-piridonskih spojeva, imidazolskih derivata, polienskih derivata, alilaminskih derivata, triazolskih derivata, morfolinskih derivata, grizeofulvinskih spojeva, kiselih spojeva, tolnaftata, flucitozina i njihovih soli.
14. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što navedeni antimikotik je ciklopiroks ili ciklopiroks olamin.
15. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što navedeni antibiotik ili antimikrobno sredstvo se bira između aminoglikozida, tetraciklina, makrolida, kinolona, sulfonamida samih ili u kombinaciji s diaminopiridinima, penicilinskih spojeva, cefalosporina i drugih β-laktamskih antibiotika, linkozamida, antiprotozoika, antibakterijskih sredstava, antiseptika i njihovih soli.
16. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što navedeni antibiotik se bira između nifuratela, metronidazola, tinidazola, klindamicina.
17. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što navedeno antivirusno sredstvo se bira između idoksuridina, aciklovira, penciklovira, podofilotoksina ili imikvimoda.
18. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što navedeni hormon se bira između estradiola, ethinilestradiola, estriola, promestriena, hidroksiprogesterona, progesterona, medroksiprogesterona, dihidrogesterona, nomegestrola, noretisterona, tibolona, testosterona, prasterona, mesterolona ili bilo kojeg fitoestrogena.
19. Upotreba u skladu s patentnim zahtjevom 11, naznačena time što navedenu pomoćnu tvar se bira između askorbinske kiseline, mliječne kiseline i njihovih soli.
20. Upotreba u skladu s patentnim zahtjevom 9, naznačena time što navedena čvrsta formulacija je tableta, po mogućnosti bioadhezivna tableta.
21. Upotreba u skladu s patentnim zahtjevom 9, naznačena time što navedena čvrsta formulacija je formulacija s kontroliranim otpuštanjem.
22. Upotreba u skladu s patentnim zahtjevom 9, naznačena time što navedenu čvrstu formulaciju se primjenjuje u šupljinu rodnice.
HR20100159T 2006-06-29 2010-03-18 Upotreba hidrofilnog matriksa koji se sastoji od derivata poliakrilne kiseline, celuloznog etera i sredstva za raspadanje u proizvodnji medikamenta za liječenje ženskih genitalnih poremećaja HRP20100159T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06116269A EP1872775A1 (en) 2006-06-29 2006-06-29 Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders
PCT/EP2007/056185 WO2008000683A1 (en) 2006-06-29 2007-06-21 Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders

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US (1) US8865201B2 (hr)
EP (2) EP1872775A1 (hr)
JP (1) JP5205374B2 (hr)
KR (1) KR101443149B1 (hr)
CN (2) CN101478951A (hr)
AR (1) AR061771A1 (hr)
AT (1) ATE455534T1 (hr)
BR (1) BRPI0713298A2 (hr)
CA (1) CA2652226C (hr)
CO (1) CO6140022A2 (hr)
CY (1) CY1109910T1 (hr)
DE (1) DE602007004486D1 (hr)
DK (1) DK2032123T3 (hr)
EA (1) EA018257B1 (hr)
ES (1) ES2339069T3 (hr)
HK (1) HK1128587A1 (hr)
HR (1) HRP20100159T1 (hr)
MA (1) MA30597B1 (hr)
MX (1) MX2008016508A (hr)
NO (1) NO20090095L (hr)
PL (1) PL2032123T3 (hr)
PT (1) PT2032123E (hr)
RS (1) RS51279B (hr)
SI (1) SI2032123T1 (hr)
WO (1) WO2008000683A1 (hr)

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CN101478951A (zh) 2009-07-08
EP1872775A1 (en) 2008-01-02
CO6140022A2 (es) 2010-03-19
EA018257B1 (ru) 2013-06-28
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EP2032123A1 (en) 2009-03-11
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US20110091555A1 (en) 2011-04-21
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