HRP20161331T1 - Modulatori opioidnih receptora - Google Patents
Modulatori opioidnih receptora Download PDFInfo
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- HRP20161331T1 HRP20161331T1 HRP20161331TT HRP20161331T HRP20161331T1 HR P20161331 T1 HRP20161331 T1 HR P20161331T1 HR P20161331T T HRP20161331T T HR P20161331TT HR P20161331 T HRP20161331 T HR P20161331T HR P20161331 T1 HRP20161331 T1 HR P20161331T1
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- Prior art keywords
- pharmaceutical formulation
- sodium
- salt
- pharmaceutically acceptable
- pharmaceutical
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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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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Claims (22)
1. Farmaceutska dozna formulacija pogodna za oralnu administraciju koja sadrži spoj koji ima strukturu:
[image]
ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač.
2. Farmaceutska dozna formulacija iz patentnog zahtjeva 1, naznačena time što je formulacija čvrsti dozni oblik.
3. Farmaceutska dozna formulacija iz patentnog zahtjeva 2, formulirana kao tableta.
4. Farmaceutska dozna formulacija prema patentnom zahtjevu 3, koja sadrži oko 100 mg spoja koji ima strukturu:
[image]
5. Farmaceutska dozna formulacija prema bilo kojem od patentnih zahtjeva od 1 do 4, naznačena time što farmaceutski prihvatljiv nosač sadrži diluent, vezivo, adheziv, dezintegrator, lubrikant, antiadheziv, glidant, ili njihovu kombinaciju.
6. Farmaceutska dozna formulacija prema patentnom zahtjevu 5, naznačena time što je diluent izabran iz grupe koju čine škrob; laktoza; saharoza; diluenti na bazi saharoze kao što je konditorski šećer, saharoza sa dodatkom 7 do 10 masenih postotaka invertnog šećera, saharoza sa dodatkom oko 3 masena postotka modificiranih dekstrina; saharoza sa dodatkom invertnog šećera, oko 4 masena postotka invertnog šećera, 0.1 do 0.2 masena postotka kukuruznog škroba i magnezij stearata; dekstroza; inozit; manitol; sorbitol; mikrokristalna celuloza; dikalcij fosfat; kalcij sulfat dihidrat; i kalcij laktat trihidrat.
7. Farmaceutska dozna formulacija prema patentnom zahtjevu 5, naznačena time što su vezivo i adheziv izabrani iz grupe koju čine akacija guma; guar guma; tragakant guma; saharoza; želatin; glukoza; škrob; celuloze kao što su metilceluloza, natrij karboksimetilceluloza, etilceluloza, hidroksipropilmetilceluloza, hidroksipropilceluloza; i u vodi topljiva ili disperzibilna veziva kao što je alginska kiselina i njene soli, magnezij aluminij silikat, hidroksietilceluloza, polietilen glikol, polisaharidne kiseline, bentoniti, polivinilpirolidon, polimetakrilati, i preželatinizirani škrob.
8. Farmaceutska dozna formulacija prema patentnom zahtjevu 5, naznačena time što je dezintegrator izabran iz grupe koju čine škrobovi kao što su kukuruzni škrob i krumpirov škrob; natrij škrobni glikolat; preželatinizirani škrobovi kao što je kukuruzni škrob; gline kao što je magnezij aluminij silikat; celuloze kao što je umrežena natrij karboksimetilceluloza i mikrokristalna celuloza; alginati; gume poput agar, guar, rogač, karaja, pektin, i tragakant gume; i umreženi polivinilpirolidon.
9. Farmaceutska dozna formulacija prema patentnom zahtjevu 5, naznačena time što su lubrikant i antiadheziv izabrani iz grupe koju čine stearati kao što su magnezij stearat, kalcij stearat i natrij stearat; stearinska kiselina; talk voskovi; stearovet; borna kiselina; natrij klorid; DL-leucin; carbovax 4000; carbovax 6000; natrij oleat; natrij benzoat; natrij acetat; natrij lauril sulfat; i magnezij lauril sulfat.
10. Farmaceutska dozna formulacija prema patentnom zahtjevu 5, naznačena time što je glidant izabran iz grupe koju čine talk, kukuruzni škrob i silika.
11. Farmaceutska dozna formulacija prema patentnom zahtjevu 5, koja dalje sadrži zaslađivač, aromu, bojilo, oblogu ili njihovu kombinaciju.
12. Farmaceutska dozna formulacija prema bilo kojem od patentnih zahtjeva od 1 do 11 za upotrebu u postupku za liječenje ili ublažavanje poremećaja posredovanog δ ili µ opioidnim receptorima, koji je izabran između bola i gastrointestinalnih poremećaja, pri čemu se postupak sastoji od davanja farmaceutskog preparata subjektu kojem je takav tretman potreban.
13. Farmaceutska dozna formulacija za upotrebu prema patentnom zahtjevu 12, naznačena time što se farmaceutska formulacija administrira sa frekvencijom od jedne do četiri administracije dnevno.
14. Farmaceutska dozna formulacija za upotrebu prema patentnom zahtjevu 12, naznačena time što se farmaceutska dozna formulacija administrira jedanput dnevno.
15. Farmaceutska dozna formulacija za upotrebu prema patentnom zahtjevu 12, naznačena time što se farmaceutska dozna formulacija administrira dva puta dnevno.
16. Farmaceutska dozna formulacija za upotrebu prema bilo kojem od patentnih zahtjeva od 12 do 15 naznačena time što poremećaj predstavlja dijarejni sindrom.
17. Farmaceutska dozna formulacija za upotrebu prema bilo kojem od patentnih zahtjeva od 12 do 15, naznačena time što bol predstavlja visceralni bol.
18. Farmaceutska dozna formulacija za upotrebu prema bilo kojem od patentnih zahtjeva 12-15, naznačena time što poremećaj predstavlja sindrom iritabilnog crijeva sa dominantnom dijarejom.
19. Farmaceutski prihvatljiva sol spoja koji ima strukturu:
[image]
naznačena time što sol predstavlja sol klorovodične, bromovodične, jodovodične, perklorne, sumporne, dušične, fosforne, octene, propionske, glikolne, mliječne, jantarne, maleinske, fumarne, jabučne, tartarne, limunske, benzojeve, bademove, metansulfonske, hidroksietansulfonske, benzensulfonske, oksalne, pamoinske, 2-naftalensulfonske, p-toluensulfonske, cikloheksan-sulfaminske, salicilne, saharinske, trifluoroctene kiseline, benzatina, kloroprokaina, kolina, dietanolamina, etilendiamina, meglumina, prokaina, aluminija, kalcija, litija, magnezija, kalija, natrija ili sol cinka.
20. Farmaceutski prihvatljiva sol prema patentnom zahtjevu 19, naznačena time, što sol predstavlja sol klorovodične, bromovodične, jodovodične, perklorne, sumporne, dušične, fosforne, octene, propionske, glikolne, mliječne, jantarne, maleinske, fumarne, jabučne, vinske, limunske, benzojeve, bademove, metansulfonske, hidroksietansulfonske, benzensulfonske, oksalne, 2-naftalensulfonske, p-toluensulfonske, cikloheksansulfaminske, salicilne, saharinske ili soli trifluoroctene kiseline.
21. Farmaceutski prihvatljiva sol prema patentnom zahtjevu 19, naznačena time, što sol predstavlja sol benzatina, kloroprokaina, kolina, dietanolamina, etilendiamina, meglumina, prokaina, aluminija, kalcija, litija, magnezija, kalija, natrija, ili sol cinka.
22. Kompozicija koja sadrži farmaceutski prihvatljivu sol prema bilo kojem od patentnih zahtjeva od 19 do 21 i farmaceutski prihvatljiv nosač.
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