SI3189830T1 - Formulacija zdravila z zakasnjenim sproščanjem - Google Patents

Formulacija zdravila z zakasnjenim sproščanjem Download PDF

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SI3189830T1
SI3189830T1 SI201331070T SI201331070T SI3189830T1 SI 3189830 T1 SI3189830 T1 SI 3189830T1 SI 201331070 T SI201331070 T SI 201331070T SI 201331070 T SI201331070 T SI 201331070T SI 3189830 T1 SI3189830 T1 SI 3189830T1
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formulation
polymeric material
delayed release
core
coating
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SI201331070T
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Gonzalez Roberto Carlos Bravo
Thomas Buser
Frederic Jean-Claude Goutte
Abdul Waseh Basit
Felipe Jose Oliveria Varum
Ana Cristina Freire
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Tillotts Pharma Ag
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Application filed by Tillotts Pharma Ag filed Critical Tillotts Pharma Ag
Publication of SI3189830T1 publication Critical patent/SI3189830T1/sl

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    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
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    • A61K31/616Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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    • A61K9/288Compounds of unknown constitution, e.g. material from plants or animals
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Claims (15)

  1. FORMULACIJA ZDRAVILA Z ZAKASNJENIM SPROŠČANJEM Patentni zahtevki
    1. Formulacija zdravila z zakasnjenim sproščanjem za peroralno dajanje za dovajanje zdravila v kolon osebka, pri čemer formulacija obsega: jedro in oblogo za jedro, pri čemer jedro obsega zdravilo in obloga obsega zunanji sloj in notranji sloj, pri čemer zunanji sloj obsega zmes prvega polimernega materiala, ki je dovzeten za napade bakterij v kolonu, in drugega polimernega materiala, ki ima mejo pH pri pH 6 ali višje in pri čemer notranji sloj obsega tretji polimerni material, ki je neionski polimer, ki je topen v črevesni tekočini ali gastrointestinalni tekočini, in vsaj en aditiv, izbran izmed pufrskega sredstva in baze.
  2. 2. Formulacija zdravila z zakasnjenim sproščanjem po zahtevku 1, pri čemer je neionski polimer izbran izmed metilceluloze (MC); hidroksipropilceluloze (HPC); hidroksipropilmetilceluloze (HPMC); poli(etilenoksid)-graft-polivinilalkohola; polivinilpirolidona (PVP); polietilen glikola (PEG); in polivinilalkohola (PVA).
  3. 3. Formulacija zdravila z zakasnjenim sproščanjem po zahtevku 1 ali zahtevku 2, pri čemer notranji sloj obsega vsaj eno pufrsko sredstvo in vsaj eno bazo.
  4. 4. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer je pufer fosfatna sol.
  5. 5. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer je pufer kalijev dihidrogenfosfat.
  6. 6. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer je pufer prisoten v notranjem sloju v količini od 0,1 mas. % do 20 mas. % na osnovi suhe mase tretjega polimernega materiala.
  7. 7. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer je baza hidroksidna baza.
  8. 8. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer je baza natrijev hidroksid.
  9. 9. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer je drugi polimerni material mešanica vsaj dveh polimerov, ki imata mejo pH pri pH 6 ali višje.
  10. 10. Formulacija zdravila z zakasnjenim sproščanjem po katerem koli od predhodnih zahtevkov, pri čemer sta prvi in drugi polimerni material prisotna v zunanjem sloju v razmerju do 60 : 40.
  11. 11. Postopek izdelave formulacije zdravila z zakasnjenim sproščanjem za peroralno dajanje za dovajanje zdravila v kolon osebka po zahtevku 1, pri čemer postopek obsega: tvorjenje jedra, ki obsega zdravilo; oblaganje jedra z uporabo pripravka za notranjo oblogo, ki obsega tretji polimerni material, ki je topen v črevesni tekočini ali gastrointestinalni tekočini, v sistemu topil, da se tvori notranje obloženo jedro, in; oblaganje notranjega obloženega jedra s pripravkom za zunanjo oblogo, ki obsega prvi polimerni material, ki je dovzeten za napad bakterij v kolonu, in drugi polimerni material, ki ima mejo pH pri pH 6 ali višje, v sistemu topil, da se tvori zunanje obloženo jedro, pri čemer je tretji polimerni material neionski polimer in pripravek za notranjo oblogo obsega vsaj en aditiv, izbran izmed pufrskega sredstva in baze.
  12. 12. Postopek po zahtevku 11, pri čemer je sistem topil pripravka za notranjo oblogo vodni.
  13. 13. Postopek po zahtevku 11, pri čemer je tretji polimerni material neionski polimer, pH pripravka za notranjo oblogo je naravnan pred oblaganjem na vsaj 0,5 pH-enote višje od meje pH drugega polimernega materiala.
  14. 14. Postopek po zahtevkih od 11 do 13, pri čemer je pH pripravka za notranjo oblogo naravnan tako, da je od pH 7,5 do pH 10, prednostno od pH 7,5 do pH 8,5, bolj prednostno okoli pH 8.
  15. 15. Postopek po katerem koli od zahtevkov od 11 do 14, pri čemer je baza hidroksid.
SI201331070T 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem SI3189830T1 (sl)

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US201261640217P 2012-04-30 2012-04-30
EP12166110.2A EP2659881B1 (en) 2012-04-30 2012-04-30 A delayed release drug formulation
EP17156227.5A EP3189830B1 (en) 2012-04-30 2013-04-29 A delayed release drug formulation

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SI201231190T SI2659881T1 (sl) 2012-04-30 2012-04-30 Formulacija zdravila z zakasnjenim sproščanjem
SI201331070T SI3189830T1 (sl) 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem
SI201331380T SI2844220T1 (sl) 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem
SI201331640T SI2844222T1 (sl) 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem
SI201331409T SI3278792T1 (sl) 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem

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SI201331640T SI2844222T1 (sl) 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem
SI201331409T SI3278792T1 (sl) 2012-04-30 2013-04-29 Formulacija zdravila z zakasnjenim sproščanjem

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