HUE033133T2 - Metilnaltrexon lipofil sói és azok orális adagolású készítményei - Google Patents

Metilnaltrexon lipofil sói és azok orális adagolású készítményei Download PDF

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HUE033133T2
HUE033133T2 HUE11157837A HUE11157837A HUE033133T2 HU E033133 T2 HUE033133 T2 HU E033133T2 HU E11157837 A HUE11157837 A HU E11157837A HU E11157837 A HUE11157837 A HU E11157837A HU E033133 T2 HUE033133 T2 HU E033133T2
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methylnaltrexone
certain embodiments
composition
formulation
opioid
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HUE11157837A
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English (en)
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Syed M Shah
Christopher Richard Diorio
Eric C Ehrnsperger
Xu Meng
Kadum A Shareffi
Jonathan Marc Cohen
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Wyeth Llc
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Application filed by Wyeth Llc filed Critical Wyeth Llc
Publication of HUE033133T2 publication Critical patent/HUE033133T2/hu

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    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • 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
    • 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
    • A61K9/2009Inorganic compounds
    • 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
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • 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
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08Oxygen atom

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  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
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  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (7)

  1. Ϊ||ί0|1ί sé! Is azok orális «lagollsá készítményei AzoKtdahn igerts vamk 1, 1-gy (!) általános leplem se
    ahol A" ijeíerrtése .ßgy anvil fii, gyógyásmiüag elfogadható segédanyag anionja, amely segéd*: artyág tartalmas agy Äiete egyenes vagy elágazó, gklkos vagy aeikükus, 4*30 szÉmtomoijIÄ osepmáóh 2> Ax L igénypont $máM. só, Ahol a vagy::-if¥esiÄ.
  2. 3. Αχ 1 igénypont szerinti só, ahol a gy*|gf!páiiá|:ÍÍÍÍgaÉ^tó-.:é%|^ai^áiiÄÄ^·. egy szulfát" í"OS();>*} csoportot,
  3. 4, Az 1-3, igénypontok, bármelyike szerinti ΐό>::ΛόΙ -Ά gyègyâszaÂI tlfèpdhatô sagéd-;:^flig::|^|nax''aiy 4-30 szenatomos aetklikusaltfeospprtek^amely adoft ésothsn ssuhszit-tuálva van, 1> Az 1-3. igénypontok bfeneîyike szerinti 1 .»· .gyÔM^f^lfeliÂiedhaiô'Jéiiày < UAa'maz „es I ' szer,atomos *" ,ιΛΊ e-opottot
  4. 6, .Az 1. igénypont szerinti só, ahol A* jelentése dodecü-szulfók ?. Gyógyászati készítmény orális adagoláshoz, amely tartalmaz, egy szilárd doxisalakot, amely tartalmaz (i) (/f)-A-meül-mdaexont vags annak gyógyászati lag elíbgáiltiÉ sl|4k Ik (U.i amísíiL gyógyászat? lag e) lógatható segóJany^g^|^íi:jpp^pdffiM^tet.f|^)váW a kész nmem, ioîjtfs tömegén u>nutku?ta?va, id-7S *'1> nwna>tségben uriakaae tRVVrociil- yllIlKôari
  5. 8, Aétlgénypónt szerinti gyógyászati készítmény» ahol a üfisg· .élfôgÂÂÄig If-at ami ifik gyúgyásxoübg elfogadható séôl^tÂ;;%lôMp^onp{irt bepez. fi: ¾. I. igénypont szerinti gyógyászati készítmény, ahol m, ionpár akkor képződik. ha a meülnaltrexon vagy annak gyógyászatiéig elfogadható sója és az amüfth gyógyászatílag: êlfe-gadható segédanyag kórülMiil had! imgyobh és körülbelül 4óíí| kisebb pH-értékü oldatban kerül íebddtsra« ló. Λ 7-0, igénypontok bármelyiké szerinti gyögyä^zÄÄzÄdöy» aine|r tartalmaz továbbá egy szétesést elősegítő anyagot is. 1 l, A 7-10, igénypontok bármelyike szerinti gyógyászati készítmény, ahol egy 100? pere tbrdulatszámmal üzemelő keverólapáttai ellátón oldatkmltő berendezésben, bOO ml 0.1 N sósavban, 3/ °€«οη. körülbelül 15 perc alatt a készítmény legalább 50 %-MépÍább t$ Wé. vagy legalább 90 9¾-a oldódik teL mÁWl, igénypontok®^ ahol a készlt^te»d»Í Éá 4 közötti pHzn meghatározott, nvetllbáítrexonm vonatkozó oktanol/vtz megoésiásl. hapy^iö§&amp; legalább (ŐS, legalább ÖJ. legalább 10, legalább 20 vagy legalább 30, 13. À 7-12. igénypontok bármelyike szerinti készítmény*.abit a keszihppsy taridlmaz egy (1) igénypont szerinti vegyületet
    ahol A: jelentése az amílfll gy|gy|szgtll|g ellígndhai© segédanyag anionja. !4i! A 10-13, igénypontok bármelyiké szerinti készítmény, ahol a szétesést elősegítő anyag egy etïerveszeens szétesést elősegíti anyag, például uidrogén-karhooát vagy nátrium*· hidrogén - krehonlí, 15, Λ 7-14. igénypontok bármelyike szerinti készítmény, ahol a készltmlöf §gy tabletta. lii M· 7*1S. igénypontok bárnieiyike szerinti készítmény, ahol a készítmény egy tabletta, amely tartalmaz legalább egy vagy több kötőanyag#!, kdátképaöt nedvesítésben, lobrikÉisl. mm funkcionális buvmmanyapf vagy ηιρ|ρΜ|Ιρ§Ιte ezek kombinációit 17, A 16. igénypont szerinti készítmény, ahol a késauruény amalmaz egy ke lat képzőt, tsiihi például EDTA-t vagyillnalíllíifsipéyáal kaÍdi®^nátmmt-EDTA-t. fl, A. 16. |g|sypotátszdjlití klagltdilhyyahó! á teMtriÄy ltitókán||: péf^· dini mapMnp-szmaráton 19. A 16. -sa^íírégl:! :-?Öfesil !:©! laïlÎââicfeÊÈK ísjg^; példán! aszkmbmsáfik 20. A 7" 19, igénypontok bármelyike szerinti készítmény optoMM. ;^ép Itrápk Ê&amp; vagy több mellékhatásának kezelésére páciensben Âénê'.alkalmse^^. 21. Λ 20. igénypont szerinti készitthiny Ä!ig#»yblt alkalmiéira» áltól a igepkhatások a következők közül % annak kiválasztva: bélmezgás gátoltllg%.p^por-b^mné§^ri,:It^tntá^ pl|í : szlIrskeáéÉi eslkkéní ÍilmoéiÍá> Mliliáfódás,, a gyomét feliááii mözg|Ms: gpMor-béhend&amp;Zfri sziinkter-szükület. tokozott sminlÂibimtôons,. fÿ^M^iMii^^kêoiSgàs-képesség gàkriMga, gyamot; kiütésének gitolíMga, liilÄtolt: igpmprilríté^ fildéges székletürítés, hányiftgér, hápy% bdrpír, puffadás, has! felfúv<|l% vere|tikezéss diszfeí% vrizketegseg és vizdelrekedés.
  6. 22. Eljárás aánloaltrexon-készfttnény előállításira, amely magiban foglalta a kovotkezo lépéseket: nretíinálÉpfönt vagy aondl gyogyászatlkg dfegapali ÉfÉtéá - aniíil, gyé|yásgaíi!á| elfogadható segédanyagként uitrhun-dodeeibszultatot ξ8Π81, valumiut legalább egy széle-ééardisegM anyepi, legalább égy kötőanyagot, legalább egy koláképzp, legalább egy Má~ vMiiMd% és adott esetben legalább «..gy töltőanyagot tartól mazo neches granulátum koszáé* se; és szilárd dèzissgvség kialakítása.
  7. 23. Többrsapus csumng, amet}- *dbb. ij^nypoatok hámsdyike szériát! egysêgdôzis- Mazltmérsv-í tartalmaz.· 24, A '7, igánv'pörg szförídti nyégyászitl kálzltrífesg ataëly a 22, ipdypppi szertptf elfá* fással lelt előállítva.
HUE11157837A 2010-03-11 2011-03-11 Metilnaltrexon lipofil sói és azok orális adagolású készítményei HUE033133T2 (hu)

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