HUE032963T2 - Fejlesztett stabilitású (Z)-2-ciano-3-hidroxi-but-2-énsav-(4'-trifluormetilfenil)-amid tabletta formuláció - Google Patents
Fejlesztett stabilitású (Z)-2-ciano-3-hidroxi-but-2-énsav-(4'-trifluormetilfenil)-amid tabletta formuláció Download PDFInfo
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- HUE032963T2 HUE032963T2 HUE10752585A HUE10752585A HUE032963T2 HU E032963 T2 HUE032963 T2 HU E032963T2 HU E10752585 A HUE10752585 A HU E10752585A HU E10752585 A HUE10752585 A HU E10752585A HU E032963 T2 HUE032963 T2 HU E032963T2
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- solid pharmaceutical
- pharmaceutical composition
- sodium
- teriflunomide
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Claims (3)
- Szabadalmi igénypontok ! . Szilárd gyögyszeréSzétii készíttpltty, atíiély alapvétőéit aíkövetkezőkM|:öik a) 1-30 tömeg% TenSlünormd vagy gyirgyszerészeiilegedlopadhntó bazisaodicios; soja. b t 5-20 tömeg'?·..· szétesést elősegítő s/er, c) 0-40 tömeg9» kötőanyag, d) ‘U -1 tömeg% keimany ag, es e! a íéánmaradó »zúzalékban fngito szerek,: azzal a: nrégkôtép;el Hogy a. vdsáru gyógyszeres/eti készítmény nem tartalmaz kolloid szilícium- diós időt. 2 Aï 1. igénypont szetinn szilárd gyógyszerészeti készítmény, ahoi n szétesést «lôsegiix* m& a kővetkezők »Ikoha samponból választott: katbosítnetfr-eellöl&K. alacsony sztibssaitnt'iós fokú hídroxíproptj* cellulóz. miktokrisiályos ceiiuioz. porított ieiinlóz. kroszKamidióz-nátri uro. metilceiUdóz, pcdakfiHm kálium, nátnunr-aiginat. nátrium-kemény nö-gilkolát vagy ezen szétesést elősegítő ingerek közűi egynek vagy többnek a keveréké. 2. igénypont vetmti „-/dard gsm/woies/v'i k zu may, uuőí a s/eteséd elósemto \/m a kbvéíHé&ÖK"·$}$$#<$& aiitósőny szirbsztínkiős íbkvf ibidrökipfiöikiikoiidlök« töikök:fistáiyös 0001:10/. porított cellulóz, kroszkarmeíKiz-oátriutn. nátrium· kenumyito-glikolat vagy ezen s/étestHt elősegítő szerek közűi egynek vagy többnek a keveréke. 4 Az ! igen'pun svernn ,ztl.it,. g« v ve _ ,xő kész imáin a ml » kofoanvu v, voxetkczok tikon a csoportból váíssztpi:: arab mézga, kanxomietil-celiuióz, iyidroxietdvceíiuléz, iudrpsifvropIl-cdMdz, dextrin, zselaun, gnarguroi, bilroxípnspjj-métii-ceiUtlóz, tnaiíöiextrit), méííleéíiíűdz, náírmm-aigináí. éíögéiesbstt keményítő, búr go n y a kérne ny i tő. kukoricakernenvitö vagy gabonakemény iío és zein vagy ezen kötőanyagok köztit egynek vagy többnek a keveréke. 1 Λ 4. igénypont szerinti sxilárd gyógyszerészeti készítmény, aho! a kötőanyag a következők alkotta csoportból választott: bidroxtpropii eeiluloz, hidroxipropii-metií eeiiidó/.. eiögélesstetí keményítő, borgonyakeményitbv : ktfköricakéiöényitö vi^k pbőnakeményitö vagy ezé«: kötőanyagok közűi egynek vágy többnek a kévéteké. tÄl. ígértyporit szerintt szilárd gyógyszerészeti készítmény. ahoi a kenőanyag a kővetkezők alkotta csoportból választott: kalemm-sztearát. giieetil-palmitosztearáí. nátninn-henzoát, nátrmmdauribsxuíiáű nátrium-sztöatibbirnarák χ/ieat msas. talkum emk ;h sa* es magnézium-./to not s tgs ezen .venoanyazok közűi egyistk vagy többnek a keveréke. 7. Λ 6. igénypont s/wimi szilárd gyögyszerészcu késziímérty, ahol a kenőanyag a következők alkotta rsitpopboj \Jwiou naürnri-Okuní-hrtarm es magnézium s/teamt vagy ezen Kenőanyagok i-o/u) egynek vagy többnek a keveréke. 8. Λ/ I. igénypont szerinti szilárd gyögyxzcres/ai készítmény, ahoi a highöszer a kővetkezők alkotta csoportból válaszúm: cellulóz, edkiioz-zteemt. dcMrátok. derbin. dextrőz, Intkső/. S ·0·«··ί>mHSkopícsnozíl-D- , rmmnit, :..giMëôfe|j&im^èi^eâ0k ;hîdïUigérsôijçit. növényi olaj, kaolin. laki it. iakrőz. kdnOz· mouobidrát. maliit, mannft. maímdexmn, mrkoz, docdcstíett kemény do, naumm-klorki, szorbit, kernénystoL szacharóz íaikttm es csitt vagy ezen higitós/crek közül egynek vagy többnek a keveréke c>. Λ 8. igénypont szerint· szilárd gyógyszerészeti készítmény. ahol a hlgttószer a következők alkotta csopóttMii: választón: laktőz, manntf os keft|ényós|ik vágy tízen IdgltóSZPék közül egynek vagy többnek a keveréke. iö. Az előző Igéoypobtok iblrtópíslkdí szzírintj szilárd ^f6g$>;szssre,sÄ Mszltmény,. .áhal a késdíméfty· bevonaaoit. ! I. A ’ő. igénypont szerinti szilárd gyógyszerészeti készítmény·. amely tabletta vagy pirula hiprornellő/ alapú bevonnom!
- 12. Az előző igénypontok bármelyike szeri!«: szilárd ttyőgjszereszeti készítmény. arndy alapvetően a következőkbe; áll: {a.i 2- í 5 UVmcgb« Teri fi tmotnid, PT mikrokristályos ed Időz vagy ttätriitm-kemeityltö-gbfeotat kőzíSÍ választott egy vagy több szétesést élösgfitŐ szét Aie ;öwegw<> ntcmvyAégben, (e) a itidrosiptxip 11,Ve11ttIóz vagy kukoncakemdiyitö közül választott egy vagy több kötőanyag IMS törneg% mennyiségben. tdKU I 0 tömey0,· keno.mve·.'. <mt öv a nsagneztmnsztearáí. és te) á fennntataek) százalékban higitó szer, amely a iaktóz-mnneshidrát:,
- 13. Az 1-12. igénynoiuak bármely tkc széna ti szilárd gyógyszerészet; készítmény a: következők kezdésében történő alkalmazásra: szepszis. allergia, graft-versus-host-reakc sók, host-verstts-graft-reaktiók. reumás izületi gyulladás, szisztémás Isums erythematosus, sclerosis multiplex, pikkelysömör, asztma, csalánkiütés:. rhifvttts, nvdíiá,: tüdöráki: ieokbirttá;: pgpféágékfák, szarkohm, SkájSostákkárköpa. soenmgtőrna, belrák, oytroKesomo-rák, agydagnaatok, emlőrák, hasttyáhrnrigyrák, prosztatarák vagy bőrrák.
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Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA115979C2 (uk) * | 2009-09-18 | 2018-01-25 | Санофі | Таблетований препарат (4'-трифторметилфеніл)аміду (z)-2-ціано-3-гідроксибут-2-еноєвої кислоти з поліпшеною стійкістю |
| RU2493845C1 (ru) * | 2012-06-07 | 2013-09-27 | Общество с ограниченной ответственностью "ВАЛЕНТА ИНТЕЛЛЕКТ" | Композиция для лечения рассеянного склероза (варианты) |
| CA2930429A1 (en) * | 2013-11-22 | 2015-05-28 | Genzyme Corporation | Novel methods for treating neurodegenerative diseases |
| CN103656657A (zh) * | 2013-12-18 | 2014-03-26 | 北京科源创欣科技有限公司 | 特立氟胺药物组合物及制备方法 |
| WO2015144804A1 (en) | 2014-03-26 | 2015-10-01 | Astex Therapeutics Ltd | Combinations |
| US20160058730A1 (en) * | 2014-08-29 | 2016-03-03 | Cadila Healthcare Limited | Pharmaceutical compositions of teriflunomide |
| WO2016079687A1 (en) * | 2014-11-18 | 2016-05-26 | Lupin Limited | Oral pharmaceutical composition of teriflunomide |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
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| CA2996632C (en) * | 2015-09-01 | 2023-10-17 | Bayer Pharma Aktiengesellschaft | Compounds and methods useful for treating or preventing hematological cancers |
| WO2017037645A1 (en) * | 2015-09-02 | 2017-03-09 | Leiutis Pharmaceuticals Pvt Ltd | Stable pharmaceutical formulations of teriflunomide |
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| WO2017125841A1 (en) * | 2016-01-20 | 2017-07-27 | Emcure Pharmaceuticals Limited | Pharmaceutical compositions of teriflunomide |
| JOP20190207A1 (ar) | 2017-03-14 | 2019-09-10 | Actelion Pharmaceuticals Ltd | تركيبة صيدلانية تشتمل على بونيسيمود |
| PL3999038T3 (pl) * | 2019-07-17 | 2024-05-13 | Cytokinetics, Inc. | Preparaty doustne inhibitora sarkomerów sercowych |
| EP4178548B1 (en) * | 2020-07-07 | 2024-07-24 | Celgene Corporation | Pharmaceutical compositions comprising (s)-4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)m ethyl) benzyl)piperazin-1-yl)-3-fluorobenzonitrile and methods of using the same |
| WO2022085015A1 (en) * | 2020-10-24 | 2022-04-28 | V-Ensure Pharma Technologies Private Limited | A solid oral composition of teriflunomide |
| GR1010137B (el) | 2020-12-15 | 2021-12-07 | Φαρματεν Α.Β.Ε.Ε., | Στερεη φαρμακοτεχνικη μορφη αμεσης αποδεσμευσης περιεχουσα τεριφλουνομιδη και μεθοδος παρασκευης αυτης |
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Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3852294A (en) * | 1968-08-27 | 1974-12-03 | Merck Patent Gmbh | Bis-quaternary pyridinium salts |
| US5268382A (en) | 1985-09-27 | 1993-12-07 | Hoechst Aktiengesellschaft | Medicaments to combat autoimmune diseases, in particular systemic lupus erythematosus |
| DE3534440A1 (de) | 1985-09-27 | 1987-04-02 | Hoechst Ag | Arzneimittel gegen chronische graft-versus-host-krankheiten sowie gegen autoimmunerkrankungen, insbesondere systemischen lupus erythematodes |
| US6133301A (en) | 1991-08-22 | 2000-10-17 | Aventis Pharma Deutschland Gmbh | Pharmaceuticals for the treatment of rejection reactions in organ transplantations |
| US5700823A (en) | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| GB9408117D0 (en) * | 1994-04-23 | 1994-06-15 | Smithkline Beecham Corp | Pharmaceutical formulations |
| AU695907B2 (en) | 1994-10-17 | 1998-08-27 | Hoechst Pharmaceuticals & Chemicals K.K. | Pharmaceutical composition for prophylaxis and treatment of type I allergic diseases |
| ATE207065T1 (de) | 1997-08-08 | 2001-11-15 | Aventis Pharma Gmbh | Kristallform von n-(4-trifluormethylphenyl)-5- methylisoxazol-4-carbonsäureamid |
| US6248363B1 (en) * | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| EP1257270B1 (en) | 2000-02-15 | 2005-04-13 | Teva Pharmaceutical Industries Ltd. | A method for synthesizing leflunomide |
| DE60226855D1 (de) | 2001-04-05 | 2008-07-10 | Aventis Pharma Inc | Verwendung von (z)-2-cyano-3-hydroxy-but-2-ensäure-(4'-trifluoromethylphenyl)-amid zur behandlung der multiplen sklerose |
| GB0123571D0 (en) * | 2001-04-05 | 2001-11-21 | Aventis Pharm Prod Inc | Use of (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-amide for treating multiple sclerosis |
| US20050158371A1 (en) | 2002-02-12 | 2005-07-21 | Sumitomo Pharmaceuticals Co., Ltd. | Novel external agent |
| WO2005023185A2 (en) * | 2003-08-29 | 2005-03-17 | Transform Pharmaceuticals, Inc. | Pharmaceutical compositions and method of using levodopa and carbidopa |
| GB2394660A (en) | 2003-12-17 | 2004-05-05 | Niche Generics Ltd | Stabilisation of pharmaceutical compositions comprising ACE inhibitor by absence of acidic excipients having large specific surface area, eg silicon dioxide |
| US20050220874A1 (en) * | 2004-04-02 | 2005-10-06 | Chien-Hsuan Han | Pharmaceutical dosage forms having immediate release and controlled release properties that contain a GABAB receptor agonist |
| US20060024376A1 (en) * | 2004-07-30 | 2006-02-02 | The University Of Chicago | Methods and compositions for reducing toxicity associated with leflunomide treatment |
| AU2005295511A1 (en) * | 2004-10-19 | 2006-04-27 | Aventis Pharmaceuticals Inc. | Use of (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-amide for treating inflammatory bowel disease |
| TWI275029B (en) * | 2005-11-18 | 2007-03-01 | Hon Hai Prec Ind Co Ltd | An embedded system and method for processing data thereof |
| CA2637925A1 (en) | 2006-01-24 | 2007-08-02 | Teva Pharmaceutical Industries Ltd. | Levetiracetam formulations and methods for their manufacture |
| DE102006017896A1 (de) | 2006-04-13 | 2007-10-25 | Tiefenbacher Pharmachemikalien Alfred E. Tiefenbacher Gmbh & Co. Kg | Leflunomid enthaltende pharmazeutische Zusammensetzungen |
| EP1990048A3 (en) | 2007-05-08 | 2009-05-06 | Ulrike Wiebelitz | Therapy of benign prostatic hyperplasia (bph) |
| UA115979C2 (uk) * | 2009-09-18 | 2018-01-25 | Санофі | Таблетований препарат (4'-трифторметилфеніл)аміду (z)-2-ціано-3-гідроксибут-2-еноєвої кислоти з поліпшеною стійкістю |
| EP2762135A1 (en) * | 2013-02-04 | 2014-08-06 | Sanofi | Methods for reducing the risk of an adverse teriflunomide and rosuvastatin interaction in multiple sclerosis patients |
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