HUE030048T2 - Új VI kristályos formájú agomelatin, elõállításának módszere és abból készült gyógyszerészeti készítmények - Google Patents
Új VI kristályos formájú agomelatin, elõállításának módszere és abból készült gyógyszerészeti készítmények Download PDFInfo
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Description
1 he présem ms ends· «dan;··: ΐο a naiv erystaiboO förm V;!:odnnsneiarme o? Aáf;2-íW-medo\\ · I ••oaphchs I annyi iaevhunnk otfforTmda (ÍV:
to a process ti'.'·· ds propitiation spit to phato?aeetd$eaf enioposiiions eoniadopg ti
Agorneknnse, or V· dès 7-wodos.y · ; -napod) tsedw tiavunsnodc. has «aitobte phanaaooiogieas properties. ít hsa de dodde ihatoro of being on äh·,- on« hand an egortts? of the receptors of the toekwmmergu. .system sad no ihn other hand an anvagcwva of tile Ή if; recepun These pro; « si tes dispart Ibereto in actiw-y to the eesitslf itorvops system and more especially in Ilia trennpaot of major degressiotn Maisénál affective disorder, steep dssonkta. cardiisvasculnf pathologies, pathologies of the thgestive :·ο«;«η·. msowrna and fiatgda dpa to jeplag. appetite disorders and obesity ,
Agomehnme. sis preparation and its stse in iherapeades have bees desesihsd in European· paten? Id 0 047 285
Crvsislime ferais of egomeiadse hasai already been díaeiosed ds the prior an, such as, for esasogfe. EP17S24A4I
In view of the phannsveuPca; «aine of this eoropottnd, if was esaemlal to obtain, st with eseelkn? parity, and: espsesally ip a perfectly mprodocrbfe form, having vtdisabie eharaelen sties of dosofenoe and ease of fernntkrtfen, pi lowing it to be stored for predopged periods withoat particalar eonditlons of fergperatnre, tight, humidify or osvgos terei.
The appiteant has now developed: ο process: Ihr obtaining eeomekumc la a s:r\ «dime form wkl eh ,is W«H deiliied, reprOdaeible and aeeofemgjy· jigs valuable ehametedsfigs of díssélutiorr grid ease of fommlahon, i foe new·· loins adddmed) gas sfahddv over um·.; xslneh is schölle wiusikuble. pen mume optimum storage: WObout special pW· aUK'U wpK ooW en νο\οηη,Ρ ,sb mises m >fo mew ne wWseï w-hoon
Ihn pressm unom wo rennes morn spec ideady in ihn oryswidue form ¥1: of ihn compound of formula (lg ehww. tensed Io ihn following X-m;·. powder dPIfowdoo wagram. measured using a Bmfer iΧηοΡηοηκ: ddlfaewnwwr (copper aoilearfsrdoj and expressed in iernm of IpiUi'piasmr distance d, Braae's made à wem and rehbvc au-nNU; tes pressen as a fx'rceritage re Suive io ihe nws· auensc Ime):
The crvsmlifoe form V! of ihn ciirrrpnurfoof formula f;i| Inn also feen ;. daweterr-cn bn she following infoa-red spectroscopy diagram; peaks observed: ai 907. c cos'g 860.7 ernfo 957.H cm'S H.;7 7 enf:; 754,6 cm'7 774,6 çpf S 698.9 enfg 077,1 cm;. OiU.O end': 61 ; 0 ein '. 588.1 cru X
The fovepbon relaies also so a process 4or ihn preparation of the cm somme io-τη ¥| of lue compound of iornmla |l}, chanaberised In usa a sofoslmi of agemielaime Pr Isopmpyl einer Is healed ai nmd up sad than fopidin corded io ur€, Λ der futrälicw in nww.u die form VI in nblälped in pare tora;
In Ihg: orrsiadismien process according io the tuvamiorr liiere rna> be used ihe conipm.ard of formula ily obtained be ana process. 'Oie invetittoh relates aise Ιό arm-her process fm sise prepnoUnw öf tliô ér^sMllsrœ Torrn VI of the coro pound of idrhdtia (ff cMracterised in thai egnmelaUne is cwsndbsod Oom a neper ethanol misaine (ärfad vmanievm-nnr, at atohiept temperature node? a high prcv.sne for 24 hours, IVete rainy, m Ihis second or estai Ns at on r pmaeay a ce eg sling to the Invention, agomeiahne will 'bo recinvtalilsed ondera high pressten of 10 khar,
In this second crysiadlsaimn : process sect some to the irw radon thorp may he used k K ' > , ! X 0 \ V ' > v
Obiamon:: Oils crystalline lorte has the advantage of perm Siting the prepsmho« of phamnwetnteal tbrmuhuwns hu el op a eon s taut nodoe prodnoihk compositum. having escellenf stabfhiy over time,
The :p harm aoo log iehi study of tire ίοηρ V: so: obtained: has shown no impmiäxü activity dp the centra! nervous systaos ami tor nuvraclreolation, allowing its dsPfiilhess to he esMhlIsherl in die treatment of stress, sleep d modem. amaefv. otaior depression,: seasotta! nfïeeiiee disorder, cardiovascular pathologies, pnthnipgles of the digestive'· system. Insomnia nod tnifigne due to jot-lag. sehizoolsrenla. panic aliachs, mcianchaha. appetite disorders, <-besüt. insomnia. pain, psyehotte disorders, epilepsy, diabetes, hari.msww dlnease, seniledeownha, vnrrnus dlaordem assoctaied m r > » <. 4 \ V s more loss, Alohetmefs discascyand also in eefehral eirenlation disorders. In another field ofaehyhy, if appears that in the treatment, the term VI of ayornotaw-e may he used in seyua] dysdaietjons, that it has progenies as an genlabon whdmce mat irnmmtoweduiaiof and that it is ea pa hie of beinp ased in the treatment of cancers.
The crystal Poe loon Vi of agomelatlne will he nsed preferably to the treatment til rna|er dépréssion, seasonal affective disorder, sleep disorders, eardmvasenbtr pathologies, gat fed ogles of she digestive system. t osonta la and fatigue dug to jet-lag, appehte ylisorderS: and obesity.
The invention relates also to pharmaceutical: compositions comprising as active ingredient the crystalline hem VI of the -aannmmd of íonnttla (I) wdh nog or tnom suitable uns ï. non ans ;c sserpienls. Among the phanoaceuhca; c; et-posh ions according w she invention, there may be mentioned, more cspecoufy. those that ore statable fbt1 pmi. parenteral (I air ave turns or snhcainiteons) or nasal adothrlslrattna, tablets or dragées, grandies, aitblrngitrd tablets, capsules, foresters, suppositories., uvatos. ouornoots. dented pela egceulde preparátum ' bonk.dT ' uepeOsteo'·. and chewing grogs.
The useful dosage cast he adapted according to the statusé ttod revedig of the disorder, the administration route astd the age and weight of use pata.n·. I he dosage varies trogt d.l tgg to ! g per day to one ognrore ubuitolsiintkhT'
The csasttplcs below blurwato ihr Igvenbon bgt do not iutus It In any way.
Jlyamdle is < r%staüfmt form Vi of AhpA;7!smeifeïrsy-l:"ïva|ibiiifî)tdîiyI|^Mîâriîiàe
lit 74. g Τ Λ g Tf T-nwthoxy-· I wiaphihynctht I : eveten arte and Tbálb g of Isopropyl ether are latrod need hue a lobe The suspension is healed as boiling tat a teptpsrglure of / 3°C) for d hours. Rapid cooling to 0 (I is then eastaed Oof. Aile· oste hour hi PC. iffirnhon In mono over a glass ltd of porosity 3: Is ogtyledi ont. The solid obtained Is characterised by Its mtdthtg point and by the Ipthttvlstg X-ray powder diOVachoti diagthoit, otehsitred hsittg I Bag: or CAsoOnnolv dlltàdctdhietdr * copper anticatilode) and expressed in ternes of mferpfaaar distance d, BraggX -angle 2 theta: and relative Intensity fespressed os wpereentage relative to the; fonsi Intense fineT
AMongρηχιο P % ' 1 : ς i speetmaeOpy dtagtätm 911/,5 cin '7 060.7 cm'7 ES2,4 cm 7 127,4 cm'7 754.6 caff 724,0 cm'7 0i;5 4 em'7 4724 cm'2 65Ö.0 epf 7 21 ! ,9 cm"7 SM.'f cm': llIffitÉLlt <'r>sn*lime tarm Vf ί>ΐ'Λ-{2·Η7-ηηθΟη;ο Iompbtln Ocdo IpwcWnndc 2 g pf Yd2 4'wnethnxy·· ; nwpluhyl telin i jnceimniik' ire pieced In 20 ret W a water/ebtabof tMxibre tSOHO vokmnv volume! at: 25""t ". Hie suspension is laltered mer a glass fru of pomsiip 4, TH:-. solthlori sotwiaed with V4 2o 7-metfwx;, · 1 · 5ráp}pitví}edryí|aceta;n:ríde Is ipPíeeied to a pm ware pf 10 klxn Λ Iter 24 hems, crystmbx,uion is cnmpHte ami the who otpahwtf w cha; aeiensed by ns melting point and by the: fpllemiog Kway powder didxsetion diagram, measared using a Broker .D.SOOQnnuk: dtiktantomeier meppw ;mOcwbodcn and expressed m terms of mierphmar distance d. Bnrggb angle 2 theta and relative nucnsu> (espres-xd as a pereemage relative to the meet pacose tlnef
4 f:7/4/0 poop; 0 / t; ·
Infra wed spectroscopy diagraop 707.5 enfb 460.7 em'7 Of 2.2 enf 7 427 4 era 7 724,0 ettf7 744.0 cm 7 094.4 enf 7 072,1 enf7 050 0 cm 7 to i 7/ cm 7 540,1 cm'7
Example 37 IHomnnwenthnd emnpmndkm
FonPtdation bír the preparation of 4000 tablets each contend og; 25 ro w (tempo ttod ; o f bxa sit pi e 1 or 2,,,,. ,.,....., 7 5 a
Lactose motmhydtpte,,,:...,,,,,..,,,,:,:.,,,..,.,.,,,,,,.,,,,.....02 g M ague.ib.ülï :... i. :,, ^.,., .·. i ÿ,i > Ϊ i . :,.„',,, ói;,;,«;,,;,,,, C :. ... :< ......... í. 3 g Mât M 6ί6Πί6, , . .......; ,...,,·. .,.,.... :.............................. :........ : aa- :,.., , 26 g M dlladáxislds..,....,.,.......,. ..,f,.. ,,,,....,. ,. ,. .,, ^..(v,. ?,,,,,..................... :6 |:
Avdiibid66:o<66666l 61 ise:;..,.:,,,,...,...;, :. 6.3 g
Prägelatinisæd aun/g staseh :> pe Λ.„x 4; § fAampk·· 4: 1*Ι»«ΐ4^1:^^^.ίΜί^Ι#Μίί rornudalg j-s 6a' de; proparadog af ;000 tablais aaed comaining 25 rag:
Campoimd of IManigfc 1. di 1„..............,,,,.,,,,.,,.,. :.,,,,,, :,.,., 25 g. I, m inas : mono h y drate ..............................,,,,....,,,..,, :62 g
Magae-aua: siearate ... ..................................................1 3 g
Povidone ,. ;.,, 2 g
Anhydrous co I Id id a 1 si 6ca........................: :. 0.3g
Sdduaa ce 1 hdose g;ycoiada,,.,,,,..:::, 3d g Staarte add 2.6 g
Claims (3)
- ázebadaims igém pontot I; |i) képlet# aiomelaí in Vfkrlstaiyfcóöáp::; 0>, irlimtel por-röntgendiffrakciós diagrammal jellemezve, amely Broker D5<Jü0matic diitekionmteriseo {réz aoiikatóddal) mért és d síkok közötti távolsággal, Bragg-fele 2-ieta szöggel és relatívintenzitással fa legintenzívebb vonalhoz visxonyftott százalékban van kifejezv^ialíemzett:2. kijárás az 1. igénypont szerinti h) képíetd vegyidet VI kristály-formájának előállítására, azzal jellemezve, hogy agomeiatin izopropü-éterben készült oldatát fozráétg n?e!egstj«io gyorsan S3 %ra Miliők, majd vákuumban szűrjek, X kijárás az l. igénypont szerinti üt keplefu vegyidet Ví kmiályfeimájának előállítására^ azzal jellemezve, hogy agwmeiatmt vlz/etanol keverékéből (SO/ŐO téíorgaí/térfogaií kristályosítják kőíOvyezeti bősnérsékJelan, Mkfebat nyomáson,, .24 érán ói
- 4. Gyógyszerészeti készítmény, amely aktiv alkotóként az 3. Igénypont szer inti agornelatin VI krlstályferruit tartalmazza egy vagy ÍÍ3 gyógyszerészei iiegelíőgsbható Inert, nem Älvs tiordozóvalegyutt. 5. A 4 Igénypont szerinti gyógyszerészeti készítmények a nselatonmerg rendszer féailéi lenessé gerne k kezelésére szolgáló gyógyszerek előállításában való alkalmazásra,
- 6. A a. igénypont szerinti gyógyszerészeti késziimény&k a következő betegségek kezelésére szolgáló gyógyszerek előállításában való alkalmazásra: alvási reodeilenessegek, stressz, szorongás, Időszakos érzelmi rendellenesség vagy erős depresszió, szlveés érrendszeri patológiás állapötők, áz emésztőrendszer patológíás állapptái, időeltolódás miatti áírnátianslg és kimerültség, |kizpfréi|á. päolktohamok. melankólia, éiks-sási ndodsiienességek. elbírás, álmatlanság, ^ájdaiom, p5.dchodkus renddkmességek, opHepsaia, diabètes.?, Parkinson-kör, öregkő?! demanda, normális vagy patológiás öregedéssel kapcsolatos különféle rendellenességek, migrén, ínemöriaesvar, Alzhekrse-' kór. agyi keongési íorxseíienességek vagy síesnáks működési tavatok, *ΐsím ovuládö gádor vagy Immen msduláferoig vagy rákok keaeîlsêbëm
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| FR0707861A FR2923482B1 (fr) | 2007-11-09 | 2007-11-09 | Nouvelle forme cristalline vi de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
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| FR2934856B1 (fr) * | 2008-08-05 | 2010-08-13 | Servier Lab | Nouveau procede d'obtention de la forme cristalline v de l'agomelatine |
| CN101585779B (zh) * | 2009-03-10 | 2014-04-02 | 上海医药工业研究院 | 阿戈美拉汀的晶型vi及其制备方法和应用 |
| WO2011006387A1 (zh) * | 2009-07-11 | 2011-01-20 | 浙江华海药业股份有限公司 | 阿戈美拉汀的制备方法、阿戈美拉汀晶形及其制备方法 |
| CN101955440B (zh) * | 2009-07-17 | 2014-04-09 | 江苏万特制药有限公司 | 一种阿戈美拉汀新晶型及其制备方法 |
| CN102001959B (zh) * | 2009-09-01 | 2014-07-02 | 北京本草天源药物研究院 | 一种药物晶体及其制备方法和用途 |
| EP2319827A1 (en) | 2009-11-09 | 2011-05-11 | Ratiopharm GmbH | Process for the production of polymorph form I of agomelatine |
| CN101781226B (zh) | 2009-12-23 | 2012-03-28 | 天津泰普药品科技发展有限公司 | 阿戈美拉汀及其药物组合物 |
| WO2011128413A1 (en) | 2010-04-15 | 2011-10-20 | Ratiopharm Gmbh | Process for the production of polymorph form i of agomelatine |
| WO2012046253A2 (en) * | 2010-10-08 | 2012-04-12 | Msn Laboratories Limited | Process for the preparation of n-[2- (7-methoxy-l-naphthyl) ethyl] acetamide and its novel crystalline forms |
| CZ303787B6 (cs) | 2011-01-21 | 2013-05-02 | Zentiva, K.S. | Metastabilní krystalové formy agomelatinu a jejich farmaceutické kompozice |
| CN102690209A (zh) * | 2011-03-23 | 2012-09-26 | 上海医药工业研究院 | 阿戈美拉汀的混晶(形式-ⅷ)、其制备方法、应用和包含其的药物组合物 |
| WO2012130837A1 (en) | 2011-03-28 | 2012-10-04 | Ratiopharm Gmbh | Solid agomelatine in non-crystalline form |
| CN102206864B (zh) * | 2011-04-13 | 2012-10-03 | 吉林省博大伟业制药有限公司 | 阿戈美拉汀的ⅵ晶型单晶及混合晶型和制备方法 |
| PH12012000132B1 (en) * | 2011-06-09 | 2014-10-20 | Servier Lab | New co-crystals of agomelatine, a process for their preparation and pharmaceutical compositions containing them |
| WO2013082302A1 (en) | 2011-11-30 | 2013-06-06 | Ratiopharm Gmbh | Agomelatine-urea complex and crystalline forms thereof |
| CZ2012108A3 (en) | 2012-02-15 | 2013-02-27 | Zentiva Ks | A method for the manufacture of a polymorphously stable pharmaceutical composition containing agomelatine |
| EP2872129B1 (en) | 2012-07-16 | 2017-03-08 | ratiopharm GmbH | Complex of agomelatine and cyclodextrin |
| CN102988315B (zh) * | 2012-09-28 | 2017-11-17 | 浙江华海药业股份有限公司 | 阿戈美拉汀固体制剂的制备方法 |
| WO2014072998A1 (en) | 2012-11-07 | 2014-05-15 | Cadila Healthcare Limited | An improved process for preparation of agomelatine |
| EP2934502A1 (en) | 2012-12-21 | 2015-10-28 | Laboratorios Lesvi S.L. | Process for prepararing n-(2-(7-methoxy-1-naphthalenyl)ethyl) acetamide and solid forms thereof |
| EP2810647A1 (en) | 2013-06-06 | 2014-12-10 | Zentiva, a.s. | Pharmaceutical formulations comprising agomelatine in the form of agomelatine co-crystal with an organic acid |
| PL2810656T3 (pl) | 2013-06-06 | 2018-01-31 | Zentiva Ks | Preparaty agomelatyny zawierające agomelatynę w postaci kokryształów |
| CZ2013621A3 (cs) | 2013-08-13 | 2015-02-25 | Zentiva, K.S. | Termodynamicky stabilní tuhý roztok agomelatinu pro použití ve farmaceutické formulaci |
| WO2015124496A1 (en) | 2014-02-19 | 2015-08-27 | Synthon B.V. | Pharmaceutical composition comprising amorphous agomelatine |
| PL3075724T3 (pl) | 2015-03-31 | 2023-12-27 | F.I.S.- Fabbrica Italiana Sintetici S.P.A. | Stała postać agomelatyny |
| EP3466923A1 (en) | 2017-10-09 | 2019-04-10 | KRKA, d.d., Novo mesto | Process for the preparation of agomelatine in crystalline form |
| EP3466413A1 (en) | 2017-10-09 | 2019-04-10 | KRKA, d.d., Novo mesto | Pharmaceutical composition containing agomelatine and process for the preparation thereof |
| CN114028335A (zh) * | 2021-12-24 | 2022-02-11 | 山东京卫制药有限公司 | 一种阿戈美拉汀溶液鼻喷剂及其应用 |
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| IT1146164B (it) | 1980-07-16 | 1986-11-12 | Selenia Ind Elettroniche | Dispositivo di filtraggio doppler adattivo alla situazione di clutter ed ecm esterna per impianti radar |
| FR2658818B1 (fr) * | 1990-02-27 | 1993-12-31 | Adir Cie | Nouveaux derives a structure naphtalenique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| SK2242003A3 (en) * | 2000-07-27 | 2003-10-07 | Teva Pharma | Crystalline and pure modafinil, and process of preparing the same |
| US6992219B2 (en) * | 2002-08-09 | 2006-01-31 | Cephalon France | Modafinil polymorphic forms |
| FR2866335B1 (fr) * | 2004-02-13 | 2006-05-26 | Servier Lab | Nouveau procede de synthese de l'agomelatine |
| US7645905B2 (en) * | 2005-08-03 | 2010-01-12 | Les Laboratoires Servier | Crystalline form IV of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
| US7358395B2 (en) * | 2005-08-03 | 2008-04-15 | Les Laboratories Servier | Crystalline form V of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
| FR2889522B1 (fr) * | 2005-08-03 | 2007-12-28 | Servier Lab | Nouvelle forme cristalline iv de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
| US7635721B2 (en) * | 2005-08-03 | 2009-12-22 | Les Laboratoires Servier | Crystalline form III of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
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