DK2838517T3 - Oralt tilgængelig farmaceutisk formulering, som er egnet til forbedret behandling af bevægelseslidelser - Google Patents
Oralt tilgængelig farmaceutisk formulering, som er egnet til forbedret behandling af bevægelseslidelser Download PDFInfo
- Publication number
- DK2838517T3 DK2838517T3 DK13725557.6T DK13725557T DK2838517T3 DK 2838517 T3 DK2838517 T3 DK 2838517T3 DK 13725557 T DK13725557 T DK 13725557T DK 2838517 T3 DK2838517 T3 DK 2838517T3
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- DK
- Denmark
- Prior art keywords
- agonist
- zolmitriptan
- pharmaceutical formulation
- buspirone
- present disclosure
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Claims (15)
1. Oral farmaceutisk formulering omfattende a. en matrixbestanddel, som omfatter en aktiv farmaceutisk bestanddel, som er en agonist af to eller flere af 5-HT1B-, 5-HT1D- og 5-HT1 F-receptorerne, som er en triptan, idet nævnte matrixbestanddel sørger for forlænget frigivelse af den aktive farmaceutiske bestanddel, og b. en bestanddel, som omfatter en aktiv farmaceutisk bestanddel, som er en agonist af 5-HT1A-receptoren, hvilken bestanddel sørger for øjeblikkelig frigivelse af den aktive farmaceutiske bestanddel.
2. Farmaceutisk formulering ifølge krav 1, hvor triptanen er valgt fra gruppen bestående af zolmitriptan, rizatriptan, sumatriptan, naratriptan, almotriptan, frovatriptan, avitrip-tan, imotriptan og eletriptan og farmaceutisk acceptable derivater deraf.
3. Farmaceutisk formulering ifølge krav 1, hvor agonisten af 5-HT1A-receptoren er valgt fra gruppen bestående af buspiron, tandospiron, gepiron, alnespiron, binospiron, ipsapiron, perospiron, befiradol, repinotan, piclozotan, osemozotan, flesinoxan, fliban-serin og sarizotan og farmaceutisk acceptable derivater deraf.
4. Farmaceutisk formulering ifølge krav 1, hvor triptanen er zolmitriptan, og agonisten af 5-HT1 A-receptoren er buspiron.
5. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor formuleringen a. er en fast doseringsform, såsom en tablet, b. omfatter matrixbestanddel a. og bestanddel b. i separate rum eller lag, c. omfatter en indre kernematrix, som sørger for forlænget frigivelse af triptanen, og et ydre overtræk, som sørger for øjeblikkelig frigivelse af agonisten af 5-HT1 A-receptoren, d. er en tolagstablet, som omfatter ét lag, der sørger for forlænget frigivelse af triptanen, og et andet lag, der sørger for øjeblikkelig frigivelse af agonisten af 5-HT1A-receptoren, hvor hvert lag er til stede i samme tablet, eller e. hvor hver af bestanddelene a. og b. tilvejebringes sammen i en kapsel, hvor kapslen omfatter bestanddelene a. og b. som separate granulater eller pellets.
6. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor ma-trixbestanddelen a. omfatter én eller flere excipienser, hvor excipienserne er valgt fra gruppen bestående af a. frigivelseskontrollerende excipienser, b. hydroxypropylmethylcellulose (HPMC), c. mikrokrystallinsk cellulose (MCC), d. en HPMC-excipiens, som er til stede i en mængde på 20-50%, såsom 20-25%, fx 25-30%, såsom 30-35%, fx 35-40%, såsom 40-45%, fx 45-50%, og e. en MCC-excipiens, som er til stede i en mængde på 50 til 80%, såsom 60-70%.
7. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor ma-trixbestanddelen a. a. yderligere omfatter talkum, hvor nævnte talkum er til stede i en mængde på 1-10%, såsom ca. 5%, b. komprimeres til en hårdhed på 50-70N, c. sørger for mindst 80% frigivelse af triptanen efter 12 timer, d. består af én eller flere HPMC'er, én eller flere MCC'er, talkum og en triptan, e. omfatter triptanen i en mængde på fra 0,1 til 10 mg, såsom fra 0,5 til 5 mg, fx omkring 1 mg, og/eller f. omfatter eller består af 10-50%, såsom 20-40%, HPMC; 40-80%, såsom 55-75% MCC; 1-10%, såsom 2-8% talkum; og 0,1-5%, såsom 0,5-2% afen trip-tan.
8. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor bestanddel b. omfatter a. en excipiens, b. en filmdannende excipiens, c. en excipiens, som er en hydroxypropylmethylcellulose (HPMC), d. eller består af mindst én HPMC og en agonist af 5-HT1 A-receptoren, e. en agonist af 5-HT1 A-receptoren i en mængde på fra 1 til 20 mg, såsom fra 5 til 15 mg, fx ca. 10 mg, og/eller f. eller består af 25-40% HPMC og 60-75% af en agonist af 5-HT1 A-receptoren.
9. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor den formulering, der består af bestanddelene a. og b., omfatter eller i det væsentlige består af a. 20-40% HPMC, b. 50-70% MCC, c. 1-10% talkum d. 0,1-10% af en triptan, som fortrinsvis er valgt fra gruppen bestående af zolmitriptan, rizatriptan, sumatriptan, naratriptan, almotriptan, frovatriptan og eletriptan, e. 1-20% af en agonist af 5-HT1 A-receptoren, som fortrinsvis er valgt fra gruppen bestående af buspiron, tandospiron, gepiron, alnespiron, binospiron, ipsapi-ron, perospiron, befiradol, repinotan piclozotan, osemozotan, flesinoxan, fliban-serin og sarizotan, f. 0,1-10% HPMC, hvor bestanddelene a., b., c. og d. er omfattet i matrixbestanddel a., og bestanddelene e. og f. er omfattet i bestanddel b.
10. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor formuleringen omfatter én eller flere yderligere aktive bestanddele.
11. Farmaceutisk formulering ifølge krav 10, hvor den yderligere aktive bestanddel er valgt fra gruppen bestående af dopamin; dopamin-prodrugs; L-DOPA, levodopa; car-boxylaseinhibitorer såsom carbidopa eller benserazid; dopaminreceptoragonister såsom bromcriptin, pergolid, pramipexol, ropinirol, piribedil, cabergolin, apomorphin, lisurid; NMDA-antagonister såsom fx amatidin; catechol-O-methyltransferaser; COMT-inhibitorer såsom tolcapon og entacapon; MAO-B-inhibitorer såsom selegilin og rasagi-lin; serotoninreceptormodulatorer; kappaopioidreceptoragonister såsom TRK-820; GABA-modulatorer; modulatorer af neuronale kaliumkanaler såsom flupirtin og reti-gabin; og glutamatreceptormodulatorer.
12. Farmaceutisk formulering ifølge et hvilket som helst af de foregående krav, hvor formuleringen er til anvendelse i behandlingen afen bevægelseslidelse.
13. Farmaceutisk formulering til anvendelse ifølge krav 12, hvor bevægelseslidelsen er valgt fra gruppen bestående af Parkinsons sygdom, bevægelseslidelser forbundet med Parkinsons sygdom såsom bradykinesi, akinesi og dyskinesi, L-DOPA-induceret dyski-nesi, tardiv dyskinesi, ataksi, akatisi, dystoni, essentiel tremor, Huntingtons sygdom, myoklonus, Rett-syndrom, Tourettes syndrom, Wilsons sygdom, dyskinesier, chorea, Machado-Joseph-sygdom, uro i benene, spasmodisk torticollis, geniospasme eller bevægelsesforstyrrelser forbundet dermed, bevægelsesforstyrrelser forbundet med anvendelse af lægemidler såsom neuroleptiske lægemidler, antipsykotiske midler, anti-depressiva og antiemetika, idiopatisk sygdom, genetiske dysfunktioner, infektioner eller andre tilstande, som fører til dysfunktion af de basale ganglier og/eller fører til ændrede synaptiske dopaminniveauer, og afvænning fra lægemidler.
14. Farmaceutisk formulering ifølge et hvilket som helst af kravene 1 -11 eller farmaceutisk formulering til anvendelse ifølge et hvilket som helst af kravene 12-13, hvor nævnte triptan skal administreres i en dosis på fra 0,001 til 10 mg/kg legemsvægt, såsom 0,001 til 5 mg/kg legemsvægt, såsom 0,01 til 1 mg/kg legemsvægt; og hvor 5-HT1A-agonis-ten skal administreres i en dosis på fra 0,01 til 10 mg/kg legemsvægt, såsom 0,01 til 5 mg/kg legemsvægt, såsom 0,1 til 1 mg/kg legemsvægt.
15. Farmaceutisk formulering ifølge et hvilket som helst af kravene 1 -11 eller farmaceutisk formulering til anvendelse ifølge et hvilket som helst af kravene 12-14, hvor formuleringen skal administreres i kombination med L-DOPA og/eller benzerazid, hvor L-DOPA og/eller benzerazid administreres sekventielt eller samtidigt.
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PCT/DK2012/050190 WO2012163365A1 (en) | 2011-06-01 | 2012-06-01 | Combinations of serotonin receptor agonists for treatment of movement disorders |
DKPA201270755 | 2012-12-04 | ||
PCT/DK2013/050111 WO2013156035A1 (en) | 2012-04-18 | 2013-04-18 | Orally available pharmaceutical formulation suitable for improved management of movement disorders |
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RU (1) | RU2670272C2 (da) |
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