HRP20210963T1 - Formulacija za kontinuirano otpuštanje kolhicina i postupci priprave istog - Google Patents
Formulacija za kontinuirano otpuštanje kolhicina i postupci priprave istog Download PDFInfo
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- HRP20210963T1 HRP20210963T1 HRP20210963TT HRP20210963T HRP20210963T1 HR P20210963 T1 HRP20210963 T1 HR P20210963T1 HR P20210963T T HRP20210963T T HR P20210963TT HR P20210963 T HRP20210963 T HR P20210963T HR P20210963 T1 HRP20210963 T1 HR P20210963T1
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- Prior art keywords
- colchicine
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- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 title claims 24
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Classifications
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Claims (9)
1. Formula za kontinuirano otpuštanje kolhicina kao aktivnog sastojka, gdje se formula sastoji od:
(a) granula koje sadrže od 0.1 do 0.6 mg kolhicina ili njegove farmaceutski prihvatljive soli;
(b) vezivnog sredstva, gdje je vezivno sredstvo hidroksipropil metilceluloza (HPMC) 6 mPa•s u količini od 1% do 30% (na težinu) formule;
(c) usporavajući agens u količini od 5% do 40% (na težinu) formule, gdje je sredstvo za usporavanje raspršivač u kompleksnom spoju jednakih dijelova po težini HPMC-a sa stupnjem viskoznosti od 4000 mPa•s i monohidrata laktoze (Retalac®); te
(d) najmanje jedna farmaceutski prihvatljiva pomoćna tvar izmiješana s granulama,
dok je formula za kontinuirano otpuštanje u tableti.
2. Formula iz patentnog zahtjeva 1, gdje je:
farmaceutski prihvatljiva pomoćna tvar odabrana iz skupine koja se sastoji od punila, sredstva za klizanje i za podmazivanje, ili njihove kombinacije;
gdje se punilo bira iz skupine koja se sastoji od saharoze, laktoze, m-čestičnog monohidrata laktoze, trehaloze, maltoze, manitola i sorbitola, natrijeve kroskarmeloze, krospovidona, alginske kiseline, natrij alginata, metakrilične kiseline divinil benzena (DVB), unakrsno vezanog polivinil pirolidona (PVP), mikrokristalne celuloze, kalijevog polakrilina, natrijevog škrobnog glikolata, škroba, pregelatiniziranog škroba i njihovih kombinacija, te gdje ukupna količina punila u formuli iznosi između otprilike 5.0 težine % i 90.0 težine % formule;
gdje se sredstvo za klizanje bira iz skupine koja se sastoji od koloidnog silikon dioksida, magnezijevog trisilikata, celuloze u prahu, talka i trobaznog kalcijevog fosfata, opcionalno gdje ukupna količina sredstva za rastvaranje u tekućinu iznosi između otprilike0.5 % težine do otprilike 5 % težine formule; te
gdje se sredstvo za podmazivanje bira iz skupine koja se sastoji od gliceril behanata, stearinske kiseline, hidrogeniziranih biljnih ulja, stearinskog alkohola, leucina, polietilen glikola, magnezijevog stearata, gliceril monostearata, polietilen glikola, polimera etilen oksida, natrijevog lauril sulfata, magnezijevog lauril sulfata, natrijevog oleata, natrijevog stearil fumarata, DL-leucina i koloidnog silikata, opcionalno gdje se sredstvo za podmazivanje uključuje u količini između otprilike0.5 težine% do otprilike5 % težine formule.
3. Formula tvrdnje 1 ili tvrdnje 2, gdje je kompresijska jačina tablete između otprilike 30N i otprilike 130N.
4. Formula prema bilo kojem od zahtjeva 1-3, za uporabu u prevenciji i/ili liječenju kardiovaskularnih bolesti, opcionalno gdje se kardiovaskularna bolest bira iz skupine koja se sastoji od akutne perikardije, ponavljajuće perikardije, post-perikardijskog sindroma (PPS) i kardiovaskularnih događaja kod pacijenata sa stabilnom koronarnom bolešću.
5. Formula za uporabu sukladno zahtjevu 4, gdje je formula za uporabu u kombinaciji s konvencionalnom terapijom za dugoročnu prevenciju akutnog kardiovaskularnog događaja kod pacijenata s ustanovljenom stabilnom koronarnom bolešću,
opcionalno gdje je rečeni akutni kardiovaskularni događaj akutni koronarni sindrom, od bolničkog zastoja srca ili nekardioembolijskog ishemijskog udara, te
opcionalno gdje konvencionalna terapija uključuje primjenu statina spojivog s kolhicinom, gdje se statin spojiv s kolhicinom primjenuje u fiksnoj ili nefiksnoj kombinaciji s kolhicinom, opcionalno gdje se statin spojiv s kolhicinom bira iz skupine koja se sastoji od atorvastatina, rosuvastatina, simvastatina i pravastatina, derivata njegovih soli.
6. Formula prema bilo kojem od zahtjeva 1-3, za uporabu kod prevencije i/ili liječenja upalne bolesti, opcionalno gdje se upalna bolest bira iz skupine koja se sastoji od gihta, porodične mediteranske groznice, Behčetove bolesti, starosno vezane degeneracije makule i Alzheimerove bolesti.
7. Formula za uporabu sukladno zahtjevu 6, gdje ukupna dnevna doza kolhicina koja se primjenjuje na subjekta ne iznosi više od otprilike 0,75 mg.
8. Proces priprave tablete s kontinuiranim otpuštanjem kolhicina koji se sastoji od:
(A) formiranja otopine rastapanjem kolhicina u vodi, gdje se kolhicin daje u količini tako da se rezultantna tableta sastoji od 0,25 do 0,75 % (na težinu) kolhicina;
(B) dodavanje vezivnog sredstva i punila u otopinu Koraka A, te formiranje vlažnog granulata, gdje je vezivno sredstvo hidroksipropil metilceluloza (HPMC) 6 mPa•s i dodaje se u količini tako da se rezultantna tableta sastoji od 1% do 30% (na težinu) vezivnog sredstva;
(C) sušenje vezivnog sredstva iz Koraka B;
(D) miješanje sušenog granulata iz Koraka C sa sredstvom za usporavanje, punilom, sredstvom za klizanje i za podmazivanje, gdje je sredstvo za usporavanje raspršivač u kompleksnom spoju jednakih dijelova po težini HPMC- sa stupnjem viskoznosti od 4000 mPa•s i monohidrata laktoze (Retalac®) i dodaje se u količini tako da se rezultantna tableta sastoji od 5 do 40 % (na težinu) sredstva za usporavanje; te
(E) komprimiranje završnog granulata iz Koraka D u tabletu.
9. Proces iz zahtjeva 8, gdje:
je u Koraku B punilo koje se rabi monohidrat laktoze i pregelatinizirani škrob; a u Koraku D punilo koje se rabi je monohidrat laktoze, sredstvo za klizanje je talk, a sredstvo za podmazivanje je stearinska kiselina; i/ili posebni sastojci i količine koji se rabe su:
[image]
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361812514P | 2013-04-16 | 2013-04-16 | |
| EP13194505 | 2013-11-26 | ||
| EP14755124.6A EP2986280B1 (en) | 2013-04-16 | 2014-04-16 | Sustained-release formulations of colchicine and methods of using same |
| PCT/IB2014/001201 WO2014170755A2 (en) | 2013-04-16 | 2014-04-16 | Sustained-release formulations of colchicine and methods of using same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20210963T1 true HRP20210963T1 (hr) | 2021-09-17 |
Family
ID=66339151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20210963TT HRP20210963T1 (hr) | 2013-04-16 | 2021-06-16 | Formulacija za kontinuirano otpuštanje kolhicina i postupci priprave istog |
Country Status (7)
| Country | Link |
|---|---|
| JP (2) | JP6697539B2 (hr) |
| DK (1) | DK2986280T3 (hr) |
| ES (1) | ES2870718T3 (hr) |
| HR (1) | HRP20210963T1 (hr) |
| HU (1) | HUE054663T2 (hr) |
| IL (1) | IL242001B (hr) |
| LT (1) | LT2986280T (hr) |
-
2014
- 2014-04-16 LT LTEP14755124.6T patent/LT2986280T/lt unknown
- 2014-04-16 HU HUE14755124A patent/HUE054663T2/hu unknown
- 2014-04-16 ES ES14755124T patent/ES2870718T3/es active Active
- 2014-04-16 DK DK14755124.6T patent/DK2986280T3/da active
-
2015
- 2015-10-11 IL IL242001A patent/IL242001B/en unknown
-
2018
- 2018-12-21 JP JP2018239862A patent/JP6697539B2/ja active Active
-
2020
- 2020-04-24 JP JP2020077153A patent/JP6887043B2/ja active Active
-
2021
- 2021-06-16 HR HRP20210963TT patent/HRP20210963T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| LT2986280T (lt) | 2021-06-25 |
| JP2019065032A (ja) | 2019-04-25 |
| JP6697539B2 (ja) | 2020-05-20 |
| JP6887043B2 (ja) | 2021-06-16 |
| JP2020125335A (ja) | 2020-08-20 |
| IL242001B (en) | 2021-07-29 |
| NZ713151A (en) | 2021-01-29 |
| NZ751885A (en) | 2021-01-29 |
| ES2870718T3 (es) | 2021-10-27 |
| DK2986280T3 (da) | 2021-06-14 |
| HUE054663T2 (hu) | 2021-09-28 |
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