DK2627319T3 - Farmaceutisk sammensætninger, der indeholder en dgat1-inhibitor - Google Patents
Farmaceutisk sammensætninger, der indeholder en dgat1-inhibitor Download PDFInfo
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- DK2627319T3 DK2627319T3 DK11779278.8T DK11779278T DK2627319T3 DK 2627319 T3 DK2627319 T3 DK 2627319T3 DK 11779278 T DK11779278 T DK 11779278T DK 2627319 T3 DK2627319 T3 DK 2627319T3
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Claims (15)
1. Farmaceutisk sammensætning i form af en tablet med valgfrit filmovertræk, der omfatter a) en terapeutisk effektiv mængde af natriumsaltet af forbindelsen //z/n.s-(4-i4-[5-(6-trifluor-methylpyridin-3-ylamino)-pyridin-2-yl]-phenyl} -cyclohexyl)-eddikesyre med formel (I),
b) natriumlaurylsulfat som overfladeaktivt stof med smøremiddelegenskaber, hvor det overfladeaktive stof er til stede i en mængde, der er 0,1 til 5 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I); c) hydroxypropylmethylcellulose eller hydroxypropylcellulose, begge med medium til høj viskositet, og kombinationer deraf som tørt bindemiddel, hvor det tørre bindemiddel er til stede i en mængde, der er 2 til 20 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I); d) et fyldstof valgt blandt mikrokrystallinsk cellulose, vandfrit dicalciumphosphat, vandfri lactose og blandinger deraf og en kombination af mikrokrystallinsk cellulose og vandfrit dicalciumphosphat og en kombination af mikrokrystallinsk cellulose og lactose, og hvor fyldstoffet er til stede i en mængde, der er 4 til 85 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I), og e) natriumstivelsesglycollat som desintegreringsmiddel, hvor desintegreringsmidlet er til stede i en mængde, der er 1 til 10 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I).
2. Farmaceutisk sammensætning ifølge krav 1, hvor fyldstoffet er til stede i en mængde, der er 20 til 85 vægt-%, fortrinsvis 50 til 80 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I).
3. Farmaceutisk sammensætning ifølge krav 1 eller 2, der yderligere omfatter et smøremiddel, hvor smøremidlet er valgt blandt natriumstearylfumarat og magnesiumstearat, og hvor smøremidlet er til stede i en mængde, der er 0,1 til 10 vægt-%, fortrinsvis 0,5 til 5 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (i). 1
4. Farmaceutisk sammensætning ifølge krav 3, hvor smøremidlet er natriumstearylfumarat.
5. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, der yderligere omfatter et glidemiddel, hvor glidemidlet er valgt blandt kolloid siliciumdioxid, magnesium-trisilicat, pulveriseret cellulose, stivelse, talkum og kombinationer deraf, og hvor glidemidlet er til stede i en mængde i intervallet fra ca. 0,05 til ca. 5 vægt-%, fortrinsvis fra ca. 0,1 til ca. 1 vægt-%, mere fortrinsvis fra ca. 0,25 til ca. 1 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I).
6. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, hvor hydroxypropylmethylcellulosen eller hydroxypropylcellulosen som tørt bindemiddel begge har viskositetsgrader på 3 eller 6 cps, mest fortrinsvis lavsubstitueret hydroxypropylcellulose (L-HPC LH-21); og kombinationer deraf.
7. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, hvor det tørre bindemiddel er til stede i en mængde, der er 5 til 15 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (1).
8. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, hvor fyldstoffet er en kombination af mikrokrystallinsk cellulose og vandfrit dicalciumphosphat eller en kombination af mikrokrystallinsk cellulose og lactose, hvor forholdet mellem fyldstofbestanddele er mellem 1:5 og 1:1, fortrinsvis 1:2.
9. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, hvor desintegreringsmidlet er til stede i en mængde, der er 2, 6 elller 9 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I).
10. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, hvor forbindelsen med formel (I) er til stede i en mængde i intervallet fra ca. 0,1 til ca. 50 vægt-%, fortrinsvis fra ca. 0,5 til ca. 30 vægt-%, mere fortrinsvis fra ca. 1 til ca. 30 vægt-% af tabletten før et eventuelt filmovertræk og baseret på den frie syre af forbindelsen med formel (I).
11. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav, hvor det overfladeaktive stof er natriumlaurylsulfat; det tørre bindemiddel er lavsubstitueret hydroxypropylcellulose (L-HPC LH-21); 2 fyldstoffet er en blanding af mikrokrystallinsk cellulose og lactose, hvor forholdet mellem mikrokrystallinsk cellulose og lactose er mellem 1:5 og 1:1, fortrinsvis 1:2, og desintegreringsmidlet er natriumstivelsesglycollat.
12. Farmaceutisk sammensætning ifølge krav 11, der yderligere omfatter smøremidlet natrium-stearylfumarat.
13. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 1 til 12 i form af en filmovertrukket tablet, hvor filmovertræksmaterialet er et polymert filmovertræksmateriale, der omfatter hydroxypropylmethylcellulose eller polyvinylalkohol, polyethylenglycol, lecithin, talkum og farvestof.
14. Farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav 1 til 13 til anvendelse til behandling eller forebyggelse af en tilstand eller forstyrrelse, der er forbundet med DGAT1 -aktivitet.
15. Fremgangsmåde til fremstilling af en farmaceutisk sammensætning ifølge et hvilket som helst af ovennævnte krav 1 til 12, som omfatter trinene: a) blanding af natriumsaltet af forbindelsen ira«,y-(4-{4-[5-(6-trifluomiethylpyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-eddikesyre med formel (I) med mindst ét farmaceutisk acceptabelt excipiens til frembringelse af en blanding; b) valsesammenpresning, herefter formaling af blandingen; c) smøring af den resulterende blanding og d) komprimering af den resulterende blanding til en fast oral doseringsform. 3
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| AR083417A1 (es) | 2010-10-14 | 2013-02-21 | Novartis Ag | Composiciones farmaceuticas que contienen un dgat1 inhibidor |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2013163508A1 (en) * | 2012-04-27 | 2013-10-31 | Novartis Ag | Tetrahydropyran dgat1 inhibitors |
| WO2013169648A1 (en) * | 2012-05-07 | 2013-11-14 | Novartis Ag | Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| CN114099496A (zh) | 2015-03-13 | 2022-03-01 | 艾斯柏伦治疗公司 | 含etc1002和依泽替米贝的组合及治疗方法 |
| MA41793A (fr) | 2015-03-16 | 2018-01-23 | Esperion Therapeutics Inc | Associations de doses fixes comprenant du etc1002 et une ou plusieurs statines permettant de traiter ou de réduire un risque cardiovasculaire |
| CN116440143A (zh) | 2015-11-19 | 2023-07-18 | 欣耀生医股份有限公司 | 预防或治疗脂肪肝的药物组合物 |
| US11975002B2 (en) | 2016-03-04 | 2024-05-07 | Taiho Pharmaceutical Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| US20180338922A1 (en) * | 2017-05-26 | 2018-11-29 | Esperion Therapeutics, Inc. | Fixed dose formulations |
| US10632092B2 (en) | 2017-08-30 | 2020-04-28 | First Fruits Business Ministry, Llc | Composition for and method to increase serum adiponectin and reduce body fat |
| CN111936137B (zh) | 2018-03-16 | 2023-09-08 | 安济药业公司 | 用于治疗严重便秘的组合物和方法 |
| EP4353222A1 (en) | 2018-03-19 | 2024-04-17 | Taiho Pharmaceutical Co., Ltd. | Use of sodium alkyl sulfate |
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| GB9613470D0 (en) | 1996-06-27 | 1996-08-28 | Ciba Geigy Ag | Small solid oral dosage form |
| DE19816070A1 (de) | 1998-04-09 | 1999-10-14 | Aventis Res & Tech Gmbh & Co | Retardtablette hergestellt aus linearen wasserunlöslichen Polysacchariden |
| KR100632339B1 (ko) * | 2001-12-21 | 2006-10-12 | 화이자 프로덕츠 인크. | 아지트로마이신의 직접적으로 압축가능한 제제 |
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| KR101219042B1 (ko) * | 2005-12-06 | 2013-01-07 | 삼성디스플레이 주식회사 | 반투과형 액정 표시 장치 |
| WO2007078726A2 (en) | 2005-12-16 | 2007-07-12 | Merck & Co., Inc. | Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin |
| PE20071315A1 (es) | 2006-03-06 | 2008-02-14 | Wyeth Corp | Formulaciones de compuestos derivados de fenilo y procesos de preparacion para tabletas que contienen dichos compuestos |
| US20070224258A1 (en) * | 2006-03-22 | 2007-09-27 | Bunick Frank J | Dosage forms having a randomized coating |
| PT2402319T (pt) * | 2006-03-31 | 2017-12-11 | Novartis Ag | Inibidores de dgat |
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- 2011-10-14 US US13/825,919 patent/US20130190354A1/en not_active Abandoned
- 2011-10-14 CA CA2813781A patent/CA2813781C/en active Active
- 2011-10-14 MX MX2013004162A patent/MX2013004162A/es not_active Application Discontinuation
- 2011-10-14 PE PE2013000837A patent/PE20140375A1/es not_active Application Discontinuation
- 2011-10-14 MA MA35806A patent/MA34599B1/fr unknown
- 2011-10-14 WO PCT/US2011/056275 patent/WO2012051488A1/en active Application Filing
- 2011-10-14 JP JP2013534025A patent/JP6060081B2/ja active Active
- 2011-10-14 SI SI201131677T patent/SI2627319T1/sl unknown
- 2011-10-14 EP EP11779278.8A patent/EP2627319B1/en active Active
- 2011-10-14 DK DK11779278.8T patent/DK2627319T3/da active
- 2011-10-14 ES ES11779278T patent/ES2712064T3/es active Active
- 2011-10-14 PT PT11779278T patent/PT2627319T/pt unknown
- 2011-10-14 RU RU2013121795/15A patent/RU2595866C2/ru active
- 2011-10-14 KR KR1020137009333A patent/KR20130100311A/ko not_active Withdrawn
- 2011-10-14 PL PL11779278T patent/PL2627319T3/pl unknown
- 2011-10-14 AU AU2011316003A patent/AU2011316003B2/en not_active Ceased
- 2011-10-14 CN CN201180049179.4A patent/CN103179957B/zh active Active
- 2011-10-14 SG SG2013021944A patent/SG189078A1/en unknown
- 2011-10-14 HU HUE11779278A patent/HUE043524T2/hu unknown
- 2011-10-14 BR BR112013008757-9A patent/BR112013008757A2/pt not_active IP Right Cessation
- 2011-10-14 TR TR2019/02435T patent/TR201902435T4/tr unknown
- 2011-10-14 NZ NZ608558A patent/NZ608558A/en not_active IP Right Cessation
- 2011-10-14 PH PH1/2013/500695A patent/PH12013500695A1/en unknown
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2013
- 2013-03-20 ZA ZA2013/02108A patent/ZA201302108B/en unknown
- 2013-03-21 IL IL225434A patent/IL225434A0/en unknown
- 2013-04-11 GT GT201300096A patent/GT201300096A/es unknown
- 2013-04-11 CO CO13094273A patent/CO6710915A2/es not_active Application Discontinuation
- 2013-04-12 CL CL2013001001A patent/CL2013001001A1/es unknown
- 2013-04-12 EC ECSP13012755 patent/ECSP13012755A/es unknown
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2015
- 2015-07-22 US US14/805,919 patent/US20150320687A1/en not_active Abandoned
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2016
- 2016-09-12 US US15/262,056 patent/US20160374947A1/en not_active Abandoned
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2018
- 2018-05-01 US US15/968,104 patent/US10646446B2/en active Active
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2020
- 2020-03-31 US US16/835,921 patent/US11304907B2/en active Active
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