ES2639995T3 - Formulación farmacéutica que comprende ezetimiba - Google Patents
Formulación farmacéutica que comprende ezetimiba Download PDFInfo
- Publication number
- ES2639995T3 ES2639995T3 ES08859677.0T ES08859677T ES2639995T3 ES 2639995 T3 ES2639995 T3 ES 2639995T3 ES 08859677 T ES08859677 T ES 08859677T ES 2639995 T3 ES2639995 T3 ES 2639995T3
- Authority
- ES
- Spain
- Prior art keywords
- weight
- ezetimibe
- pharmaceutical formulation
- particle size
- article
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Links
- OLNTVTPDXPETLC-XPWALMASSA-N ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 title abstract description 5
- 229960000815 ezetimibe Drugs 0.000 title abstract description 5
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000002245 particle Substances 0.000 abstract description 5
- 238000000034 method Methods 0.000 abstract description 4
- 239000000843 powder Substances 0.000 abstract description 2
- 239000011230 binding agent Substances 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000007884 disintegrant Substances 0.000 abstract 1
- 239000000314 lubricant Substances 0.000 abstract 1
- 239000008137 solubility enhancer Substances 0.000 abstract 1
- 229920002261 Corn starch Polymers 0.000 description 8
- 239000008120 corn starch Substances 0.000 description 8
- 229940099112 cornstarch Drugs 0.000 description 8
- 239000008187 granular material Substances 0.000 description 8
- 239000000203 mixture Substances 0.000 description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 238000005538 encapsulation Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 229960001021 lactose monohydrate Drugs 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 239000012064 sodium phosphate buffer Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Obesity (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
Abstract
Una composición farmacéutica que comprende: del 5 al 20 % en peso de ezetimiba, del 50 al 85 % en peso de diluyente, del 3 al 25 % en peso de disgregante, del 2 al 5 % en peso de potenciador de solubilidad del 1 al 10 % en peso de aglutinante, y del 0,5 al 1 % en peso de lubricante, caracterizada por que la ezetimiba tiene una distribución del tamaño de partícula de d(0,9) de 9 μm a 20 μm y de d(0,5) de 4 μm a 10 μm, en la que el tamaño de partícula se determina por difracción láser usando el "método en polvo húmedo".
Description
*Medio de disolución diferente: Tampón fosfato sódico 0,01 M pH 7 + SLS al 0,5 % 50 rpm, 900 ml
Ejemplo 3 (Ejemplo de referencia)
Formulación de acuerdo con la presente divulgación
1 Ezetimiba 10 2 Lactosa monohidrato 71 3 Almidón de maíz 13 4 Pasta de almidón de maíz usando 5 partes de 5
agua purificada 5 Estearato de magnesio 1 Peso total del comprimido 100 5 Método de fabricación:
Dispersar artículo N.º 4 en agua fría (1 parte de almidón de maíz con respecto a 5 partes de agua). Calentar la mezcla a aproximadamente 95 °C para formar una past a y enfriar a aproximadamente 50 ºC. Mezclar el artículo N.º
10 1, 2 y 3 en una mezcladora adecuada durante 10 a 15 minutos y granular con pasta de almidón de maíz. Moler los gránulos húmedos de un tamiz grueso, si es necesario. Secar los gránulos húmedos. Tamizar los gránulos secos a través de una malla apropiada (malla n.º 30), si es necesario, y mezclar con el artículo N.º 5 durante 3-5 minutos. Comprimir la mezcla hasta un tamaño y peso apropiados en una máquina de comprimidos adecuada o rellenar en cápsulas de gelatina dura adecuadas en una máquina de encapsulación adecuada.
15 La velocidad de disolución a los 30 minutos de los comprimidos del ejemplo 3 mostró más del 90 % de liberación de fármaco, por lo tanto, puede usarse el aumento de la cantidad de pasta y la reducción de la cantidad de agua según el estado de la técnica para mejorar problemas relacionados con el proceso sin afectar a la liberación del fármaco.
Formulación de acuerdo con la presente divulgación
1 Ezetimiba 10 2 Lactosa monohidrato 51 3 Celulosa microcristalina 20 4 Almidón de maíz 13 5 Pasta de almidón de maíz usando 5 partes de 5
agua purificada
6 Estearato de magnesio 1 Peso total del comprimido 100
Método de fabricación:
25 Dispersar artículo N.º 5 en agua fría (1 parte de almidón de maíz con respecto a 5 partes de agua). Calentar la mezcla a aproximadamente 95 °C para formar una past a y enfriar a aproximadamente 50 ºC. Mezclar el artículo N.º 1, 2, 3 y 4 en una mezcladora adecuada durante 10 a 15 minutos y granular con pasta de almidón de maíz. Moler los gránulos húmedos de un tamiz grueso, si es necesario, secar los gránulos húmedos. Tamizar los gránulos secos a
30 través de una malla apropiada (malla n.º 30), si es necesario, y mezclar con el artículo N.º 5 durante 3-5 minutos. Comprimir la mezcla hasta un tamaño y peso apropiados en una máquina de comprimidos adecuada o rellenar en cápsulas de gelatina dura adecuadas en una máquina de encapsulación adecuada.
Ejemplo 5
a) Determinación del tamaño de partícula de acuerdo con el "método en polvo seco".
40 Condiciones instrumentales típicas: A) Instrumento: Analizador del tamaño de partícula Malvern "Master sizer S" B) Lente de alcance: 300 mm C) Longitud del haz: 10 mm
8
11
Claims (1)
-
imagen1 imagen2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2579DE2007 | 2007-12-10 | ||
| INDE25792007 | 2007-12-10 | ||
| PCT/EP2008/010431 WO2009074286A2 (en) | 2007-12-10 | 2008-12-09 | Pharmaceutical formulation comprising ezetimibe |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2639995T3 true ES2639995T3 (es) | 2017-10-31 |
Family
ID=40416944
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08859677.0T Active ES2639995T3 (es) | 2007-12-10 | 2008-12-09 | Formulación farmacéutica que comprende ezetimiba |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8858994B2 (es) |
| EP (2) | EP2965752A1 (es) |
| CA (1) | CA2708159C (es) |
| EA (1) | EA022269B1 (es) |
| ES (1) | ES2639995T3 (es) |
| UA (1) | UA103179C2 (es) |
| WO (1) | WO2009074286A2 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3379591A1 (en) | 1999-12-01 | 2018-09-26 | The Trustees of Princeton University | Complexes of form l2mx |
| EP2127641A1 (en) | 2008-05-26 | 2009-12-02 | Inke, S.A. | Micronisable form of salmeterol xinafoate |
| EP2216016A1 (en) * | 2009-02-06 | 2010-08-11 | LEK Pharmaceuticals d.d. | Process for the preparation of a pharmaceutical composition comprising ezetimibe |
| HUP1000327A2 (en) | 2010-06-18 | 2012-01-30 | Druggability Technologies Ip Holdco Jersey Ltd | Composition containing nanostructured ezetibime and process for it's preparation |
| EP2468258A1 (en) * | 2010-12-22 | 2012-06-27 | LEK Pharmaceuticals d.d. | Process for the preparation of a pharmaceutical composition comprising a low soluble pharmaceutically active ingredient |
| WO2013066279A1 (en) * | 2011-10-13 | 2013-05-10 | Mahmut Bilgic | Solid dosage forms comprising ezetimibe |
| CN104173307A (zh) * | 2014-08-29 | 2014-12-03 | 四川制药制剂有限公司 | 依折麦布片剂的制备方法 |
| CA2978204A1 (en) | 2015-03-13 | 2016-09-22 | Esperion Therapeutics, Inc. | Fixed dose combinations and formulations comprising etc1002 and ezetimibe and methods of treating or reducing the risk of cardiovascular disease |
| 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 |
| EP3437636A1 (en) | 2017-08-02 | 2019-02-06 | Adamed sp. z o.o. | Pharmaceutical composition comprising ezetimibe |
| US11622939B2 (en) * | 2017-11-23 | 2023-04-11 | Zhejiang Hisun Pharmaceutical Co., Ltd. | HS-25 tablet and preparation method therefor |
| WO2021220236A1 (en) * | 2020-05-01 | 2021-11-04 | Cadila Healthcare Limited | Pharmaceutical compositions for combination therapy |
| WO2024041746A1 (en) * | 2022-08-22 | 2024-02-29 | Newamsterdam Pharma B.V. | Fixed dose combination composition of obicetrapib and ezetimibe |
| WO2024042061A1 (en) * | 2022-08-22 | 2024-02-29 | Newamsterdam Pharma B.V. | Obicetrapib and ezetimibe combination treatment and fixed dose pharmaceutical compositions |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5631365A (en) | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
| JPH10501811A (ja) | 1994-06-20 | 1998-02-17 | シェーリング コーポレイション | 低コレステロール化剤として有用な置換アゼチジノン化合物 |
| SK287988B6 (sk) | 2001-01-26 | 2012-09-03 | Schering Corporation | Composition, oral dosage form and use thereof |
| US9173847B2 (en) * | 2003-10-10 | 2015-11-03 | Veloxis Pharmaceuticals A/S | Tablet comprising a fibrate |
| JP2007526251A (ja) | 2004-12-03 | 2007-09-13 | テバ ファーマシューティカル インダストリーズ リミティド | エゼチミベ多形体 |
| EP1741427A1 (en) | 2005-07-06 | 2007-01-10 | KRKA, D.D., Novo Mesto | Pharmaceutical composition comprising simvastatin and ezetimibe |
| US20070049748A1 (en) | 2005-08-26 | 2007-03-01 | Uppala Venkata Bhaskara R | Preparation of ezetimibe |
| EP1849459A1 (en) | 2006-03-06 | 2007-10-31 | Teva Pharmaceutical Industries Ltd. | Ezetimibe compositions |
| US20070275052A1 (en) | 2006-05-24 | 2007-11-29 | Glenmark Pharmaceuticals Limited | Pharmaceutical compositions containing sterol inhibitors |
| WO2008032338A2 (en) | 2006-09-11 | 2008-03-20 | Manne Satyanarayana Reddy | Improved process for the preparation of ezetimibe and its intermediates |
| CN103203185B (zh) | 2007-01-20 | 2016-01-13 | 戴斯分析公司 | 具有包含经加热空气的干燥腔室的干燥器 |
| EP2125715A2 (en) | 2007-01-24 | 2009-12-02 | Krka | Process for the preparation of ezetimibe and derivatives thereof |
| EP2120882A2 (en) | 2007-02-23 | 2009-11-25 | Krka | Pharmaceutical composition containing a cholesterol absorption inhibitor |
| EP2231118B2 (en) * | 2007-12-17 | 2017-05-17 | KRKA, tovarna zdravil, d.d., Novo mesto | Suspension comprising non-micronized ezetimibe micro-particles |
-
2008
- 2008-12-09 ES ES08859677.0T patent/ES2639995T3/es active Active
- 2008-12-09 CA CA2708159A patent/CA2708159C/en active Active
- 2008-12-09 US US12/747,270 patent/US8858994B2/en active Active
- 2008-12-09 EP EP15171262.7A patent/EP2965752A1/en active Pending
- 2008-12-09 WO PCT/EP2008/010431 patent/WO2009074286A2/en active Application Filing
- 2008-12-09 EP EP08859677.0A patent/EP2217214B1/en active Active
- 2008-12-09 UA UAA201007034A patent/UA103179C2/ru unknown
- 2008-12-09 EA EA201000752A patent/EA022269B1/ru not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009074286A3 (en) | 2009-07-30 |
| EP2217214A2 (en) | 2010-08-18 |
| EP2965752A1 (en) | 2016-01-13 |
| UA103179C2 (ru) | 2013-09-25 |
| WO2009074286A2 (en) | 2009-06-18 |
| EA201000752A1 (ru) | 2010-12-30 |
| CA2708159A1 (en) | 2009-06-18 |
| EA022269B1 (ru) | 2015-12-30 |
| EP2217214B1 (en) | 2017-07-19 |
| US8858994B2 (en) | 2014-10-14 |
| US20100291207A1 (en) | 2010-11-18 |
| CA2708159C (en) | 2016-01-26 |
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