EP2603288A1 - Pharmaceutical granulate comprising imatinib mesylate - Google Patents
Pharmaceutical granulate comprising imatinib mesylateInfo
- Publication number
- EP2603288A1 EP2603288A1 EP10747433.0A EP10747433A EP2603288A1 EP 2603288 A1 EP2603288 A1 EP 2603288A1 EP 10747433 A EP10747433 A EP 10747433A EP 2603288 A1 EP2603288 A1 EP 2603288A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- imatinib mesylate
- granulate
- imatinib
- composition
- mesylate
- 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.)
- Withdrawn
Links
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61P35/00—Antineoplastic agents
Definitions
- WO 2006/121941 discloses a melt granulation process which comprises the steps of (a) forming a mixture of imatinib mesylate with at least one release retardant, e.g., a release retarding polymer, a plasticizer or a release modifier; (b) granulating the mixture using an extruder and (c) cooling the granules.
- a release retardant e.g., a release retarding polymer, a plasticizer or a release modifier
- US 2007/0036850 discloses a dry granulation (by compaction) process for the preparation of imatinib Form a or ⁇ granules prior to the tabletting process.
- the imatinib granule cores contain between 25 and 80% of imatinib together with filler-binder additives , e.g. with microcrystalline cellulose and crospovidone.
- the population of granules has an average size of between 250-800 ⁇ , as determined by sieve analysis.
- the invention provides a process for making a granulate comprising imatinib mesylate, which process comprises wetting imatinib mesylate with a granulation liquid, which is preferably water, ethanol and/or isopropanol and most preferably in an amount of 5 - 50 weight %, in respect to the mass of imatinib mesylate, and granulating the mixture in a suitable granulator, e.g. high shear or fluid bed granulator, followed by drying, and optionally sieving and/or milling of the produced population of granules.
- a suitable granulator e.g. high shear or fluid bed granulator
- the last aspect deals with the use of the pharmaceutical imatinib mesylate granulate of the present invention and/or a composition comprising it for making a medicament.
- compositions comprising imatinib mesylate and useful for making compressed dosage forms, such as tablets, comprises the step of granulation of imatinib with filler-binders excipients to yield a "composite" granulate, i.e. a granulate comprising imatinib and at least one granulate-forming excipient.
- the "wet granulation” as used herein is a process, which itself is well known in the art and comprises, within many technological variants, moistening a solid component or a mixture of solid components with a liquid, and vigorous mixing of the composition, whereby the wet particles of solids adhere together by cohesive forces to form larger, sometimes essentially spherical, agglomerates (a granulate).
- the excess of the granulation liquid may be removed from the raw granulate by drying and the suitable size range of particles is obtained by sieving and/or milling the population of granules.
- imatinib mesylate can be wet granulated without using any granulate-forming excipient, such as a filler and/or binder , to form a free flowing solid granulate material comprising ,based on a solvent-free basis, only imatinib (small amounts of used granulation liquid may be present).
- a granulation liquid which is preferably water and/or an alcohol, e.g. ethanol or isopropanol, and processing the mixture in a suitable granulator results in a stable free flowing granulate form of imatinib mesylate with suitable characteristics for further processing.
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/EP2010/005214 WO2012019633A1 (en) | 2010-08-11 | 2010-08-11 | Pharmaceutical granulate comprising imatinib mesylate |
Publications (1)
Publication Number | Publication Date |
---|---|
EP2603288A1 true EP2603288A1 (en) | 2013-06-19 |
Family
ID=44065563
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP10747433.0A Withdrawn EP2603288A1 (en) | 2010-08-11 | 2010-08-11 | Pharmaceutical granulate comprising imatinib mesylate |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP2603288A1 (es) |
MX (1) | MX2013001653A (es) |
RU (1) | RU2013110058A (es) |
WO (1) | WO2012019633A1 (es) |
ZA (1) | ZA201300872B (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9750700B2 (en) * | 2011-06-22 | 2017-09-05 | Natco Pharma Limited | Imatinib mesylate oral pharmaceutical composition and process for preparation thereof |
US20160015708A1 (en) * | 2012-02-21 | 2016-01-21 | Ranbaxy Laboratories Limited | Stable dosage forms of imatinib mesylate |
EP2749271A1 (en) * | 2012-12-31 | 2014-07-02 | Deva Holding Anonim Sirketi | Optimized manufacturing method and pharmaceutical formulation of imatinib |
ES2683361T3 (es) | 2013-05-14 | 2018-09-26 | Hetero Research Foundation | Composiciones de Imatinib |
EP3019159A4 (en) * | 2013-07-09 | 2017-01-18 | Shilpa Medicare Limited | Oral pharmaceutical compositions comprising imatinib mesylate |
EP3257499A1 (en) | 2016-06-17 | 2017-12-20 | Vipharm S.A. | Process for preparation of imatinib methanesulfonate capsules |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW225528B (es) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
GB0209265D0 (en) * | 2002-04-23 | 2002-06-05 | Novartis Ag | Organic compounds |
WO2006040779A2 (en) | 2004-10-11 | 2006-04-20 | Natco Pharma Limited | Controlled release gastric floating matrix formulation containing imatinib |
MY148074A (en) | 2005-05-10 | 2013-02-28 | Novartis Ag | Pharmaceutical compositions comprising imatinib and a release retardant |
DE502006005084D1 (de) | 2005-08-15 | 2009-11-26 | Siegfried Generics Int Ag | Filmtablette oder Granulat enthaltend ein Pyridylpyrimidin |
PL390611A1 (pl) * | 2010-03-04 | 2011-09-12 | Tomasz Koźluk | Sposób otrzymywania polimorficznej formy alfa i nowa forma polimorficzna mesylanu imatinibu |
WO2011121593A1 (en) * | 2010-03-29 | 2011-10-06 | Hetero Research Foundation | Stable pharmaceutical composition of imatinib |
-
2010
- 2010-08-11 RU RU2013110058/15A patent/RU2013110058A/ru unknown
- 2010-08-11 EP EP10747433.0A patent/EP2603288A1/en not_active Withdrawn
- 2010-08-11 MX MX2013001653A patent/MX2013001653A/es unknown
- 2010-08-11 WO PCT/EP2010/005214 patent/WO2012019633A1/en active Application Filing
-
2013
- 2013-02-01 ZA ZA2013/00872A patent/ZA201300872B/en unknown
Non-Patent Citations (2)
Title |
---|
None * |
See also references of WO2012019633A1 * |
Also Published As
Publication number | Publication date |
---|---|
RU2013110058A (ru) | 2014-09-20 |
MX2013001653A (es) | 2013-05-22 |
ZA201300872B (en) | 2014-04-30 |
WO2012019633A1 (en) | 2012-02-16 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP4875001B2 (ja) | アリピプラゾールの湿式造粒医薬組成物 | |
EP2988733B1 (en) | Pharmaceutical composition containing crystalline macitentan | |
WO2012019633A1 (en) | Pharmaceutical granulate comprising imatinib mesylate | |
JP6804585B2 (ja) | 医薬剤形 | |
MX2009002336A (es) | Composiciones de imatinib. | |
AU2009235426A1 (en) | Granulation of active pharmaceutical ingredients | |
CN113939289A (zh) | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 | |
CA2737380C (en) | Tabletting excipient based on lactose and cellulose | |
EP3860606A1 (en) | Pharmaceutical composition comprising lenvatinib esylate or tosylate | |
TWI794214B (zh) | 包含5-氯-n4-[2-(二甲基磷醯基)苯基]-n2-{2-甲氧基-4-[4-(4-甲基哌嗪-1-基)哌啶-1-基]苯基}嘧啶-2,4-二胺之醫藥調配物 | |
JP2017520619A (ja) | セリチニブ製剤 | |
EP3731817A1 (en) | Pharmaceutical composition of lenalidomide pharmaceutically acceptable acid addition salt | |
JP4774739B2 (ja) | 漢方エキス含有錠剤組成物およびその製造方法 | |
KR20110104059A (ko) | 경구 생체이용률이 낮은 화합물의 예비압축된 신속-붕해 제형 | |
CA2924016A1 (en) | Pharmaceutical composition | |
CN112057427A (zh) | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 | |
JP6199922B2 (ja) | 化学的な安定性が向上したイルベサルタン含有錠剤 | |
CN115212176B (zh) | 泽布替尼缓释片剂 | |
WO2022042646A1 (zh) | 盐酸鲁拉西酮组合物及其制备方法 | |
RU2183119C1 (ru) | Фармацевтическая композиция, обладающая спазмолитической активностью, способ ее получения | |
JP2021167306A (ja) | 崩壊性粒子の製造方法 | |
KR20240055103A (ko) | 벰페도산의 약학 조성물 | |
WO2023158411A1 (en) | A tablet of tolvaptan and at least one binder processed with wet granulation | |
RU2289422C2 (ru) | Фармацевтическая композиция на основе ноопепта | |
JP2019189554A (ja) | 溶出性を改善させた医薬組成物 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
17P | Request for examination filed |
Effective date: 20130311 |
|
AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR |
|
DAX | Request for extension of the european patent (deleted) | ||
17Q | First examination report despatched |
Effective date: 20160414 |
|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
|
18D | Application deemed to be withdrawn |
Effective date: 20190206 |