RU2013110058A - PHARMACEUTICAL GRANULATE CONTAINING IMATINIB MESILATE - Google Patents
PHARMACEUTICAL GRANULATE CONTAINING IMATINIB MESILATE Download PDFInfo
- Publication number
- RU2013110058A RU2013110058A RU2013110058/15A RU2013110058A RU2013110058A RU 2013110058 A RU2013110058 A RU 2013110058A RU 2013110058/15 A RU2013110058/15 A RU 2013110058/15A RU 2013110058 A RU2013110058 A RU 2013110058A RU 2013110058 A RU2013110058 A RU 2013110058A
- Authority
- RU
- Russia
- Prior art keywords
- imatinib mesylate
- granulate
- composition
- granulator
- liquid
- Prior art date
Links
- 239000008187 granular material Substances 0.000 title claims abstract 22
- 229960002411 imatinib Drugs 0.000 title claims 2
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 title claims 2
- YLMAHDNUQAMNNX-UHFFFAOYSA-N imatinib methanesulfonate Chemical compound CS(O)(=O)=O.C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 YLMAHDNUQAMNNX-UHFFFAOYSA-N 0.000 claims abstract 26
- 229960003685 imatinib mesylate Drugs 0.000 claims abstract 22
- 239000000203 mixture Substances 0.000 claims abstract 13
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract 12
- 239000007788 liquid Substances 0.000 claims abstract 10
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims abstract 8
- 238000000034 method Methods 0.000 claims abstract 8
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims abstract 6
- 238000005469 granulation Methods 0.000 claims abstract 6
- 230000003179 granulation Effects 0.000 claims abstract 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 3
- 239000013078 crystal Substances 0.000 claims abstract 2
- 238000001035 drying Methods 0.000 claims abstract 2
- -1 ethanol Chemical compound 0.000 claims abstract 2
- 238000000227 grinding Methods 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 230000001376 precipitating effect Effects 0.000 claims abstract 2
- 238000007873 sieving Methods 0.000 claims abstract 2
- 239000002904 solvent Substances 0.000 claims abstract 2
- 238000009736 wetting Methods 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 1
- 238000007580 dry-mixing Methods 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
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
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)
Abstract
1. Гранулят, содержащий 95-99% иматиниба мезилата и 1-5% летучей жидкости.2. Гранулят по п.1, где иматиниба мезилат представляет собой кристаллический иматиниба мезилат, предпочтительно кристаллический иматиниба мезилат формы α, получаемый путем осаждения кристаллического иматиниба мезилата формы α из раствора иматиниба мезилата в растворителе, отличном от метанола, таком как этанол, и без добавления затравочного кристалла β-кристаллической формы иматиниба мезилата.3. Гранулят по п.1 или 2, где летучая жидкость представляет собой воду, этанол, изопропанол и их смеси.4. Гранулят по п.1, состоящий из гранул, имеющих средний размер 250-800 мкм.5. Способ получения гранулята иматиниба мезилата, который включает смачивание иматиниба мезилата жидкостью для грануляции и грануляцию смеси в грануляторе с последующим высушиванием, и необязательно просеивание и/или измельчение полученной совокупности гранул.6. Способ по п.5, где жидкостью для грануляции является вода, этанол и/или изопропанол.7. Способ по п.5 или 6, где количество жидкости для грануляции составляет 5-50 масс.% относительно массы иматиниба мезилата.8. Способ по п.5, где гранулятор представляет собой гранулятор с высоким сдвиговым усилием или гранулятор с псевдоожиженным слоем.9. Фармацевтическая композиция для перорального введения иматиниба мезилата, содержащая гранулят иматиниба мезилата по пп.1-4 и/или изготовленная по пп.5-8, и необязательно по меньшей мере один фармацевтически приемлемый эксципиент.10. Композиция по п.9 в форме таблетки.11. Композиция по п.9 или 10, содержащая по меньшей мере 50 масс.%, более предпочтительно по меньшей мере 60 масс.% гранулята.12. Композиция по п.91. Granulate containing 95-99% imatinib mesylate and 1-5% volatile liquid. 2. The granulate according to claim 1, wherein the imatinib mesylate is crystalline imatinib mesylate, preferably crystalline imatinib mesylate form α, obtained by precipitating crystalline imatinib mesylate form α from a solution of imatinib mesylate in a solvent other than methanol, such as ethanol, and without the addition of a seed crystal. β-crystalline form of imatinib mesylate. 3. The granulate according to claim 1 or 2, wherein the volatile liquid is water, ethanol, isopropanol and mixtures thereof. The granulate according to claim 1, consisting of granules having an average size of 250-800 microns. A method for producing imatinib mesylate granulate, which comprises wetting imatinib mesylate with granulation liquid and granulating the mixture in a granulator, followed by drying, and optionally sieving and / or grinding the resulting granule set. 6. The method of claim 5, wherein the granulation liquid is water, ethanol and / or isopropanol. The method according to claim 5 or 6, where the amount of liquid for granulation is 5-50 wt.% Relative to the weight of imatinib mesylate. The method of claim 5, wherein the granulator is a high shear granulator or a fluidized bed granulator. A pharmaceutical composition for oral administration of imatinib mesylate containing imatinib mesylate granules according to claims 1-4 and / or manufactured according to claims 5-8, and optionally at least one pharmaceutically acceptable excipient. 10. The composition of claim 9 in tablet form. A composition according to claim 9 or 10, containing at least 50 wt.%, More preferably at least 60 wt.% Of the granulate. The composition according to claim 9
Claims (18)
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 |
|---|---|
| RU2013110058A true RU2013110058A (en) | 2014-09-20 |
Family
ID=44065563
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013110058/15A RU2013110058A (en) | 2010-08-11 | 2010-08-11 | PHARMACEUTICAL GRANULATE CONTAINING IMATINIB MESILATE |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP2603288A1 (en) |
| MX (1) | MX2013001653A (en) |
| RU (1) | RU2013110058A (en) |
| WO (1) | WO2012019633A1 (en) |
| ZA (1) | ZA201300872B (en) |
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 |
| IN2014DN07898A (en) * | 2012-02-21 | 2015-04-24 | Ranbaxy Lab Ltd | |
| EP2749271A1 (en) * | 2012-12-31 | 2014-07-02 | Deva Holding Anonim Sirketi | Optimized manufacturing method and pharmaceutical formulation of imatinib |
| EP2803353B1 (en) | 2013-05-14 | 2018-05-23 | Hetero Research Foundation | Compositions of Imatinib |
| AU2014288866B2 (en) * | 2013-07-09 | 2017-07-13 | 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 |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (en) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| CO4940418A1 (en) | 1997-07-18 | 2000-07-24 | Novartis Ag | MODIFICATION OF A CRYSTAL OF A DERIVATIVE OF N-PHENYL-2-PIRIMIDINAMINE, PROCESSES FOR ITS MANUFACTURE AND USE |
| 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 |
| ES2334933T3 (en) | 2005-08-15 | 2010-03-17 | Siegfried Generics International Ag | COVERED OR GRANULATED TABLET CONTAINING A PYRIDYL PIRIMIDINE. |
| PL390611A1 (en) * | 2010-03-04 | 2011-09-12 | Tomasz Koźluk | Process for the preparation of polymorphic alpha form and new polymorphic form of imatinib mesylate |
| EP2552447A4 (en) * | 2010-03-29 | 2013-09-11 | Hetero Research Foundation | Stable pharmaceutical composition of imatinib |
-
2010
- 2010-08-11 RU RU2013110058/15A patent/RU2013110058A/en unknown
- 2010-08-11 EP EP10747433.0A patent/EP2603288A1/en not_active Withdrawn
- 2010-08-11 MX MX2013001653A patent/MX2013001653A/en unknown
- 2010-08-11 WO PCT/EP2010/005214 patent/WO2012019633A1/en not_active Ceased
-
2013
- 2013-02-01 ZA ZA2013/00872A patent/ZA201300872B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012019633A1 (en) | 2012-02-16 |
| MX2013001653A (en) | 2013-05-22 |
| EP2603288A1 (en) | 2013-06-19 |
| ZA201300872B (en) | 2014-04-30 |
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