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PHARMACEUTICAL GRANULATE CONTAINING IMATINIB MESILATE
专利权人:
СИНТОН Б.В. (NL)
发明人:
ВАН ДЕН ХЕВЕЛ Денни Йохан Марейн (NL)
申请号:
RU2013110058/15
公开号:
RU2013110058A
申请日:
2010.08.11
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. 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 91. 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 кристалл
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中国工程科技知识中心
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