Crystal system of chlorhydric acid palonosetron and preparation method thereof

A technology of palonosetron and hydrochloric acid, which is applied in the field of crystal forms of palonosetron hydrochloride and its preparation, can solve the problems of unmentioned crystal form spectral characteristics, unmentioned palonosetron hydrochloride crystal forms and preparation method etc.

Inactive Publication Date: 2008-09-03
HANGZHOU JIUYUAN GENE ENG +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, the above-mentioned documents do not mention the crystal form and preparation method

Method used

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  • Crystal system of chlorhydric acid palonosetron and preparation method thereof
  • Crystal system of chlorhydric acid palonosetron and preparation method thereof
  • Crystal system of chlorhydric acid palonosetron and preparation method thereof

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Embodiment 1

[0036] The preparation of embodiment 1 palonosetron hydrochloride A crystal form one

[0037]Take 5 g of palonosetron hydrochloride, add 115 ml of isopropanol and 4 ml of water, and heat to dissolve it. After all the solids are dissolved, continue heating, distill 36ml of liquid under normal pressure, cool to 0°C, stir, crystallize for 2 hours, filter after crystallization, and vacuum dry at 80°C for 4 hours to obtain 4.4g of pure crystals. The purity by HPLC was 99.7%.

Embodiment 2

[0038] The preparation of embodiment 2 palonosetron hydrochloride A crystal form two

[0039] Take 8 g of palonosetron hydrochloride, add 124 ml of isopropanol and 6.4 ml of water, and heat to dissolve it. After all the solids were dissolved, 54ml of isopropanol was added, cooled to 0°C, stirred, crystallized for 4 hours, filtered after crystallization, and vacuum-dried at 80°C for 4 hours to obtain 7.56g of pure crystals, the purity of which was determined by HPLC as 99.6%.

Embodiment 3

[0040] The preparation of embodiment 3 palonosetron hydrochloride B crystal form one

[0041] Take 5 g of palonosetron hydrochloride, add 200 ml of ethanol, heat to dissolve the solid, cool, stir and crystallize at 10°C for 2 hours, filter, and dry in vacuum at 80°C for 4 hours to obtain 4.3 grams of pure crystals, which are detected by HPLC The purity is 99.2%.

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Abstract

The invention relates to two novel crystal forms of palonosetron hydrochloride that are A and B crystal forms. The A and B crystal forms have characteristic diffraction peaks when x-ray diffraction is used on the powder under Cu-K alpha radiation conditional (lamed=1. 54059) and the bragg 2theta angle between 0 and 50 degree C. The A crystal form has aendothermic peak near 320. 678 degree C, and the B crystal form has a endothermic peak near 320. 68 degree C after performed differential thermal analysis. Further the invention also relates to a process for preparing the crystal forms and pharmaceutical compositions containing the crystal forms.

Description

technical field [0001] The present invention relates to a crystal form of palonosetron hydrochloride, a preparation method thereof and a pharmaceutical composition containing these crystal forms. Background of the invention [0002] Palonosetron hydrochloride (Palonosetron hydrochloride, trade name Aloxi) is a selective 5-HT3 receptor antagonist developed by Switzerland Helsinn company, chemical name: (3aS)-2-[(3S)-1-aza The molecular structure of bicyclo[2.2.2]octyl]-2,3,3a,4,5,6-hexahydro-1-oxo-1H-phenylhydrazine[de]isoquinoline hydrochloride is as follows. On July 25, 2003, the product was approved by the US Food and Drug Administration (FDA) for the treatment of acute and delayed nausea and vomiting caused by moderate or highly emetogenic chemotherapy. [0003] [0004] Palonosetron hydrochloride is the fourth approved 5-HT 3 receptor antagonists. An important feature of palonosetron is its long half-life, about 40 hours, while other 5-HT 3 Receptor antagonists ha...

Claims

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Application Information

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IPC IPC(8): C07D453/02A61K31/473A61P1/08
Inventor 陈学军张海欧李勇徐飞虎孙汉栋
Owner HANGZHOU JIUYUAN GENE ENG
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