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Tropisetron hydrochloride compound, its preparation method, and pharmaceutical composition containing the same

A technology of tropisetron hydrochloride and compounds, which is applied in the field of medicine, can solve problems such as unsatisfactory fluidity, and achieve the effects of improving fluidity, good stability, and improving quality

Active Publication Date: 2013-10-23
金鸿药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although its hygroscopicity and stability have been significantly improved according to the method of CN102351857A, the fluidity is still not satisfactory

Method used

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  • Tropisetron hydrochloride compound, its preparation method, and pharmaceutical composition containing the same
  • Tropisetron hydrochloride compound, its preparation method, and pharmaceutical composition containing the same
  • Tropisetron hydrochloride compound, its preparation method, and pharmaceutical composition containing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] [Example 1] Preparation of Tropisetron Hydrochloride Compound

[0053] 1) Take 50g of tropisetron hydrochloride raw material, add 150ml of mixed solvent of ethanol and tetrahydrofuran (the volume ratio of ethanol and tetrahydrofuran is 3:1), heat to 50°C, keep it warm for 30 minutes, filter while it is hot, and obtain the filtrate for later use ;

[0054] 2) Naturally cool the spare filtrate to room temperature;

[0055] 3) Add 30ml of ethyl acetate dropwise to the filtrate at a stirring speed of 20rpm, continue stirring for 30 minutes after dropping, let stand for 8 hours, filter to obtain a filter cake, wash the filter cake with ethanol, and then dry it under reduced pressure for 2 hours , to obtain the tropisetron hydrochloride compound. Yield 71.2%, HPLC content 99.95%.

[0056] The X-ray powder diffraction pattern of the tropisetron hydrochloride compound of gained is shown in figure 1 shown. It is measured by D / Max-2500.9161 X-ray diffractometer, measurement ...

Embodiment 2

[0057] [embodiment 2] preparation of tropisetron hydrochloride compound

[0058] 1) Take 50g of tropisetron hydrochloride raw material, add 350ml of mixed solvent of ethanol and tetrahydrofuran (the volume ratio of ethanol and tetrahydrofuran is 8:1), heat to 60°C, keep it warm for 15 minutes, filter while it is hot, and obtain the filtrate for later use ;

[0059] 2) Naturally cool the spare filtrate to room temperature;

[0060] 3) Add 43.75ml of ethyl acetate dropwise to the filtrate at a stirring speed of 30rpm, continue stirring for 20 minutes after dropping, let stand for 6 hours, filter to obtain a filter cake, wash the filter cake with ethanol, and then dry under reduced pressure 4h to obtain the tropisetron hydrochloride compound. Yield 71.6%, HPLC content 99.98%.

[0061] The X-ray powder diffraction pattern of the obtained tropisetron hydrochloride compound is consistent with the results of Example 1, and its assay method is the same as that of Example 1.

Embodiment 3

[0062] [embodiment 3] preparation of tropisetron hydrochloride compound

[0063] 1) Take 50g of tropisetron hydrochloride raw material, add 210ml of mixed solvent of ethanol and tetrahydrofuran (the volume ratio of ethanol and tetrahydrofuran is 6:1), heat to 55°C, keep it warm for 20 minutes, filter while it is hot, and obtain the filtrate for later use ;

[0064] 2) Naturally cool the spare filtrate to room temperature;

[0065] 3) Add 30ml of ethyl acetate dropwise to the filtrate at a stirring speed of 25rpm. After dropping, continue to stir for 25 minutes, let it stand for 7 hours, and filter to obtain a filter cake. The filter cake is washed with ethanol, and then dried under reduced pressure for 3 hours , to obtain the tropisetron hydrochloride compound. Yield 71.3%, HPLC content 99.96%.

[0066] The X-ray powder diffraction pattern of the obtained tropisetron hydrochloride compound is consistent with the results of Example 1, and its assay method is the same as that...

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Abstract

Belonging to the technical field of medicines, the invention particularly relates to a Tropisetron hydrochloride compound, its preparation method, and a pharmaceutical composition containing the same. The Tropisetron hydrochloride compound has a structural formula shown as formula (I), wherein, the Tropisetron hydrochloride compound adopts Cu-K alpha ray for characteristic X ray powder determination, the X ray powder atlas is as shown in figure 1. Compared with the prior art, the Tropisetron hydrochloride compound provided in the invention has a different crystal form, which has good stability and improved liquidity at the same time, thus improving the preparation quality.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tropisetron hydrochloride compound, a preparation method thereof and a pharmaceutical composition containing the compound. Background technique [0002] Tropisetron hydrochloride is the third 5-HT3 receptor antagonist on the market after ondansetron and granisetron. It was developed by the Swiss company Sandoz and was first launched in the Netherlands in 1992. The trade name is Navoban. , is the drug of choice for the treatment of nausea and vomiting, and is currently clinically used to prevent and treat nausea and vomiting caused by cancer chemotherapy. Compared with other 5-HT3 receptor antagonists, tropisetron has the characteristics of mild side effects, good tolerance, low drug-drug reaction and long duration of action. Single-dose administration, no tolerance, reproducible effect in each chemotherapy course; no extrapyramidal effects. With the recommended d...

Claims

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Application Information

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IPC IPC(8): C07D451/12A61K31/46A61P1/08
Inventor 上官清
Owner 金鸿药业股份有限公司
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