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Tropisetron hydrochloride composition injection capable of treating nausea and vomiting caused by chemotherapy

A technology for tropisetron hydrochloride and water injection, applied in the field of medicine, can solve the problems of affecting stability, difficult preparation of preparations, unsatisfactory hygroscopicity of crystal forms of impurity content and the like

Inactive Publication Date: 2015-11-25
QINGDAO HUAZHICAO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, there have been many studies on the crystal form of tropisetron hydrochloride, but the impurity content, stability and hygroscopicity of the crystal form are still not ideal, which affects its own stability and also brings problems to the preparation of the preparation. here comes the difficulty

Method used

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  • Tropisetron hydrochloride composition injection capable of treating nausea and vomiting caused by chemotherapy
  • Tropisetron hydrochloride composition injection capable of treating nausea and vomiting caused by chemotherapy
  • Tropisetron hydrochloride composition injection capable of treating nausea and vomiting caused by chemotherapy

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1: Preparation of Tropisetron Hydrochloride Crystals

[0024] (1) Dissolving the crude product of tropisetron hydrochloride into a mixed solution of methanol and carbon tetrachloride whose volume is 10 times the weight of tropisetron hydrochloride at 35°C, the volume ratio of methanol and carbon tetrachloride is 4 :2.5;

[0025] (2) adding activated carbon whose weight is 0.2 times the weight of tropisetron hydrochloride for decolorization, and filtering to obtain tropisetron hydrochloride solution;

[0026] (3) Heat up the tropisetron hydrochloride solution to 45°C, and add dichloromethane dropwise to the tropisetron hydrochloride solution under stirring conditions, the volume of dichloromethane is 8 times the weight of tropisetron hydrochloride, 0.5 The uniform dropwise addition is completed within h, and the stirring rate is 30rmp;

[0027] (4) After the dropwise addition, cool down to -15°C at a rate of 15°C / hour, continue to stir at a stirring rate of 1...

Embodiment 2

[0029] Example 2: The preparation method of tropisetron hydrochloride composition

[0030] The composition is: 1 part by weight of tropisetron hydrochloride crystal prepared by the present invention, and 0.3 part by weight of calcium chloride.

[0031] The preparation method is:

[0032] Get the prescribed amount of tropisetron hydrochloride and calcium chloride, add water for injection to dissolve, add 1% activated carbon of tropisetron hydrochloride weight and stir at room temperature for 30 minutes, filter to remove carbon, add water for injection to the filtrate to 2000ml, pass through 0.22 μm Filter the membrane, pack into 2ml ampoules, sterilize by autoclaving at 121°C for 45 minutes, and inspect with light to obtain tropisetron hydrochloride aqueous injection.

Embodiment 3

[0033] Example 3: Preparation of tropisetron hydrochloride composition

[0034] The composition is: 1 part by weight of tropisetron hydrochloride crystal prepared by the present invention, and 0.4 part by weight of calcium chloride.

[0035] The preparation method is:

[0036] Get the prescribed amount of tropisetron hydrochloride and calcium chloride, add water for injection to dissolve, add 1% activated carbon of tropisetron hydrochloride weight and stir at room temperature for 30 minutes, filter to remove carbon, add water for injection to the filtrate to 2000ml, pass through 0.22 μm Filter the membrane, pack into 2ml ampoules, sterilize by autoclaving at 121°C for 45 minutes, and inspect with light to obtain tropisetron hydrochloride aqueous injection.

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PUM

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Abstract

The invention relates to tropisetron hydrochloride composition injection capable of treating nausea and vomiting caused by chemotherapy, belonging to the technical field of medicines. The composition injection is composed of tropisetron hydrochloride and calcium chloride, wherein tropisetron hydrochloride is crystal, and an X-ray powder diffraction diagram obtained by Cu-Kalpha ray measurement is shown as figure I. The novel crystal form of tropisetron hydrochloride provided by the invention is different from the crystal structure in the prior art, through experimental verification, the inventor surprisingly finds that the compound with the novel crystal form is high in purity, good in mobility, high in stability, low in impurity content, and safe and reliable in clinic application, the moisture absorption probability is small, and the injection prepared by adopting the compound with the novel crystal is simple in component and good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to an aqueous injection of a tropisetron hydrochloride composition for treating nausea and vomiting caused by chemotherapy. Background technique [0002] Tropisetron hydrochloride is a selective peripheral neuron and central nervous system 5-hydroxytryptamine receptor antagonist, which can selectively block the vomiting reflex center, the excitation of peripheral neuron presynaptic 5-hydroxytryptamine receptors, and act on afferent The 5-hydroxytryptamine receptor active in the vagus nerve in the postrema area of ​​the central nervous system can prevent and treat nausea and vomiting caused by chemotherapy without causing extrapyramidal adverse reactions. [0003] In the prior art, there have been many studies on the crystal form of tropisetron hydrochloride, but the impurity content, stability and hygroscopicity of the crystal form are still not ideal, which affects its own stability ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/46C07D451/12A61P1/08
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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