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Tropiseiron hydrochloride compound

A technology of tropisetron hydrochloride and compounds, which is applied in the field of medicine and can solve problems such as ineffective treatment of patients

Active Publication Date: 2013-06-12
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, chemotherapy and radiotherapy are still the main means of anti-tumor, but because they can cause nausea and vomiting, the treatment of patients often cannot be carried out effectively.

Method used

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  • Tropiseiron hydrochloride compound
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  • Tropiseiron hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] In a 1000ml reaction bottle equipped with stirring, thermometer, and condenser, add 80g of tropisetron hydrochloride (1 refined product) and 560ml of acetone-water (8:2) mixture, start stirring, and heat up to 60 ℃-65℃, wait until it is completely dissolved, keep it warm for 30 minutes, and filter while it is hot. The filtrate was naturally cooled to room temperature, and then kept warm for 2 hours to precipitate crystals, filter, and dry to obtain high-purity tropisetron hydrochloride crystals, melting point: 280.1°C-281.1°C, purity 99.96% (HPLC normalization method), solvent residue The detection meets the requirements.

[0049] Elemental Analysis Results:

[0050]Measured value (calculated value), C:63.64(63.57),H:6.60(6.62),N:8.73(8.72),

[0051] Cl: 11.05(11.01);

[0052] The X-ray diffraction pattern of the crystal is shown in FIG. 1 . Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50 ° ; ...

Embodiment 2

[0055] Use standard, routine technology to prepare the injection containing tropisetron hydrochloride compound of the present invention, specification:

[0056] 5mg / 5ml / branch.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a tropiseiron hydrochloride compound and a preparation method thereof. The invention also relates to application of an injection containing the tropiseiron hydrochloride compound in preparation of drugs for treating nausea and vomit.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tropisetron hydrochloride compound and a preparation method thereof, and also relates to using the crystal to manufacture a medicine for treating nausea and vomiting. Background technique [0002] At present, chemotherapy and radiotherapy are still the main means of anti-tumor, but because they can cause nausea and vomiting, the treatment of patients often cannot be carried out effectively. The mechanism of nausea and vomiting caused by chemotherapy and radiotherapy is that radiotherapy and chemotherapy act on the mucosal tissue of the gastrointestinal tract, causing the chromaffin-like cells of the gastrointestinal tract to release dopamine and 5-hydroxytryptamine (5-HT). -HT 3 Receptor binding, through nerve reflex action on the vomiting center, causing nausea and vomiting. Therefore, 5-HT is an important chemical transmitter causing vomiting, and its basic str...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D451/12A61K31/46A61K9/08A61P1/08
Inventor 严洁黄欣
Owner TIANJIN HANKANG PHARMA BIOTECH
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