Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid

A technology of tropane citrate and tropisetron, which is applied in the direction of making medicines into special physical or taking forms of devices, medicine formulations, medicine combinations, etc. The solubility of other salts is not ideal, etc., to achieve good safety and tolerance, and the effect of mild adverse reactions

Active Publication Date: 2010-09-22
JIANGXI DONGFU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In the process of the present invention, other salts of tropisetron such as: sulfate, nitrate, fumarate, etc. have been synthesized successively, but it is found that sulfate, nitrate are easily oxidized, and the compound turns from white to yellow after storage, while other salts The solubility of the class is not ideal

Method used

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  • Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid
  • Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid
  • Citric acid tropisetron raw material medicine and preparation technology of raw material medicine and injection liquid

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Experimental program
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Embodiment 1

[0045] Embodiment 1: the preparation technology of tropisetron citrate crude drug

Embodiment 2

[0046]Embodiment 2: the preparation technology of tropisetron citrate crude drug

Embodiment 3

[0047] Embodiment 3; The preparation technology of tropisetron citrate injection

[0048] Embodiment 1: the preparation technology of tropisetron citrate crude drug

[0049] 1. Acylation reaction

[0050] Add 6.5-7.5 parts of dioxane and 0.9-1.7 parts of pyridine into a three-necked flask, stir in an ice-water bath, add 1.5-2.5 parts of trichloroacetyl chloride dropwise within 0.5 hours, and remove the ice after 0.5 hours of reaction after adding and stirring. bath, add 0.7 to 1.4 parts of indole at 30°C at one time, stir and react at room temperature for 2 hours; pour the reaction solution into ice water, and a yellow granular solid is precipitated. After standing still, the solid is filtered out to obtain the compound, which is fully washed with water After drying, it is used for the next reaction;

[0051] 2. Alkaline hydrolysis reaction

[0052] Put the above compound into a flask, add 12-16 parts of water and 1.5-3 parts of sodium hydroxide, stir and react at 110°C for...

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Abstract

The invention relates to a citric acid tropisetron raw material medicine and a preparation technology of the citric acid tropisetron raw material medicine and an injection liquid, and belongs to the field of chemical pharmacy; in the process of tropisetron salifying, the citric acid is used as acid radical; the chemical name of the citric acid tropane tropisetron is [(1alpha H, 5alpha H)-8-methyl-azepine bicyclo-(3, 2, 1) octyl group-3alpha-]-1H- benzpyrole-3- formic ether citrate; and the molecular formula is C23H28N209. In the process of tropisetron salifying, the tropisetron is dissolved in ethanol; the mixture is added with ethanol solution of the citric acid, evenly stirred and stands till the needed solid is separated out; the crude citric acid tropisetron is filtered, heated and dissolved in distilled water, is added with the activated carbon for backflowing and decoloring, cools and stands after being filtered so as to separate out white cystal; the mixture is filtered; the filter cake is dried and then distilled water is used for the secondary recrystallization to obtain the refined citric acid tropane tropisetron. The clinical research shows that compared with the imported muriatic acid tropisetron injection solution, the citric acid tropisetron injection solution has similar curative effect and safety.

Description

technical field [0001] The invention relates to a bulk drug of tropisetron citrate, and a preparation process of the bulk drug of tropisetron citrate and an injection, belonging to the field of chemical pharmacy. Background technique [0002] Tropisetron is recommended in the third series of "National Guidelines for the Development of New Chemical and Pharmaceutical Products". 3 ) receptor antagonists, used to control nausea and vomiting caused by chemotherapy. It is characterized by high efficiency, high selectivity, and long acting time. It can selectively block the presynaptic 5-HT of peripheral neurons that causes vomiting reflex 3 Stimulation of receptors, 5-HT acting on afferent vagal activity in the area postrema 3 receptor. 5-HT at therapeutic doses 4 Receptor has slight affinity for 5-HT 1 , 5-HT 2 Receptor has no affinity for other receptors such as histidine H 1 with H 2 receptors, nicotine, muscarinic acid, substance P and dopamine receptors, adrenal α 1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D451/12A61K31/46A61K9/08A61J3/00A61P43/00A61P1/08A61P1/14
Inventor 王大冲郭仲坚翟绪武袁伟芳陈黎琳王建张恒王向东
Owner JIANGXI DONGFU PHARMA CO LTD
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