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Crystalline quetiapine fumarate and pharmaceutical compositions thereof

A technology of quetiapine fumarate and crystalline form, which is applied in the direction of drug combination, pharmaceutical formula, carboxylate preparation, etc., which can solve the problems of unfavorable resource saving, large water consumption, and reduction of production costs, so as to overcome environmental pollution and high cost, the effect of significant cost and yield advantages

Active Publication Date: 2011-10-05
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method consumes a lot of water and consumes a lot of energy, which is not conducive to saving resources and reducing production costs.

Method used

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  • Crystalline quetiapine fumarate and pharmaceutical compositions thereof
  • Crystalline quetiapine fumarate and pharmaceutical compositions thereof
  • Crystalline quetiapine fumarate and pharmaceutical compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Take 5g of quetiapine fumarate, add 15g of water, stir and mix to obtain a mixture, heat to 95°C, the mixture becomes a clear solution, stir and cool, the solution is relatively viscous, mechanical stirring is required, quetiapine fumarate slowly precipitates, Filter under reduced pressure to obtain quetiapine fumarate crystals. After drying and weighing, the yield is 98%.

[0033] After HPLC analysis, the content after crystallization is 99.1%, and the related substances are <0.2%.

Embodiment 2

[0035] Take 5g of quetiapine fumarate, add 20g of water, stir and mix to obtain a mixture, heat to 92°C, the mixture becomes a clear solution. After stirring and cooling, quetiapine fumarate slowly precipitated, and filtered under reduced pressure to obtain quetiapine fumarate crystals. After drying and weighing, the yield is 93%.

[0036] After HPLC analysis, the content after crystallization is 99.6%, and the related substances are <0.1%. There is no change in related substances after crystallization.

Embodiment 3

[0038] Take 5g of quetiapine fumarate, add 30g of water, stir and mix to obtain a mixture, heat to 85°C, the mixture becomes a clear solution. After stirring and cooling, quetiapine fumarate slowly precipitated, and filtered under reduced pressure to obtain quetiapine fumarate crystals. After drying and weighing, the yield is 96%.

[0039] After HPLC analysis, the content after crystallization is 99.7%, and the related substances are <0.1%. There is no change in related substances after crystallization.

[0040] Through the above-mentioned examples, it is found that as the water consumption increases, the temperature required to obtain the quetiapine fumarate aqueous solution is lower, and if the water consumption is reduced, a higher temperature is required to obtain the quetiapine fumarate solution.

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PUM

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Abstract

The invention relates to a method for producing crystalline quetiapine fumarate which is produced by using water as a solvent, heating, dissolving and cooling crystallization. The invention also discloses a preparation using crystalline quetiapine fumarate prepared by the method. A quetiapine fumarate tablet which is prepared by mixing the crystalline quetiapine fumarate with auxiliary materials, granulating the mixture, adding a lubricant into the granulated mixture and tabletting, has fast soluble speed, and is capable of effectively improving product bioavailability.

Description

technical field [0001] The present invention relates to a new preparation method of crystalline quetiapine fumarate and a preparation prepared by using the crystalline quetiapine fumarate obtained according to the method. Background technique [0002] Quetiapine is an atypical antipsychotic. Its structure is similar to that of clozapine. It belongs to dibenzodiazepine derivatives. Cell deficiency, obesity, anticholinergic and other adverse reactions. now with (SEROQUEL) is marketed under the trade name for the treatment of schizophrenia, as monotherapy or as an adjunct to lithium or divalproex sodium, and for the treatment of acute manic episodes associated with bipolar I disorder . [0003] Quetiapine chemical name: 11-{4-[2-(2-(hydroxyethoxy)ethyl-1-piperazine])dibenzo[b,f][1,4]thiazepine} · 1 / 2 fumarate. [0004] Drug solubility and dissolution rate are key influencing factors for drug onset in vivo. The crystallization solvent and method tend to have a greater imp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D281/16A61K31/554C07C57/15C07C51/41A61K9/20A61P25/18
Inventor 葛光华黄龙梅王红莲李巧霞彭俊清胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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