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Prepn process and prepn of new soluble voriconazole salt

A voriconazole and soluble technology, which is applied in the field of preparation of soluble salts, can solve the problems of low solubility, toxicity, and difficulty in achieving therapeutic effects, and achieve the effects of high solubility, simple preparation process, and avoiding toxic effects

Inactive Publication Date: 2006-10-18
大道隆达(北京)医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is undoubtedly a good solution to make freeze-dried powder injection, but its low solubility is difficult to achieve the concentration of therapeutic effect without solubilization
[0004] Chinese patent CN1261287 discloses a method in which voriconazole is made into freeze-dried powder injection through cyclodextrin inclusion solubilization, but the cyclodextrin used is dibutyl ether sulfur-β-cyclodextrin, which has harmful effects on the body. certain toxicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Dissolve 5g of voriconazole in 60ml of ethanol, and dissolve fully under stirring at 15°C; add 2ml of hydrochloric acid dropwise during stirring, and continue stirring for 20 minutes; stand for crystallization at room temperature, filter the solid, wash it with a small amount of ethanol, and dry it. Voriconazole hydrochloride was obtained;

Embodiment 2

[0018] Dissolve 10g of voriconazole in 80ml of ethanol, fully dissolve under stirring at 25°C; add 2ml of hydrochloric acid dropwise during stirring, and continue stirring for 20 minutes; stand for crystallization at room temperature, filter the solid, wash with a small amount of ethanol, and dry That is voriconazole hydrochloride;

Embodiment 3

[0020] Prescription: voriconazole hydrochloride 20g

[0021] Water for injection 1000ml

[0022] Preparation method:

[0023] Take 20 g of voriconazole hydrochloride, add 800 ml of water for injection to dissolve, adjust the pH to 3.5-5.5 with NaoH solution, and add 0.1% activated carbon for needles. Stir and absorb for 15 minutes, decarbonize and filter, add water for injection to 1000ml, filter and fill with a 0.45um microporous membrane, and sterilize by autoclaving.

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Abstract

The preparation process of soluble Voriconazole salt includes the following steps: 1. dissolving Voriconazole of 1-10 weight portions in alcohol of 60-90 weight portions at 15-40 through stirring; 2. dropping acid of 2-5 weight portions through stirring for 20-40 min; and 3. recrystallizing at normal temperature, filtering, washing with small amount of alcohol, and drying. The prepared salt is added with pharmaceutically acceptable supplementary material to prepare medicine powder for injection, emulsion for intravenous injection and injection. The present invention has high solubility and no toxicity.

Description

technical field [0001] The invention relates to a preparation method of a soluble salt, in particular to a preparation method of a soluble salt of voriconazole. Background technique [0002] Voriconazole is a synthetic triazole drug, which is the second generation of synthetic fluconazole derivatives. As a new type of antifungal drug, it has the characteristics of broad antibacterial spectrum and strong antibacterial efficacy. Pfizer company discovered this product in the 1980s, which can be used for the treatment of severe fungal infections with high mortality. Previously marketed treatments were limited to fungal infections or could cause severe toxicity, and some of them were not available in oral and intravenous formulations. This product can be taken orally or for injection. It is absorbed quickly after oral administration, and the plasma peak time is 1 to 2 hours, and the bioavailability is high, up to 96%. Food can affect the absorption of this product, so it should...

Claims

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Application Information

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IPC IPC(8): C07D403/10A61K9/08A61K9/10A61K9/14A61K31/506A61P31/10
Inventor 周英
Owner 大道隆达(北京)医药科技发展有限公司
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