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A kind of method for preparing amorphous substance

An amorphous and material technology, applied in the field of chemistry, can solve the problem of effective concentration duration affecting drug action, etc., and achieve good application prospects and wide applicability

Active Publication Date: 2016-05-25
北京泰克美高新技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Since the drug must reach a certain concentration in the body to be effective after taking it, the increase of blood drug concentration and the prolongation of effective concentration duration may affect the drug effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve ceftriaxone sodium soluble in aqueous solution into water, add 1%-5% hyaluronic acid, then slowly add acetone, stop when the volume percentage of acetone in the solution is 50-80%, filter the precipitate, and use 50%-80% acetone aqueous solution was washed three times and dried to obtain a solid amorphous form of the substance to be prepared. It was determined to be an amorphous powder by powder XRD measurement.

Embodiment 2

[0029] Take 10g of cefditoren pivoxil raw material, dissolve it in 100mL of 1N hydrochloric acid solution (containing 2% sodium hyaluronate), and slowly add 100ml of 1N sodium hydroxide for neutralization. carried out under conditions, finally filtered the precipitate, washed three times with 30ml of 2% sodium hyaluronate aqueous solution, and dried at 40°C to obtain amorphous cefditoren pivoxil, which was determined to be an amorphous powder by powder XRD determination.

Embodiment 3

[0031] Dissolve cefotaxime acid soluble in alkaline aqueous solution into alkaline aqueous solution, add 1%-5% hyaluronic acid, then slowly add hydrochloric acid for neutralization (at a rate of about 1.2-2.1ml / min), filter Precipitate, wash three times with 1%-5% hyaluronic acid aqueous solution, and dry to obtain a solid amorphous of the substance to be prepared, which is determined to be an amorphous powder by powder XRD determination.

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PUM

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Abstract

The invention relates to the field of chemistry, and discloses a method for preparing an amorphous substance. The method comprises the following steps: providing a uniform water solution of the substance and hyaluronic acid or salt or derivative thereof, changing conditions to convert the substance into an insoluble state, filtering to obtain a precipitate, washing, and drying to obtain the amorphous substance. The method disclosed by the invention is simple and easy to implement, has wide applicability, and has favorable application prospects.

Description

technical field [0001] The invention relates to the field of chemistry, in particular to a method for preparing amorphous substances. Background technique [0002] The state of existence of solid drugs is an important content in drug research. Since the amorphous state of solid drugs often has better in vitro dissolution and in vivo absorption properties, and may achieve better clinical efficacy, related research has attracted more and more attention. Amorphous form is a special crystal form of substances. In the amorphous state, the various physical and chemical properties and clinical efficacy characteristics of drugs are often different from those of general crystal form drugs. Therefore, in the study of polymorphic forms of solid drugs, it is of special significance to deeply explore the state of amorphous substances. [0003] At present, there are mainly three viewpoints to explain the continuous evolution between the pure amorphous state and the pure crystalline stat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/36
Inventor 王兵王涛邢艳平戴学良陈尚义
Owner 北京泰克美高新技术有限公司
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