Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

High-purity micafungin or salt thereof, and preparation method and application thereof

A micafungin and high-purity technology, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, and cyclic peptide components, can solve the problems of poor product stability, increase the difficulty of industrial production, and high equipment investment, so as to reduce the process Operational difficulty coefficient, good product stability, and the effect of reducing production costs

Active Publication Date: 2020-04-24
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
View PDF4 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the micafungin products prepared by the conventional methods currently reported cannot meet the ICH regulations on solvent residues (see ICH Q3C for details)
If the investment in equipment is high, the production scale is easy to be limited, and the operation is difficult, which is obviously not conducive to industrial production. At the same time, the obtained product has poor stability and needs to be stored below -70°C, which brings difficulties in product transportation, which undoubtedly increases industrial production. The difficulty seriously limits the scale of industrial production

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • High-purity micafungin or salt thereof, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Preparation of micafungin with low solvent residue and low salt

[0069] Dissolve the compound of formula 1 (2.0g) in the system of methanol (0.13ml) and water (2.2ml) at 15°C, add isobutanol (25ml) after dissolving, stir well, and slowly drop Ethyl acetate (27.4ml), after dropping, stirred at 12°C for 12h. It was filtered, washed several times with a mixture of methanol and ethyl acetate (1.7:1), and the solid was collected by centrifugation. Introduce air with a humidity above 85%, then place the sample in a vacuum drying oven, and place a plate of tap water at the bottom of the vacuum drying oven, dry it at 15°C for 2 hours under vacuum conditions, and then wait until the humidity of the drying oven is 75%. Continue vacuum drying at 15° C. for 14 h to obtain micafungin sodium (1.50 g, mass yield 75%). HPLC showed that the purity was 99.90%, the single impurity was below 0.1%, and the mass percentages of isobutanol, methanol, ethyl acetate and ethanol were 0.03%, 0....

Embodiment 2

[0071] Preparation of micafungin with low solvent residue and low salt

[0072] Dissolve the compound of formula 1 (2.0g) in the system of methanol (0.13ml) and water (2.2ml) at 10°C, add isobutanol (25ml) after dissolving, stir well, and slowly drop Ethyl acetate (27.4ml), after dropping, stirred at 8°C for 2h. It was filtered, washed several times with a mixture of methanol and ethyl acetate (1.7:1), and the solid was collected by centrifugation. Introduce air with a humidity above 82%, then place the sample in a vacuum drying oven, and place a plate of tap water at the bottom of the vacuum drying oven, dry it at 10°C for 4 hours under vacuum conditions, and then wait until the humidity of the drying oven is 78%. Continue vacuum drying at 10° C. for 10 h to obtain micafungin sodium (1.50 g, mass yield 75%). HPLC showed that the purity was 99.90%, the single impurity was below 0.1%, and the mass percentages of isobutanol, methanol, ethyl acetate and ethanol were 0.02%, 0.05...

Embodiment 3

[0074] Preparation of micafungin with low solvent residue and low salt

[0075] Under the condition of 15°C, dissolve the raw material (2.0g) containing the compound of formula 1 in the system of methanol (0.25ml) and water (2.2ml), add isobutanol (25ml) after dissolving, and stir evenly. Ethyl acetate (30ml) was slowly added dropwise, and the mixture was stirred at 15°C for 2h. It was filtered, washed several times with a mixture of methanol and ethyl acetate (1.7:1), and the solid was collected by centrifugation. Introduce air with a humidity above 88%, then place the sample in a vacuum drying oven, and place a plate of pure water at the bottom of the vacuum drying oven, dry at 15°C for 6 hours under vacuum conditions, and then wait until the humidity of the drying oven is 80% , and continued vacuum drying at 15° C. for 12 h to obtain micafungin sodium (1.70 g, mass yield 85%). HPLC showed a purity of 99.91%. The mass percent contents of isobutanol, methanol, ethyl acetat...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
purityaaaaaaaaaa
purityaaaaaaaaaa
purityaaaaaaaaaa
Login to View More

Abstract

The invention discloses a high-purity micafungin or a salt thereof, and a preparation method and an application thereof. The content of a residual organic solvent in the micafungin or the salt thereofis lower than 1.8%. Air with a certain humidity is introduced into a drying box during preparation,, a raw material containing micafungin or the salt thereof is put into the drying box, and the raw material a water system undergo vacuum drying, and when the humidity of the drying box reaches 70% or above, air introduction is stopped. The preparation method has the advantages of mild conditions, simple operation process, high yield, good stability and convenient transportation of the product, great reduction of the technological operation difficulty coefficient, and reduction of the productioncost. The micafungin or the salt thereof can be used for preparing medicines for preventing or treating diseases caused by fungal infection.

Description

technical field [0001] The invention relates to the field of organic compounds, in particular to a high-purity micafungin or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. Background technique [0002] Fungal infection has become the main cause of high morbidity and mortality in immunocompromised patients. The incidence of fungal infections has increased significantly over the past 20 years. High-risk groups for fungal infections include critically ill patients, surgical patients, and those with HIV infection, leukemia, and other neoplastic diseases. Those who have undergone organ transplantation are also at high risk of fungal infection. [0003] Echinocandins, a new class of antifungal drugs, are effective in the treatment of infections caused by Candida or Aspergillus. This class of drugs is represented by micafungin and caspofungin. Echinocandin drugs inhibit fungi by inhibiting the formation of 1,3-β glycosidic bonds, there...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/56A61K38/12A61P31/10
CPCC07K7/56A61P31/10A61K38/00Y02A50/30
Inventor 陈敏王园圆李严季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com