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

Amorphous vancomycin hydrochloride as well as preparation method, application and pharmaceutical composition thereof

A vancomycin hydrochloride, non-crystallization technology, applied in the direction of drug combinations, anti-infective drugs, glycopeptide components, etc., can solve problems such as difficult to take, large capsule particles, etc., to achieve increased effective components, reduced impurities, and improved appearance and color Effect

Active Publication Date: 2009-12-30
ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
View PDF2 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the vancomycin hydrochloride used clinically is to use freeze-dried powder as raw material to prepare oral and injection dosage forms. In the capsule dosage form of oral dosage form, because the density of the freeze-dried powder is relatively small, the prepared capsule particles are relatively large and difficult to take.

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
  • Amorphous vancomycin hydrochloride as well as preparation method, application and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: the preparation of vancomycin crude product

[0035] The vancomycin fermentation broth is filtered under alkaline conditions, and the obtained clarified filtrate passes through the macroporous adsorption resin XAD-1600, and the vancomycin is adsorbed on the resin. After the resin is washed with water, it is eluted with an acidic aqueous solution of 40% ethanol. After elution, the eluent containing vancomycin was decolorized by adding activated carbon, and the filtrate obtained by filtering was concentrated to obtain vancomycin hydrochloride aqueous solution, and then NH 4 HCO 3 Precipitate to obtain crude vancomycin. The content of vancomycin B in crude vancomycin is 86.8%, and the potency is 599u / mg.

[0036] Take 2500g of this crude product, add 20.0L of purified water, add NaOH solution to adjust the pH to 10.0, and use 0.2M 2 25.0L of vancomycin filtrate was obtained by filtering through a ceramic membrane with a pore size of 0.5 μm, the solution ti...

Embodiment 2

[0037] Embodiment 2: the precipitation of vancomycin hydrochloride

[0038] Get 500 mL of the concentrated solution in Example 1, filter through 0.45 μm and 0.2 μm filter membranes and add 25 g NaHCO while stirring 3 , Vancomycin precipitated from it, forming a slurry, adding HCl aqueous solution to adjust the pH to 2.80, and continuing to stir for 60min to make it evenly mixed, stop stirring and let stand for 38 hours, the process temperature is controlled at 14-15°C. The mixture was separated by filtration and top-washed with 200mL90% ethanol earlier, and the conductivity of the top-wash liquid was 385us / cm at the end of the top-wash, and then top-washed with 200mL absolute ethanol to obtain 99.7g of vancomycin hydrochloride wet product, wet product Obtain intermediate 72.5g after removing residual ethanol by drying, obtain vancomycin hydrochloride finished product 63.2g after high vacuum drying again, finished product moisture is 3.4%, its bulk density of vancomycin hydroch...

Embodiment 3

[0039] Embodiment 3: the precipitation of vancomycin hydrochloride

[0040] Get 500 mL of the concentrated solution in Example 1, filter through 0.45 μm and 0.2 μm filter membranes and add 15 g of NaHCO while stirring 3 , Vancomycin precipitated from it, forming a slurry, adding HCl aqueous solution to adjust the pH to 3.50, and continuing to stir for 30min to make it evenly mixed, stop stirring and let stand for 48 hours, the process temperature is controlled at 5-6°C. The mixture was separated by filtration and top-washed with 200mL 90% ethanol earlier, and the conductivity of the top-wash solution was 293us / cm at the end of the top-wash, and then top-washed with 200mL absolute ethanol to obtain 92.3g of vancomycin hydrochloride wet product, wet Product obtains intermediate 68.5g after drying to remove residual ethanol, then obtains vancomycin hydrochloride finished product 58.6g after high vacuum drying, and the finished product moisture is 3.1%, and its bulk density of van...

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
Bulk densityaaaaaaaaaa
Bulk densityaaaaaaaaaa
Bulk densityaaaaaaaaaa
Login to View More

Abstract

The invention provides a high-density amorphous vancomycin hydrochloride, a preparation method thereof, an application of the vancomycin hydrochloride for oral administration or injection administration and a pharmaceutical composition containing the vancomycin hydrochloride. The vancomycin hydrochloride in an amorphous state has the characteristics similar to the diffraction pattern of an X-ray powdery crystal shown in the attached drawing 1. The effective components of vancomycin hydrochloride prepared by the preparation method are enhanced greatly, other impurities are reduced to a large extent, the purity is high, and the chromatographic purity can reach more than 95 percent. The amorphous vancomycin hydrochloride not only can be used as injections, but also can be used as capsules and other solid preparations. Meantime, the appearance and the color of products are improved obviously, and the products are suitable for oral administration or injection administration.

Description

technical field [0001] The present invention relates to a vancomycin hydrochloride, in particular to a high-density non-crystalline vancomycin hydrochloride and a preparation method thereof, and the use of the vancomycin hydrochloride for oral or injection administration, and containing The pharmaceutical composition of vancomycin hydrochloride. Background technique [0002] Vancomycin hydrochloride is an amphoteric glycopeptide antibiotic produced by Nocardia orientalis under controlled fermentation conditions, and its chemical formula is C 66 h 75 C 12 N 9 o 24 • HCl, molecular weight 1,486. The production of vancomycin by the fermentation of the microorganism Amycolatopis orientalis (formerly Nocardia orientalis) has been described in more detail in US Patent 3,067,099 (filed 1955) and WO 91 / 08,300. The freeze-dried powder of vancomycin hydrochloride is off-white, and its aqueous solution is a transparent solution with a pH of 2.5-4.5. [0003] Clinically, vancomyc...

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
IPC IPC(8): C07K9/00A61K38/14A61P31/00
Inventor 王小勇张国钧劳学军孙新强
Owner ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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