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

Clarithromycin water soluber preparation for injection use

A clarithromycin, water-soluble technology, applied in the field of water-soluble preparations in which water-soluble derivatives form inclusion complexes, can solve the problems of inability to ensure stability, large volume, inability to freeze-dry, and inconvenience for clinical use, and to improve bioavailability degree, high clinical application value, and the effect of improving solubility

Inactive Publication Date: 2007-10-03
REGENEX PHARMA LTD
View PDF1 Cites 43 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This technology solves the defects of low solubility of ordinary clarithromycin or its analogues, too large volume after dissolution, unable to freeze-dry, unable to guarantee stability, and inconvenient for clinical use.

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Dissolve 45g of hydroxypropyl-β-cyclodextrin and 8.14g of midecamycin in an appropriate amount of 50mN acetic acid, stir well to dissolve, use 0.5N NaOH as a pH regulator, add slowly drop by drop and keep stirring for about 2 hours , adjust the pH to 4.5, and sterilize and repackage to obtain. At this time, the drug concentration of the clathrate is 30 mg / ml.

Embodiment 2

[0028] Mix 37.5g hydroxypropyl-β-cyclodextrin with 4.14g rotamycin, add an appropriate amount of 50mN acetic acid, stir to dissolve completely, slowly add 0.2N NaOH drop by drop to adjust the pH value to 5.5 after stabilization, and stir well Make a stable clathrate solution. At this time, the drug concentration of the clathrate is 40 mg / ml. Add 5 g of trehalose as a freeze-drying excipient to dissolve, sterilize, sub-package, freeze-dry to obtain.

Embodiment 3

[0030] Dissolve 112.5g β-cyclodextrin and 25.05g dirithromycin in an appropriate amount of 2mN hydrochloric acid, stir to dissolve completely; then slowly add 20mN arginine solution and stir to dissolve, then adjust the pH value to 6.5. Fully stir to form a stable clathrate solution. At this time, the clathrate drug concentration is 25 mg / ml. Add 10 g of lactose as a freeze-drying excipient to dissolve, sterilize, subpackage, freeze-dry to obtain.

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

No PUM Login to View More

Abstract

A water-soluble clarithromycin for injection is prepared from clarithromycin or its analog, and beta-cyclodextrin or its pharmacologically acceptable water-soluble derivative through proportional mixing, adding diluted acid, stirring for dissolving, and regulating pH=4.5-6.5 to obtain a stable inclusion compound.

Description

technical field [0001] The present invention relates to a water-soluble preparation of clarithromycin for injection or its analogues, in particular to the formation of clarithromycin for injection or its analogues with β-cyclodextrin and its pharmaceutically acceptable water-soluble derivatives Water-soluble preparations of clathrates. Background technique [0002] Macrolides antibiotics are a class of antibiotics obtained by Streptomyces fermentation (fourteen-membered or sixteen-membered macrocycles) or semi-synthesized on the basis of fermentation products (fifteen-membered macrocycles). Commonly used drugs for fourteen-membered macrolide antibiotics are erythromycin, roxithromycin, clarithromycin, dirithromycin, telithromycin, etc. and their derivatives; commonly used drugs for fifteen-membered macrolide antibiotics It is azithromycin, etc. Commonly used drugs for sixteen-membered macrolide antibiotics include josamycin, kitasamycin, rotamycin, etc. and their derivative...

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): A61K31/7048A61K9/08A61K9/19A61P31/04
Inventor 卢智俊
Owner REGENEX PHARMA 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