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
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  • 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 vo

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0025] Example 1:

[0026] Dissolve 45g hydroxypropyl-β-cyclodextrin and 8.14g midiomycin in an appropriate amount of 50mN acetic acid, stir well to dissolve, use 0.5N NaOH as a pH adjuster, slowly add dropwise and keep stirring for about 2 hours , the pH was adjusted to 4.5, and it was ready for sterilization and packaging. At this time, the drug concentration of the inclusion compound was 30 mg / ml.

Example Embodiment

[0027] Example 2:

[0028] Mix 37.5g hydroxypropyl-β-cyclodextrin with 4.14g rotamycin, add an appropriate amount of 50mN acetic acid, stir to dissolve completely, after stabilization, slowly add 0.2N NaOH dropwise to adjust the pH value to 5.5, stir well A stable clathrate solution is made, and the clathrate drug concentration is 40mg / ml at this time, 5g of trehalose is added as a freeze-drying excipient to dissolve, and it is obtained by sterilizing, sub-packaging and freeze-drying.

Example Embodiment

[0029] Example 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, and then use 1N NaOH to adjust the pH value to 6.5, fully stir to form a stable inclusion compound solution, the drug concentration of the inclusion compound is 25mg / ml at this time, add 10g of lactose as a freeze-drying excipient to dissolve, and sterilize the package and freeze-dry it.

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PUM

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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

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Application Information

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IPC IPC(8): A61K31/7048A61K9/08A61K9/19A61P31/04
Inventor 卢智俊
Owner REGENEX PHARMA LTD
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