Application of the hydroxypropyl-belta-cyclodextrin in eyedrops of chloramphenicol and method thereof

A technology of chloramphenicol and hydroxypropyl is applied in the application field of hydroxypropyl-β-cyclodextrin in chloramphenicol eye drops, which can solve the problem of chloramphenicol eye drops precipitation, non-compliance with quality requirements, Solubility problems such as low, to achieve the effect of low hemolysis, promote dissolution rate, improve stability

Active Publication Date: 2009-10-07
YUNNAN PHYTOPHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But beta-cyclodextrin can cause chloramphenicol eye drops to precipitate in storage due to its low solubility in water, which does not meet the quality requirements of chloramphenicol eye drops Pharmacopoeia (2005 edition)

Method used

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  • Application of the hydroxypropyl-belta-cyclodextrin in eyedrops of chloramphenicol and method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Drug composition:

[0109] Chloramphenicol 2.625g / L

[0110] Borax 0.625g / L

[0111] Boric acid 17g / L

[0112] Phenylmercury acetate 0.02g / L

[0113] HP-β-CD 15g / L

[0114] Water up to 1L

[0115] Standard: the content of chloramphenicol diol shall not exceed 8%, and p-nitrobenzaldehyde shall not exceed 0.5%.

[0116] Preparation method:

[0117] 1. Put the formula amount of chloramphenicol and HP-β-CD into 150mL water, stir for 30min to fully dissolve and mix evenly, place it for later use;

[0118] 2. Put the formula amount of borax and boric acid into 300mL water, stir to dissolve them fully, and set aside;

[0119] 3. Put the formula amount of phenylmercuric acetate (or benzalkonium bromide, thimerosal) into 500mL water, stir well to dissolve it, place it for later use;

[0120] 4. Put the solutions of 1, 2, and 3 above into a container together, add water to 1L, stir for 10 minutes to make it evenly mixed, and then fill it into a small bottle to get ready. ...

Embodiment 2

[0122] In the drug component, the dosage of HP-β-CD is 10g / L, and the other ingredients and preparation method are the same as in Example 1.

Embodiment 3

[0124] In the drug component, the dosage of HP-β-CD is 25g / L, and the other ingredients and preparation method are the same as in Example 1.

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Abstract

The present invention is application of the hydroxypropyl-belta-cyclodextrin in eyedrops of chloramphenicol and method thereof. Adding hydroxypropyl-belta-cyclodextrin into formula of the eyedrops of chloramphenicol, the addition is 10-80 g / L. The invention finds HP-belta-CD (hydroxypropyl-belta-cyclodextrin) for improving stability of the eyedrops of chloramphenicol by a series of experiments, capable of improving dissolvability of the chloramphenicol for six times, and because of inclusion of the cavity structure to chloramphenicol, blocking chloramphenicol hydrolysis reaction catalyzed by various ions in solution effectively, degradation of the chloramphenicol in aqueous solution is greatly relieved, by experiments, accelerating for six months and normal temperature storing for 24 months, every index of the chloramphenicol eyedrops still conforms to request of the standard, content of chloramphenicol glycol is less than 8%, content of methyl aldehyde is 0, so stability of the chloramphenicol eyedrops is greatly improved.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to the application and method of hydroxypropyl-beta-cyclodextrin in chloramphenicol eye drops. Background technique [0002] Chloramphenicol is D-threo-(-)-N-[α-(hydroxymethyl)-β-hydroxy-p-nitrophenethyl]-2,2-dichloroacetamide. It is white needle-like or slightly yellow-green needle-like, long flaky crystal or crystalline powder, bitter in taste, easily soluble in methanol, ethanol, acetone, propylene glycol; slightly soluble in water. [0003] Chloramphenicol, discovered in 1947, is a broad-spectrum antibiotic produced by Streptomyces venezuela, and it is also the world's first fully chemically synthesized antibiotic. Due to its wide antibacterial spectrum, good effect and low cost, it has been widely used in various dosage forms, such as tablets, capsules, oral suspensions, solutions, ointments, oils, injection powders and ophthalmic preparations. Clinical, but because it inhi...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/165A61P27/02A61K47/69
Inventor 郭文李俊董维
Owner YUNNAN PHYTOPHARML
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