Veterinary aqueous injectable suspensions containing florfenicol

A florfenicol, suspension technology, applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, organic active ingredients, etc., can solve pain, irritation and pain, low osmotic pressure, etc. question

Inactive Publication Date: 2006-09-06
CALLUNA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the formulation reportedly exhibited acceptable tissue tolerance at the injection site, it was considered painful by licensed veterinarians to inject the formulation
[0007] Although the injectable formulation described in European patent 0 546 018 B1 may improve the previous injectable solution (such as the preparation dissolved in pure N-methyl-2-pyrrolidone), if combined with other physiologically acceptable Said formulations are also very irritating and irritating compared to aqueous solutions and suspensions (containing lower concentrations of physiologically acceptable solvents, having a physiologically acceptable pH, and having significantly lower osmotic pressure at the injection site). painful

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Micronized Florfenicol 300mg

[0060] Sodium citrate 50.0mg

[0061] Potassium dihydrogen phosphate 1.5mg

[0062] Glucose monohydrate 80.0mg

[0063] Low viscosity sodium carboxymethylcellulose (CMC) 2.0mg

[0064] Polyvinylpyrrolidone K12 3.5mg

[0065] Lecithin 3.0mg

[0066] Sodium formaldehyde sulfoxylate 2.5mg

[0067] Sodium metabisulfite 0.1mg

[0068] Sodium edetate 0.1mg

[0069] Methylparaben 1.0mg

[0070] Propylparaben 0.5mg

[0071] Add appropriate amount (q.s.ad) of water for injection 1ml

Embodiment 2

[0073] Micronized Florfenicol 250mg

[0074] Sodium citrate 50.0mg

[0075] Sorbitol (70%) 250.0mg

[0076] Medium viscosity sodium carboxymethylcellulose (CMC) 0.8mg

[0077] Polyvinylpyrrolidone K15 3.5mg

[0078] Polysorbate 80 1.0mg

[0079] Sorbitan monooleate 1.0mg

[0080] Sodium formaldehyde sulfoxylate 2.5mg

[0081] Sodium phosphite 10.0mg

[0082] Sodium edetate 0.1mg

[0083] Benzyl Alcohol 9.0mg

[0084] Add appropriate amount of water for injection 1ml

Embodiment 3

[0086] Micronized Florfenicol 400.0mg

[0087] Sodium citrate 80.0mg

[0088] Potassium dihydrogen phosphate 10.0mg

[0089] Sodium Gluconate 150.0mg

[0090] Low viscosity sodium carboxymethylcellulose (CMC) 1.5mg

[0091] Polyvinylpyrrolidone K12 3.5mg

[0092] Lecithin 3.0mg

[0093] Sodium formaldehyde sulfoxylate 2.5mg

[0094] Sodium metabisulfite 0.1mg

[0095] Sodium edetate 0.1mg

[0096] Methylparaben 1.0mg

[0097] Propylparaben 0.5mg

[0098] Add appropriate amount of water for injection 1ml

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Abstract

This invention relates to pharmaceutical compositions for veterinary use in form of aqueous injectable suspensions comprising Florfenicol or Florfenicol in form of a substantially water-insoluble complex, co-crystal or salt, sterile and micronised, in a concentration up to 500 mg/ml. The suspensions enable parenteral antimicrobial therapies in animals, with limited numbers of injections and showing good general- and local tolerances. They also possess a limited sedimentation on standing as well as after shipping, are easily resuspendable and have good syringiblity.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for veterinary use containing a high concentration of florfenicol as a pharmaceutically active ingredient, more particularly said composition is an aqueous injectable suspension. Background technique [0002] Florfenicol [D-(threo)-1-p-methylsulfonylphenyl-2-dichloroacetamido-3-fluoro-1-propanol] is an antibacterial agent known to be commonly used for veterinary purposes. Florfenicol is a broad-spectrum antibiotic active to a variety of pathogenic veterinary bacteria (NEU et al., Antimicrob. 19, 2, 294-297). [0003] Injectable formulations containing florfenicol have been described in several patents. [0004] European Patent 0 014 437 B1 discloses not only the synthesis of Florfenicol but also examples of different formulations, including oral suspensions, injectable solutions in water / dimethylacetamide mixtures and instant reconstituted bacteria powder. [0005] European Patent 0 546 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K47/32A61K47/38A61K47/12A61K47/26
CPCA61K31/165A61K47/26A61K47/38A61K47/12A61K9/0019A61P31/04
Inventor 埃尔温·恩布莱驰简·恩布莱驰
Owner CALLUNA PHARMA
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