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Nocathiacin antibiotic medicament composition containing emulsifying agent

A technology of composition and emulsifier, which is applied in antibacterial drugs, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of nocafloxacin containing emulsifier, etc., and achieve high cost, simple and safe equipment, and low efficiency Effect

Inactive Publication Date: 2012-07-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the microsphere dosage form of nocafloxacin containing emulsifier

Method used

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  • Nocathiacin antibiotic medicament composition containing emulsifying agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment one: common emulsion

[0044] prescription:

[0045] Soybean oil 200μl; Lecithin 10mg;

[0046] Poloxamer 20mg; 0.9% sodium chloride solution (pH7.4) 800μl;

[0047] Nocafloxacin I 10mg.

[0048] Preparation Process:

[0049] Disperse the prescribed amount of poloxamer in 0.9% sodium chloride solution and grind it evenly, then add the oil phase containing the prescribed amount of phospholipids and the main drug, stir vigorously to make colostrum, and then add 0.9% sodium chloride solution to dissolve The colostrum is diluted and quantified to obtain a uniformly dispersed emulsion; the solubility of nocafloxacin I is 4.13 mg / ml as detected by high performance liquid chromatography; the solution is diluted 500-1000 times with 0.9% sodium chloride solution and there is no precipitation within 72 hours .

Embodiment 2

[0050] Embodiment two: common emulsion

[0051] prescription:

[0052] 500μl soybean oil; 10mg lecithin;

[0053] Poloxamer 10mg; 0.9% sodium chloride solution (pH7.4) 500μl;

[0054] Nocafloxacin I 10mg.

[0055] Preparation Process:

[0056] Disperse the prescribed amount of poloxamer in 0.9% sodium chloride solution and grind it evenly, then add the oil phase containing the prescribed amount of phospholipids and the main drug, stir vigorously to make colostrum, and then add 0.9% sodium chloride solution to dissolve The colostrum is diluted and quantified to obtain a uniformly dispersed emulsion; the solubility of nocafloxacin I is 2.175 mg / ml as detected by high performance liquid chromatography; the solution is diluted 500-1000 times with 0.9% sodium chloride solution and there is no precipitation within 72 hours .

Embodiment 3

[0057] Embodiment three: submicron emulsion

[0058] prescription:

[0059] MCT 200μl; egg yolk phospholipid 20mg;

[0060] Poloxamer 10mg; Povidone 10mg;

[0061] 3 μl of oleic acid; 800 μl of 0.9% sodium chloride solution (pH7.4);

[0062] Nocafloxacin I 10mg.

[0063] Preparation Process:

[0064] Dissolve the prescribed amount of povidone and poloxamer in 0.9% sodium chloride solution, dissolve egg yolk phospholipids, oleic acid and the main drug in MCT, sonicate so that each component is dissolved in each phase, centrifuge to remove insoluble, and then remove the oil Phases were added dropwise to the constantly stirring water phase, and then ultrasonically treated for 30 minutes until a uniformly dispersed emulsion was formed; the solubility of nocafloxacin I was detected by high performance liquid chromatography to be 5.27mg / ml; the solution was treated with 0.9% sodium chloride After the solution was diluted 500-1000 times, there was no precipitation within 72 hour...

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Abstract

The invention belongs to a medicament composition, and particularly relates to solution of a nocathiacin antibiotic-containing medicament composition. The invention particularly discloses a nocathiacin antibiotic-containing medicament composition, which comprises nocathiacin, medicament carrier, water-soluble emulsifying agent and fat-soluble emulsifying agent, wherein the medicament carrier consists of an aqueous phase and an oil phase; the water-soluble emulsifying agent is selected from one or mixture of poloxamer and povidone; the fat-soluble emulsifying agent is selected from one or mixture of two of lecithin, yolk phospholipid and soya bean phospholipid; the total mass of the water-soluble emulsifying agent and the fat-soluble emulsifying agent in each 1 milliliter of composition is30 to 50 milligrams; and the mass ratio of the water-soluble emulsifying agent to the fat-soluble emulsifying agent is 2-1:1. The provided medicament composition can obviously improve the dissolubility of the nocathiacin, the preparation process is safe, the used materials are economic, the used equipment is simple, and the process steps are a few; and the nocathiacin has remarkable medicament-resistant bacteria activity resistance, so the medicament composition has important clinical application value.

Description

technical field [0001] The invention belongs to a pharmaceutical composition, in particular to an emulsified dosage form, a submicroemulsion type, a nanomicroemulsion type, and a microsphere of a nocafloxacin antibiotic pharmaceutical composition containing an emulsifier. Background technique [0002] In the history of human beings fighting against diseases, bacterial infection has always been the number one killer of human death. As people use more and more antibiotics to treat diseases, they also exercise the resistance of bacteria. With the abuse of antibiotics and the rapid evolution of pathogenic bacteria, more and more drug-resistant strains have appeared clinically, especially strains resistant to multiple antibiotics such as methicillin-resistant Staphylococcus aureus (MRSA), Penicillin-resistant Streptococcus pneumoniae (PRSP), as well as the recently discovered "super bacteria", people often seem helpless in the face of the rapid infection rate of these pathogenic ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K38/12A61K47/32A61K47/34A61P31/04A61K47/10A61K47/26
Inventor 冯坤陈依军
Owner CHINA PHARM UNIV