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Linezolid-containing anti-infection pharmaceutical composition and preparation method thereof

A technology of linezolid and composition, applied in the field of anti-infective medicinal composition and preparation thereof, can solve the problems of low solubility and difficult preparation of linezolid and the like

Inactive Publication Date: 2015-05-06
YABANG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Because the solubility of linezolid in water is very small, it is only slightly soluble in water, and the solubility in water at room temperature is less than 3mg / ml, so it is difficult to prepare a higher concentration of water-based preparations

Method used

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  • Linezolid-containing anti-infection pharmaceutical composition and preparation method thereof
  • Linezolid-containing anti-infection pharmaceutical composition and preparation method thereof
  • Linezolid-containing anti-infection pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Alcohol Prescription:

[0047]

[0048] Gel Base Prescription:

[0049]

[0050] Preparation Process:

[0051] (1) Preparation of sterile linezolid ethosomes:

[0052] ①Weigh the prescribed amount of linezolid, phosphatidylcholine, and cholesterol, dissolve them with the prescribed amount of dimethyl sulfoxide, place them in a ground-mouth rotary evaporator, and remove the dimethyl sulfoxide by rotary evaporation in a constant temperature water bath at 40°C under reduced pressure. Sulfone;

[0053] ②At 40°C, add an appropriate amount of glass beads to the ground-mouth rotary evaporating flask, add the prescribed amount of pH6.8 phosphate buffer solution and the prescribed amount of propylene glycol solution, and rotate and stir for 20 minutes;

[0054] ③Remove the glass beads from the above mixture, add the prescribed amount of vitamin E, oscillate evenly, and use appropriate ultrasound;

[0055] ④ The above mixture was passed through a 0.22 μm microporous mem...

Embodiment 2

[0065] Alcohol Prescription:

[0066]

[0067] Gel Base Prescription:

[0068]

[0069] Preparation Process:

[0070] (1) Preparation of sterile linezolid ethosomes:

[0071] ① Weigh the prescribed amount of linezolid, phosphatidylcholine, and cholesterol, dissolve them in the prescribed amount of chloroform, place them in a ground-mouth rotary evaporator, and remove the chloroform by rotary evaporation in a constant temperature water bath at 40°C under reduced pressure;

[0072] ②At 40°C, add an appropriate amount of glass beads to the ground-mouth rotary evaporating flask, add the prescribed amount of pH6.8 phosphate buffer solution and the prescribed amount of propylene glycol solution, and rotate and stir for 20 minutes;

[0073] ③Remove the glass beads from the above mixture, add the prescribed amount of vitamin C, oscillate evenly, and sonicate appropriately;

[0074] ④ Pass the above solution through a 0.22 μm microporous membrane to obtain sterile linezolid et...

Embodiment 3

[0084] Alcohol Prescription:

[0085]

[0086] Gel Base Prescription:

[0087]

[0088] Preparation Process:

[0089] (1) Preparation of sterile linezolid ethosomes:

[0090] ① Weigh the prescribed amount of linezolid, phosphatidylcholine, and cholesterol, dissolve in the prescribed amount of ethyl acetate, place in a ground-mouth rotary evaporator, and remove chloroform by rotary evaporation in a constant temperature water bath at 40°C under reduced pressure;

[0091] ②At 40°C, add an appropriate amount of glass beads, the prescribed amount of phosphate buffer solution and the prescribed amount of propylene glycol solution into the ground-mouth rotary evaporating flask, and rotate and stir for 20 minutes;

[0092] ③Remove the glass beads from the above mixture, add the prescribed amount of vitamin C, oscillate evenly, and sonicate appropriately;

[0093] ④ Pass the above solution through a 0.22 μm microporous membrane to obtain sterile linezolid ethosomes.

[0094] ...

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Abstract

The invention discloses a linezolid-containing anti-infection pharmaceutical composition and a preparation method thereof. The pharmaceutical composition contains 1.0-5.0% (g / ml) of linezolid and is composed of an ethosome drug-loading system and a hydrogel system; and the pharmaceutical composition can be prepared into a linezolid-ethosome gel spray, and can be externally applied to anti-infection treatment.

Description

technical field [0001] The invention provides an anti-infection pharmaceutical composition containing linezolid and a preparation method thereof, belonging to the technical field of drug delivery systems. Background technique [0002] Skin bacterial infection, that is, bacterial infectious skin disease, is clinically manifested as skin furuncle, gangrene, cellulitis, folliculitis, etc. The strains causing skin infection are mainly Gram-positive bacteria, accounting for 84.7% of the total isolates, and Staphylococcus accounts for 94.4% of Gram-positive bacteria, of which Staphylococcus aureus accounts for 63.9%, so Staphylococcus, especially Staphylococcus aureus Bacteria are considered the main pathogens causing skin infections. [0003] Staphylococcus aureus is also the main pathogen of nosocomial infection and community infection. It is highly pathogenic and can cause various infections such as sepsis, catheter-derived infection, wound infection, systemic infection, and t...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K9/06A61K31/5377A61K47/10A61K47/34A61K47/28A61P31/04
Inventor 王淑娟陈再新庄鹏飞赵晓红朱峰王勇军
Owner YABANG PHARMA
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