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Etimicin sulfate liposome inhalant and preparation method thereof

A technology of etimicin sulfate and micin lipid, which can be used in liposome delivery, pharmaceutical formulation, aerosol delivery, etc., and can solve the problems of limited clinical use and high nephrotoxicity.

Pending Publication Date: 2020-10-20
WUXI JIMIN KEXIN SHANHE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its relatively high ear and kidney toxicity, its clinical application is largely limited.

Method used

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  • Etimicin sulfate liposome inhalant and preparation method thereof
  • Etimicin sulfate liposome inhalant and preparation method thereof
  • Etimicin sulfate liposome inhalant and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0070] Mix 15 g of etimicin sulfate and 300 g of soy lecithin, then add 500 ml of absolute ethanol to dissolve at a temperature of 50°C. Concentrate on a rotary evaporator to remove the ethanol, add 2000 ml of pH 7.4 PBS buffer, and shake slightly. After high-pressure homogeneous cutting, the speed is 1200rpm, and the cutting time is 2min. After the emulsion is prepared, it is homogenized and circulated 4 times under a pressure of 150Mpa to prepare etimicin sulfate liposomes, and then add 16g of sodium chloride and coke. Dissolve 0.072g of sodium sulfite, adjust the pH to 6.2 with 10% sodium hydroxide solution, filter, and fill.

Embodiment 2

[0072] Mix 15 g of etimicin sulfate and 225 g of soy lecithin, then add 400 ml of absolute ethanol to dissolve the solution at a temperature of 55°C. Concentrate on a rotary evaporator to remove the ethanol, add 1875 ml of pH 7.4 PBS buffer, and shake it slightly. After high-pressure homogeneous cutting, the speed is 1500rpm, and the cutting time is 3min. After the emulsion is prepared, it is homogenized and circulated 5 times under a pressure of 100Mpa to prepare etimicin sulfate liposomes, and then add 10g of sodium chloride and coke. Sodium sulfite 0.019g, dissolve it, adjust the pH to 6.4 with 10% sodium hydroxide solution, filter, and fill.

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Abstract

The invention discloses an etimicin sulfate liposome inhalant and a preparation method thereof. The liposome inhalant is prepared from 1 part by weight of etimicin sulfate, 15-20 parts by weight of phospholipid, 125-150 parts by weight of a buffer solution and a proper amount of auxiliary materials. The pH value of the inhalant ranges from 6.2 to 6.4. The preparation method comprises the followingsteps of mixing the etimicin sulfate, the phospholipid and an organic solvent, performing dissolving, performing concentration to remove the organic solvent, adding the buffer solution, performing shaking slightly, and carrying out high-pressure homogeneous cutting to obtain etimicin sulfate liposome; and adding a proper amount of auxiliary materials, and performing dissolving, filtering and filling. The inhalant has an excellent targeting effect; compared with a common injection, the inhalant has the advantages that the bioavailability is higher, the concentration of drugs at toxic parts canbe reduced, and the safety of the drugs is greatly improved. The preparation method is simple and feasible and is suitable for industrial production.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations for the treatment of infections, in particular to an etimicin sulfate liposome inhalant and a preparation method thereof Background technique [0002] Etimicin sulfate belongs to aminoglycoside antibiotics. Unlike most antibiotics that inhibit the synthesis of microbial protein, aminoglycoside antibiotics can play a bactericidal effect and have a strong killing effect on quiescent bacteria. It is a quiescent antibiotic. At the same time, it also has the characteristics of synergistic effect with antibiotics such as β-lactam and the existence of post-antibiotic effect (PAE) on many pathogenic bacteria. However, due to its high ear and kidney toxicity, its clinical use is greatly restricted. [0003] Aminoglycoside drugs are concentration-dependent antibiotics. The higher the concentration, the stronger the bactericidal effect, but the toxicity of the drug is also positively related to the blood...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/127A61K31/7036A61K47/24A61P31/04
CPCA61K31/7036A61K9/127A61K9/1277A61K9/0073A61K47/24A61P31/04
Inventor 王丹丹俞婷刘薇薇
Owner WUXI JIMIN KEXIN SHANHE PHARMA
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