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Lavo-ofloxacin liposome and preparation method thereof

A technology of levofloxacin liposome and levofloxacin is applied in the field of levofloxacin liposome and its preparation, and can solve the problems of reduced encapsulation rate, poor stability, unstable room temperature placement and the like

Inactive Publication Date: 2009-04-08
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Levofloxacin is an amphiphilic weakly basic drug, and the encapsulation efficiency is low by the traditional passive drug loading method, but it is prepared by the ammonium sulfate gradient method with a high encapsulation efficiency, which has defects such as poor stability and unstable storage at room temperature. Liposomes are preserved by freeze-drying, and the pH gradient on both sides of the membrane will disappear after liposomes are freeze-dried, and a large amount of drugs will leak out, resulting in a large reduction in encapsulation efficiency, which greatly limits its application.

Method used

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  • Lavo-ofloxacin liposome and preparation method thereof
  • Lavo-ofloxacin liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: adopt ammonium sulfate gradient method to prepare levofloxacin liposome, the steps are as follows:

[0021] (1) Weigh 3.2g of phosphatidylcholine, 0.4g of cholesterol and 4mg of vitamin E, dissolve the three with 100mL of chloroform, mix well to obtain a lipid solution, then place it on a rotary evaporator to remove chloroform under reduced pressure, and the lipid The substance forms a layer of lipid film on the wall of the vessel;

[0022] (2) precision preparation concentration is the ammonium sulfate solution of 0.3mol / L;

[0023] (3) 72.5mL of the above-mentioned prepared ammonium sulfate solution is poured into the lipid film obtained in step (1), and after being fully hydrated, energy is provided by a high-pressure milk homogenizer to prepare liposomes;

[0024] (4) Place the prepared liposomes in a dialysis bag, and dialyze with 1000mL0.9% isotonic saline for 18 hours;

[0025] (5) preparation concentration is the 1% glacial acetic acid solution 7...

Embodiment 2

[0026] Embodiment 2: adopt ammonium sulfate gradient method to prepare levofloxacin liposome, the steps are as follows:

[0027] (1) Weigh 0.889g phosphatidylcholine, 0.111g cholesterol and 2mg vitamin E, dissolve the three with 100mL chloroform, mix well to obtain a lipid solution, then place it on a rotary evaporator to remove chloroform under reduced pressure, and the lipid The substance forms a layer of lipid film on the wall of the vessel;

[0028] (2) precision preparation concentration is the ammonium sulfate solution of 0.1mol / L;

[0029] (3) 77mL of ammonium sulfate solution prepared above is poured into the lipid film obtained in step (1), and after being fully hydrated, energy is provided by a high-pressure homogenizer to prepare liposomes;

[0030] (4) Place the prepared liposome in a dialysis bag, and dialyze with 1000mL9% sucrose solution for 24 hours;

[0031] (5) preparation concentration is 3mL of the 1% glacial acetic acid solution 3mL of the levofloxacin o...

Embodiment 3

[0032] Embodiment 3: adopt ammonium sulfate gradient method to prepare levofloxacin liposome, the steps are as follows:

[0033] (1) Weigh 4.445g of phosphatidylcholine, 0.555g of cholesterol and 5mg of vitamin E, dissolve the three with 100mL of chloroform, mix well to obtain a lipid solution, then place it on a rotary evaporator to remove chloroform under reduced pressure, and the lipid The substance forms a layer of lipid film on the wall of the vessel;

[0034] (2) precision preparation concentration is the ammonium sulfate solution of 0.5mol / L;

[0035] (3) Get 65mL of ammonium sulfate solution prepared above and pour into the lipid film obtained in step (1), after being fully hydrated, provide energy to prepare liposomes by a high-pressure homogenizer;

[0036] (4) Place the prepared liposome in a dialysis bag, and dialyze with 1000mL9% sucrose solution for 8 hours;

[0037] (5) preparation concentration is 15mL of the 1% glacial acetic acid solution 15mL of the levofl...

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Abstract

The invention discloses a levofloxacin liposome, which comprises a levofloxacin and a liposome preparation, wherein the concentration of the levofloxacin is between 1 and 20 milligrams per milliliter; the liposome preparation comprises four lipid compositions of phosphatidyl choline, cholesterol, vitamin E and PEG2,000, the liposome is prepared first in the process of preparation, the levofloxacin is added in the liposome after dialysis, and the temperature of the mixture is kept so that the levofloxacin liposome is obtained. The levofloxacin liposome makes use of the PEG2,000 to modify the surface of the liposome so that a layer of hydration membrane can be formed on the surface of the liposome, and a polymer layer on the surface of the liposome can form a conformation cloud to prevent solute permeation, reduce the leakage of the drug in the liposome, and improve the stability of the liposome. The levofloxacin liposome has better stability, can slow the release of the levofloxacin to prolong the half-life of the drug in human body, and can increase the intracellular uptake to improve the anti-inflammatory activity.

Description

technical field [0001] The invention relates to a levofloxacin liposome and a preparation method thereof. Background technique [0002] Infectious disease is a century-old disease of human beings, seriously endangering human health, and is a common and frequently-occurring disease in our country. Although the development and research progress of antibiotics have provided favorable conditions for the prevention and treatment of infectious diseases. However, with the aging of the population and the changes of pathogenic bacteria, the incidence of infectious diseases continues to rise, and the case fatality rate is still high. At the same time, due to the increasingly serious and complex problem of bacterial drug resistance, refractory, mixed, and infectious diseases have increased significantly. Therefore, the prevention and treatment of clinical infectious diseases is still an important task at present. [0003] Levofloxacin is a third-generation quinolone drug. Its main m...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/5383A61P31/04
Inventor 黄桂华张新科石洋
Owner SHANDONG UNIV