Preparation method of moxifloxacin hydrochloride liposome

A technology of moxifloxacin hydrochloride lipid and moxifloxacin hydrochloride, which is applied in the field of preparation of moxifloxacin hydrochloride liposomes, can solve the problems of low encapsulation efficiency and drug loading, poor stability, etc., and achieve prolongation of drug retention time, Good stability and the effect of improving the encapsulation rate

Inactive Publication Date: 2020-07-10
JIANGSU YONGDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Moxifloxacin hydrochloride is a water-soluble small-molecule drug, and the encapsulation efficiency and drug-loading capacity of liposomes for water-soluble small-molecule drugs have always been low, and the stability is poor

Method used

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  • Preparation method of moxifloxacin hydrochloride liposome

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A preparation method of moxifloxacin hydrochloride liposomes, comprising the following steps:

[0029] S1, phospholipid and cholesterol are dissolved in chloroform, the mass concentration of phospholipid is 50mg / mL, the mass ratio of phospholipid and cholesterol is 5:1, add ammonium sulfate aqueous solution (the molar concentration of ammonium sulfate aqueous solution is 550mmol / L, ammonium sulfate The addition amount of aqueous solution is 2mL / 50mg phospholipid) carries out short-time ultrasonic treatment (power is 550W, time is 25s), then add xanthan gum and carboxymethyl chitosan, the mass ratio of xanthan gum and phospholipid is 1:4 , the mass ratio of carboxymethyl chitosan and phospholipids is 1:6, placed in a pressure of 800bar and a temperature of 65°C to carry out high-pressure homogenization treatment, high-pressure homogenization cycle 4 times, to obtain liposome protobody, lipid The liposomes were placed in an extruder, extruded whole particles with a 145nm ...

Embodiment 2

[0033] A preparation method of moxifloxacin hydrochloride liposomes, comprising the following steps:

[0034] S1, phospholipid and cholesterol are dissolved in chloroform, the mass concentration of phospholipid is 40mg / mL, the mass ratio of phospholipid and cholesterol is 4:1, add ammonium sulfate aqueous solution (the molar concentration of ammonium sulfate aqueous solution is 500mmol / L, ammonium sulfate The addition amount of aqueous solution is 1mL / 50mg phospholipid) carries out short-time ultrasonic treatment (power is 500W, time is 20s), then add xanthan gum and carboxymethyl chitosan, the mass ratio of xanthan gum and phospholipid is 1:3 , the mass ratio of carboxymethyl chitosan and phospholipids is 1:5, placed in a pressure of 700bar and a temperature of 60°C to carry out high-pressure homogenization treatment, high-pressure homogenization cycle 3 times, to obtain liposome protobody, lipid The liposomes were placed in an extruder, extruded whole particles with a 140nm ...

Embodiment 3

[0038] A preparation method of moxifloxacin hydrochloride liposomes, comprising the following steps:

[0039] S1, phospholipid and cholesterol are dissolved in chloroform, the mass concentration of phospholipid is 60mg / mL, the mass ratio of phospholipid and cholesterol is 6:1, add ammonium sulfate aqueous solution (the molar concentration of ammonium sulfate aqueous solution is 600mmol / L, ammonium sulfate The addition amount of aqueous solution is 3mL / 50mg phospholipid) carries out short-time ultrasonic treatment (power is 600W, time is 30s), then add xanthan gum and carboxymethyl chitosan, the mass ratio of xanthan gum and phospholipid is 1:5 , the mass ratio of carboxymethyl chitosan and phospholipids is 1:7, placed in a pressure of 900bar and a temperature of 70°C for high-pressure homogenization treatment, high-pressure homogenization cycle 5 times, to obtain liposome protobody, lipid The liposomes were placed in an extruder, extruded whole particles with a 150nm microporo...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a preparation method of moxifloxacin hydrochloride liposome in order to prepare the moxifloxacin hydrochloride liposome with high encapsulation efficiency, large drug loading capacity and high stability. An improved ammonium sulfate gradient method is adopted, xanthan gum and carboxymethyl chitosan are added on the basis of conventional liposome preparation, and the moxifloxacin hydrochloride liposome is prepared. Experiments for determining the encapsulation efficiency and the drug loading capacityshow that the encapsulation efficiency of the moxifloxacin hydrochloride liposome prepared by the method disclosed by the invention can reach more than 90%, and the drug loading capacity of the moxifloxacin hydrochloride liposome prepared by the method can reach more than 30%; stability investigation experiments show that the moxifloxacin hydrochloride liposome prepared by the method provided by the invention has no obvious change in 30d encapsulation efficiency and internal particle size, and has high stability. Therefore, the moxifloxacin hydrochloride lipidosome prepared by the invention ishigh in encapsulation efficiency, large in drug loading capacity, high in stability and not prone to leak due to external influence.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a method for preparing moxifloxacin hydrochloride liposomes. Background technique [0002] The chemical name of moxifloxacin hydrochloride is 1-cyclopropyl-6-fluoro-8-methoxy-7-([S,S]-2,8-diazabicyclo[4.3.0]nonan-8- base)-4-oxo-1,4-dihydro-3-quinolinecarboxylate hydrochloride. Moxifloxacin hydrochloride has a spectrum of antibacterial activity, and is active against gram-positive bacteria, gram-negative bacteria, anaerobic bacteria, acid-fast bacteria and atypical microorganisms such as mycoplasma, chlamydia and legionella, and its safety is better than that of other quinolones. [0003] Liposome (liposome) refers to the ultra-miniature spherical drug carrier preparation made by encapsulating the drug in the middle of the film formed by the lipid bilayer. Because its structure is similar to a biological membrane, it can encapsulate water-soluble and fat-soluble substa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4709A61K47/36A61P31/04
CPCA61K9/1271A61K31/4709A61K47/36A61P31/04
Inventor 曹庆华
Owner JIANGSU YONGDA PHARMA
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