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Preparation method for valnemulin liposome

A technology of vernimulin and liposomes, which is applied in the direction of liposome delivery, active ingredients of esters, antibacterial drugs, etc., can solve the problems of increasing drug toxicity and side effects, drug residues, increasing drug resistance, drug waste, etc. , to prolong the effective time of action, improve solubility, and reduce toxic and side effects

Inactive Publication Date: 2014-06-11
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If you want to increase the drug concentration in the target area, you must increase the dose, which not only increases the cost and causes waste of drugs, but also increases the side effects of drugs and drug residues in the body, increasing the possibility of drug resistance

Method used

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  • Preparation method for valnemulin liposome
  • Preparation method for valnemulin liposome
  • Preparation method for valnemulin liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The preparation method of the present embodiment warnimulin liposome comprises the following steps:

[0023] 1) Prepare NaHCO with a concentration of 25mg / ml 3 solution;

[0024] 2) Prepare a citric acid buffer solution with a pH of 6.0;

[0025] 3) Preparation of blank liposomes: Weigh 0.3 parts by mass of phospholipids and 0.1 parts by mass of cholesterol, add absolute ethanol to dissolve in a water bath at 60°C, evaporate the ethanol to form a film, add citric acid buffer at the same temperature for 20 part, stirred and hydrated in a water bath at 60°C for 10 minutes, then stirred at 30°C for 50 minutes, added distilled water to 20 parts after fully hydrated, and the obtained liposome solution was filtered through a microporous membrane to granulate;

[0026] 4) Weigh the original powder of Vernemulin and add it to ethanol and stir until fully dissolved to make a drug solution of Vernemulin with a concentration of 3mg / ml;

[0027] 5) Active drug loading: according...

Embodiment 2

[0030] The preparation method of the present embodiment warnimulin liposome comprises the following steps:

[0031] 1) Prepare NaHCO with a concentration of 25mg / ml 3 solution;

[0032] 2) Prepare a citric acid buffer solution with a pH of 4.5;

[0033] 3) Preparation of blank liposomes: Weigh 0.3 parts by mass of phospholipids and 0.1 parts by mass of cholesterol, add absolute ethanol to dissolve in a water bath at 64°C, evaporate the ethanol to form a film, add citric acid buffer at the same temperature for 20 part, stirred and hydrated in a water bath at 64°C for 10 minutes, then stirred at 45°C for 45 minutes, added distilled water to 20 parts after fully hydrated, and the obtained liposome solution was filtered through a microporous membrane to granulate;

[0034] 4) Weigh the original powder of Vernemulin and add it to ethanol and stir until fully dissolved to make a drug solution of Vernemulin with a concentration of 3mg / ml;

[0035] 5) Active drug loading: according...

Embodiment 3

[0038] The preparation method of the present embodiment warnimulin liposome comprises the following steps:

[0039] 1) Prepare NaHCO with a concentration of 25mg / ml 3 solution;

[0040] 2) Prepare a citric acid buffer solution with a pH of 3.0;

[0041] 3) Preparation of blank liposomes: Weigh 0.3 parts by mass of phospholipids and 0.1 parts by mass of cholesterol, add absolute ethanol to dissolve in a 70°C water bath, evaporate the ethanol to form a film, add citric acid buffer at the same temperature for 20 part, stirred and hydrated in a water bath at 70°C for 10 minutes, and then stirred at 60°C for 40 minutes, after fully hydrating, distilled water was added to make up to 20 parts, and the obtained liposome solution was filtered through a microporous membrane to granulate;

[0042] 4) Weigh the original powder of Vernemulin and add it to ethanol and stir until fully dissolved to make a drug solution of Vernemulin with a concentration of 3mg / ml;

[0043] 5) Active drug ...

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Abstract

The invention discloses a preparation method for a valnemulin liposome. The method comprises the following steps: 1) preparation of a NaHCO3 solution; 2) preparation of a citric acid buffer solution; 3) preparation of a blank liposome: a step of dissolving phosphatide and cholesterol in absolute ethyl alcohol in a water bath, allowing ethanol to volatilize and a film to be formed, then adding the citric acid buffer solution, carrying out complete hydration and filtering an obtained liposome solution with a millipore filter to realize whole grain filtering; 4) preparation of valnemulin fluid by dissolving raw valnemulin powder in ethanol; 5) active loading: a step of successively adding the valnemulin fluid and the NaHCO3 solution into the blank liposome and carrying out uniform mixing so as to obtain a crude liposome product; and 6) low temperature high speed centrifugation of the crude product obtained in step 5) so as to prepare the valnemulin liposome. According to the invention, through preparation of the blank liposome and active loading, the valnemulin liposome with a high entrapment rate and good clinical effects is obtained; the method is simple and easily practicable, and solubility of valnemulin in water and effective acting time, stability and targeting of valnemulin are improved.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and in particular relates to a preparation method of warnemulin liposome. Background technique [0002] Vernimulin is a new generation of pleuromutilin semi-synthetic antibiotics. It belongs to diterpenes and belongs to the same class of drugs as tiamulin. disease and Gram-positive bacterial infections. The mechanism of action of warnemulin is to inhibit bacterial protein synthesis at the ribosome level, and also inhibit RNA synthesis at high concentrations. It is mainly antibacterial, and it can also kill bacteria at high concentrations. It has a broad antibacterial spectrum, is effective against G+ and G- bacteria, and is highly effective against Mycoplasma and Spirochetes. [0003] The pharmacokinetic characteristics of varnimulin are fast absorption, high absorption rate, good drug efficacy, and high bioavailability, but the maintenance time of effective blood drug concentratio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/22A61P31/04
Inventor 吴红云郭俊清李建正董晓盈
Owner ZHENGZHOU HOUYI PHARMA
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