Febantel lipidosome and preparation method thereof

A non-Bantyr and liposome technology, applied in the field of non-Bantyr liposome and its preparation, can solve the problems of low bioavailability, short half-life, incomplete absorption, etc.

Inactive Publication Date: 2018-02-23
HENAN SOAR VETERINARY PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There are non-Bantyr anti-insect drugs on the market now, which are insoluble in water, incomplete absorption, low bioavailability, and short half-life in vivo

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A preparation method of non-Bantyle liposomes, the steps are as follows:

[0023] (1) In terms of mass ratio, weigh 12.5 mg of Febantyr and 375 mg of PEG-modified lipid derivative, the PEG-modified lipid derivative is PEG2000-distearoylphosphatidylethanolamine;

[0024] (2) Preparation of blank liposome suspension by injection method: dissolve PEG-modified lipid derivatives in absolute ethanol to make a lipid solution, absorb the lipid solution and inject slowly into 7.5mL pH=4, concentration 300mmol In the citrate-citrate sodium buffer solution (hydration medium) of / L, inject and continue to stir to remove ethanol, make blank liposome suspension after ultrasonic dispersion;

[0025] (3) Ultrasonically disperse non-bantyr in 2.5mL absolute ethanol to prepare non-bantyr ethanol dispersion;

[0026] (4), mixing the blank liposome suspension obtained in step (2) and the non-bantyr ethanol dispersion obtained in step (3), supercritical CO at 50°C and 12Mpa 2 After proces...

Embodiment 2

[0028] A preparation method of non-Bantyle liposomes, the steps are as follows:

[0029] (1) In terms of mass ratio, weigh 12.5 mg of Febantyr and 500 mg of PEG-modified lipid derivative, the PEG-modified lipid derivative is PEG2000-distearoylphosphatidylethanolamine;

[0030] (2) Preparation of blank liposome suspension by reverse evaporation method: dissolve PEG-modified lipid derivatives in absolute ethanol to make a lipid solution, then add 5 mL of citrate with pH=2.7 and a concentration of 200 mmol / L In acid-citrate sodium buffer solution (hydration medium), high-speed shearing makes it form stable W / O colostrum, and then evaporates the organic solvent under reduced pressure to obtain a blank liposome suspension;

[0031] (3) Ultrasonically disperse non-bantyr in 1.5mL absolute ethanol to prepare non-bantyr ethanol dispersion;

[0032] (4), mixing the blank liposome suspension obtained in step (2) and the non-bantyr ethanol dispersion obtained in step (3), supercritical ...

Embodiment 3

[0034] A preparation method of non-Bantyle liposomes, the steps are as follows:

[0035] (1) In terms of mass ratio, weigh 12.5 mg of Febantyr and 450 mg of PEG-modified lipid derivative, the PEG-modified lipid derivative is PEG5000-distearoylphosphatidylglycerol;

[0036] (2) Preparation of blank liposome suspension by spray-drying method: dissolve PEG-modified lipid derivatives in absolute ethanol to make a lipid solution, spray-dry the lipid solution to obtain a lipid powder, and use 6 mL pH = 5.2, citrate-citrate sodium buffer solution (hydration medium) with a concentration of 400mmol / L hydrates the lipid powder to prepare a blank liposome suspension;

[0037] (3) Ultrasonically disperse non-bantyr in 1.25mL of absolute ethanol to prepare non-bantyr ethanol dispersion;

[0038] (4), mixing the blank liposome suspension obtained in step (2) and the non-bantyr ethanol dispersion obtained in step (3), supercritical CO at 50°C and 15Mpa 2 Treat for 5 minutes to obtain non-B...

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Abstract

The invention belongs to the field of a veterinary medicine, and in particular discloses febantel lipidosome and a preparation method thereof. The preparation method comprises the following steps: weighing febantel and a PEG modified lipid derivative, wherein the mass ratio of the febantel to the PEG modified lipid derivative is 1 to (30 to 40), and the PEG modified lipid derivative is PEG-distearoyl phosphoethanolamine or PEG-distearoyl phosphatidyl glycerol; adding ethanol to dissolve the PEG modified lipid derivative, and preparing blank lipidosome suspension by taking a citric acid-sodiumcitrate buffer solution with the pH of 2.7 to 5.2 and the concentration of 200 to 400mmol / L as a hydration medium; ultrasonically dispersing the febantel into ethanol and preparing febantel-ethanol dispersion liquid with the concentration of 5 to 10mg / mL; mixing the blank lipidosome suspension and the febantel-ethanol dispersion liquid, and performing supercritical CO2 treatment for 5 to 10 minutes at 50 to 55 DEG C and under 10 to 15MPa to obtain the febantel lipidosome. The mixed liquid of the blank lipidosome suspension and the febantel-ethanol dispersion liquid is subjected to supercritical CO2 treatment, so that the febantel lipidosome is prepared successfully.

Description

technical field [0001] The invention belongs to the field of veterinary medicine, and in particular relates to a non-bantyr liposome and a preparation method thereof. Background technique [0002] Febantyr is a colorless powder, soluble in acetone, chloroform, tetrahydrofuran and dichloromethane, insoluble in water and ethanol. [0003] Febantyr is a benzimidazole precursor anthelmintic, which has been approved in the United States as an anthelmintic for various animals. Both febantyl and nitopramine are benzimidazole prodrugs, which are converted into fenbendazole (and its sulfoxide) and oxfendazole in the gastrointestinal tract to exert an effective anthelmintic effect. [0004] Febantyr is mostly marketed in the United States as a compound preparation. For example, products for dogs and cats are often combined with praziquantel to expand the range of deworming. [0005] According to the metabolism studies of cattle and sheep, it is shown that most drugs are rapidly meta...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K31/27A61P33/10
CPCA61K9/1271A61K9/1277A61K31/27A61K47/24
Inventor 孙江宏陈华崔俊亚常磊梁小菊付晓鹤
Owner HENAN SOAR VETERINARY PHARMA
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