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Method for preparing hydrochloric acid berberine long circulation liposome with ammonium sulphate gradient method-film evaporation method

A long-circulating liposome, ammonium sulfate gradient method technology, applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve problems such as drug leakage, easy rupture, and reduced application value. , to achieve the effect of uniform particle size and high encapsulation efficiency

Inactive Publication Date: 2008-01-23
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After liposomes enter the human circulatory system, due to the action of proteins and opsonins in the blood, they are prone to rupture, and the encapsulated drugs leak quickly and are recognized and absorbed by the reticuloendothelial system (RES), thereby reducing the application value

Method used

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  • Method for preparing hydrochloric acid berberine long circulation liposome with ammonium sulphate gradient method-film evaporation method
  • Method for preparing hydrochloric acid berberine long circulation liposome with ammonium sulphate gradient method-film evaporation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Take by weighing 400mg egg yolk lecithin (EPC) and 133mg cholesterol (CH) with a 50ml Erlenmeyer flask, and dissolve 60mgPEG2000 in 2ml ethanol. Rotary evaporator recovers ethanol under reduced pressure, until there is no alcohol smell (about 90 minutes), a film is formed on the wall of the flask, inject 25ml of 2.0mol l -1 Concentrated ammonium sulfate solution can be appropriately ultrasonicated to dissolve the membrane material and hydrated for 1h-2h, then put the solution into a dialysis bag, use distilled water as the dialysis medium, and generally dialyze for 15-20h to create a gradient of ammonium sulfate, and finally get blank liposomes , take 5ml of blank liposomes and transfer it to a 50ml Erlenmeyer flask, add 5ml of 1mg·l -1 Berberine hydrochloride solution was incubated in a water bath at 40°C for 60 minutes, then 1ml was transferred to a dialysis bag with distilled water as the external fluid for dialysis at 4°C for 12 hours, and the dialysate w...

Embodiment 2

[0030] Example 2: Take by weighing 400mg egg yolk lecithin (EPC) and 133mg cholesterol (CH) with a 50ml conical flask, and dissolve 60mgPEG2000 in 2ml ethanol. Rotary evaporator recovers ethanol under reduced pressure, until there is no alcohol smell (about 90 minutes), a film is formed on the wall of the flask, inject 25ml of 2.0mol l -1 Concentrated ammonium sulfate solution can be appropriately ultrasonicated to dissolve the membrane material and hydrated for 1h-2h, then put the solution into a dialysis bag, use distilled water as the dialysis medium, and generally dialyze for 15-20h to create a gradient of ammonium sulfate, and finally get blank liposomes , take 5ml of blank liposomes and transfer it to a 50ml Erlenmeyer flask, add 5ml of 1mg·l -1 Berberine hydrochloride solution, incubate at 40°C for 10 minutes in a water bath, then take 2ml and transfer it to a dialysis bag, use distilled water as the external fluid for dialysis, and dialyze at 4°C for 12 hours, change t...

Embodiment 3

[0031] Example 3: Take by weighing 400mg egg yolk lecithin (EPC) and 133mg cholesterol (CH) with a 50ml Erlenmeyer flask, and dissolve 60mgPEG2000 in 2ml of ethanol. Rotary evaporator recovers ethanol under reduced pressure, until there is no alcohol smell (about 90 minutes), a film is formed on the wall of the flask, inject 25ml of 2.5mol l -1 Concentrated ammonium sulfate solution can be appropriately ultrasonicated to dissolve the membrane material and hydrated for 1h-2h, then put the solution into a dialysis bag, use distilled water as the dialysis medium, and generally dialyze for 15-20h to create a gradient of ammonium sulfate, and finally get blank liposomes , take 5ml of blank liposomes and transfer it to a 50ml Erlenmeyer flask, add 5ml of 1mg.l -1Berberine hydrochloride solution, incubate at 60°C for 60 minutes in a water bath, then transfer 1ml to a dialysis bag, use distilled water as the external fluid for dialysis, and dialyze at 4°C for 12 hours, changing the di...

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Abstract

A method for preparing a macrocyclic lipidosome of berberine hydrochloride with ammonium sulphate gradient method-thin film evaporation method is provided, which comprises: 1) dissolve egg yolk lecithin, cholesterin with 1 / 3 egg yolk lecithin quality, polyethyleneglycol 2000 with 1 / 20 to 1 / 5 egg yolk lecithin quality; 2) decompress the recycled ethanol to form a film on vessel wall; infuse ammonium sulphate solution to dissolve the film material; hydrate for 1h to 2h; 3) take distilled water as dialysis medium to dialyse for 15 to 20h, make ammonium sulphate gradient to get blank lipidosome; 4) add berberine hydrochloride solution into the blank lipidosome; 5) incubate under the temperature of 30 to 60 degree for 10 to 60 minutes; 6) take the solution after inculation, dialyse it under different temperatures for 12h with distilled water as dialysis medium, get colorless and transparent fluid. Transfer and define constant volume of the dialysis fluid to get macrocyclic lipidosome with high encapsulation rate, excellent stability and even grain diameter. The macrocyclic lipidosome prepared in the invention has the advantages of high encapsulation rate, excellent stability and even grain diameter.

Description

technical field [0001] The invention belongs to the technical field of intelligent drug carriers, and in particular relates to a method for preparing berberine hydrochloride long-circulation liposomes by comprehensively utilizing an ammonium sulfate gradient method and a thin film evaporation method. Background technique [0002] Liposomes are closed vesicles composed of lipid bilayers with an aqueous interior. The liposomes, which are composed of phosphocid bilayers, are alternately separated by water layers and phospholipid bilayers, and can embed hydrophilic or lipophilic substances. As a smart drug carrier, liposome has attracted more and more attention because of its excellent targeting, biocompatibility, improved drug stability, therapeutic index, and reduced drug toxicity. After liposomes enter the human circulatory system, due to the action of proteins and opsonins in the blood, they are prone to rupture, and the encapsulated drugs leak quickly and are recognized an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4375A61K47/24
Inventor 安学勤朱琨
Owner NANJING NORMAL UNIVERSITY
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