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Method for preparing brain targeting liposome pharmaceutical

A technology targeting liposomes and pharmaceutical preparations, applied in the medical field, can solve the problems of reducing the penetration performance of drugs on the blood-brain barrier, weak affinity, and limited drug loading

Inactive Publication Date: 2004-11-10
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the difficulty and cost of the synthesis process are increased; 2), most of the ligands are hydrophilic compounds, and the ligand-modified drug molecule reduces the fat solubility, although it increases the affinity for the receptor, but from another perspective , which reduces the penetration of the drug to the blood-brain barrier; 3), the ligand-receptor affinity used in the chemical targeting of nutrient receptors is weak; 4), the ligand-modified drug is One-to-one, so drug loading is limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: Preparation of the brain-targeted liposome formulation of 0.02% (molar ratio) fat-soluble drug

[0033] name

[0034] Preparation method: Dissolve the prescribed amount of various excipients in 20ml of ethanol, heat to 45°C while stirring on an electromagnetic stirrer to completely dissolve, and let cool; dissolve the drug in chloroform to make a 50mg / ml solution , mix the above two solutions, then slowly add the mixed solution to 150ml water for injection under the state of shearing machine high-speed stirring (3000 rpm), and continue to stir for 30 minutes under the condition of nitrogen protection, to obtain Multiphasic brain-targeting liposomal drug solutions. The liposome drug solution was repeatedly ultrafiltered with an ultrafilter to remove the organic solvent, and 0.9% sodium chloride solution was used as a replenishing liquid, and the volume of the final ultrafiltrate was 100ml. The ultrafiltrate was extruded repeatedly with five lay...

Embodiment 2

[0035] Embodiment 2: Preparation of the brain-targeted liposome formulation of 20% (molar ratio) fat-soluble drug

[0036] name

Content (%)

Lecithin

15.02

cholesterol

15.0

cephalin

10.0

Sphingomyelin

24.48

glutamate-phospholipid

10.0

Vitamin E

0.5

polyethylene glycol-phospholipid

5.0

drug

20.0

total

100

[0037] Preparation method: Dissolve the prescribed amount of various excipients in 20ml of ethanol, heat to 45°C while stirring on an electromagnetic stirrer to completely dissolve, and let cool; dissolve the drug in chloroform to make a 50mg / ml solution , mix the above two solutions, then slowly add the mixed solution to 150ml water for injection under the state of shearing machine high-speed stirring (3000 rpm), and continue to stir for 30 minutes under the condition of nitrogen protection, to obtain Multiphasic brain-ta...

Embodiment 3

[0040] Example 3: Preparation of brain-targeting liposome preparation containing 2% (molar ratio) of synthetic phospholipids with significant brain-targeting function

[0041] name

[0042] Method of making: same as embodiment 1

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PUM

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Abstract

The invention discloses a brain targeting liposome and the process for preparing brain targeting liposome pharmaceutical preparation, wherein the brain targeting liposome pharmaceutical preparation comprises medicament, various synthesized or natural phosphatide with brain targeting function as liposome coating material, cephalin having brain tissue absorption accelerating agent, liposome coating material, sphingomyelin with brain tropism and immunity activation, cholestrin for liposome coating material and liposome stabilizing agent, vitamin E as anti-oxidizing agent and polyoxyethylene glycols and phosphatide derivative for extending the half-decay time of liposome pharmaceutical blood.

Description

technical field [0001] The invention belongs to a preparation method of a medicament in the medical field, in particular to a preparation method of a brain-targeted liposome pharmaceutical preparation. Background technique [0002] Both cephalin (phosphatidylethanolamine) and sphingomyelin are separated and purified from brain tissue or central nervous tissue membrane. Sphingomyelin is mostly extracted from bovine brain or pig brain, and they are the main lipid compounds in brain tissue after cholesterol. The brain-targeted liposome pharmaceutical preparations containing these phospholipids have a strong selective tendency to brain tissue. At the same time, when liposomes are targeted to brain tissue, based on the similarity between cephalin and sphingomyelin and phospholipids in human brain tissue, they can promote the fusion of liposome membranes and brain cells, deliver drugs into brain cells, and exert effect. [0003] Nutrient receptor-mediated chemical targeted drug...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24
Inventor 陈涛商澎傅经国王九成
Owner XIAN LIBANG PHARMA TECH
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