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Vinthitine liposome

A technology of vinpocetine and cetine lipid, applied in the field of vinpocetine liposome and its preparation, can solve the problems of high irritation of the preparation, poor quality, complicated preparation process, etc., and achieves the improvement of curative effect and poor oral absorption. Effect

Inactive Publication Date: 2006-01-25
胡才忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] In the process of drug preparation research, some drugs that are difficult to dissolve in water are often encountered. When these drugs are developed into liquid preparations such as injections, methods such as solubilization, solubilization, and inclusion are usually used, and some even use non-aqueous solvents. The prepared preparation has complex process, poor stability, unqualified quality and high production cost
Some preparations are very irritating, and during the course of treatment, patients can hardly bear it and give up treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Preparation of vinpocetine liposomes by ethanol injection: take soybean phospholipids, cholesterol, VE and dissolve them in absolute ethanol and inject them into vinpocetine aqueous solution, stir at constant temperature and high speed, evaporate under reduced pressure to remove ethanol, pass through a microporous membrane to granulate, that is Vinpocetine liposomes were obtained, and the encapsulation efficiency could reach 72.8%.

Embodiment 2

[0013] Film dispersion method prepares vinpocetine liposomes: get soybean lecithin, cholesterol, VE dissolves in 150ml eggplant-shaped bottle with 15ml chloroform, forms a film under reduced pressure on a rotary thin film evaporator and removes all organic solvents, adds 10ml vinpocetine The aqueous solution is hydrated, and the vinpocetine liposome is obtained by passing through a microporous membrane to obtain vinpocetine liposomes, and the encapsulation efficiency can reach 70.1%.

Embodiment 3

[0015] Prepare vinpocetine liposomes by reverse-phase evaporation: weigh soybean lecithin, cholesterol, VE and add 5ml chloroform to dissolve, then add 10ml ether, then add 15ml vinpocetine in phosphate buffer, bath ultrasonic to make uniform For single-phase system, remove chloroform ether by vacuum evaporation until gel is formed, continue to evaporate under reduced pressure for 5 to 10 minutes, and vortex until the aqueous suspension, that is, liposome, is formed. Encapsulation efficiency can reach 37.5%.

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PUM

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Abstract

A vinpocetine lipid with high absorptivity, biologic utilization rate and stability for treating cardiovascular and cerebropathy caused by senility is prepared proportionally from vinpocetin, phosphatide, cholesterol and the supporting agent chosen from sorbitol, mannitol, cane sugar, sodium chloride, water-soluble starch etc.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a vinpocetine liposome (including proliposome) and a preparation method thereof. Background technique [0002] In the process of drug preparation research, some drugs that are difficult to dissolve in water are often encountered. When these drugs are developed into liquid preparations such as injections, methods such as solubilization, solubilization, and inclusion are usually used, and some even use non-aqueous solvents. The prepared preparation has complex process, poor stability, unqualified quality and high production cost. Some preparations are very irritating, and during the course of treatment, patients can hardly bear it and give up treatment. [0003] Vinpocetine (Vinpocetine) is a kind of indole alkaloid, the drug developed by Hungarian Jirui Company in the 1970s, which was listed in many countries in Europe and America. In 1995, it was listed as one of the top ten a...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K9/127A61P9/10A61P9/00
Inventor 胡才忠
Owner 胡才忠
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