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Solamargine liposome, preparation method and usage thereof

A technology of solanine liposomes and solanines, which is applied in the field of alkaloid liposomes, can solve problems such as hemolysis and other toxic side effects, application obstacles, etc., achieve improved anti-tumor effects, improve muscle and blood vessel stimulation, and facilitate industrial production Effect

Active Publication Date: 2011-04-06
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But solanine is insoluble in water, and has certain toxic and side effects such as hemolysis, which hinders its application as a monomer drug
At present, there is no relevant report on making solanine into liposome

Method used

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  • Solamargine liposome, preparation method and usage thereof
  • Solamargine liposome, preparation method and usage thereof
  • Solamargine liposome, preparation method and usage thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0165] Example 1. Solanine liposome preparation.

[0166] Party:

[0167] Australian solanine 0.1g

[0168] Soy Lecithin for Injection 1.5g

[0169] Cholesterol 0.4g

[0170] Tween-80 0.2g

[0171] pH=4.9 phosphate buffered saline solution 100ml

[0172] Weigh the soybean lecithin and cholesterol for injection of the prescribed amount and dissolve them in 300ml of ether, dissolve solanine in 100ml of phosphate buffered saline solution, mix the organic phase and the aqueous phase evenly, then add the prescribed amount of Tween-80, Heated in a water bath to 35°C, treated with ultrasound for 15 minutes, evaporated the organic solvent under reduced pressure until there was no ether smell, and then dispersed it with ultrasound to obtain solanine liposomes with an encapsulation efficiency of 61.5%.

Embodiment 2

[0173] Example 2. Solanine liposome preparation.

[0174] Party:

[0175] Australian solanine 0.1g

[0176] Soy Lecithin for Injection 1.5g

[0177] Cholesterol 0.4g

[0178] Tween-80 0.2g

[0179] pH=4.9 phosphate buffered saline solution 100ml

[0180] Weigh the prescribed amount of soybean lecithin and cholesterol for injection, dissolve in 300ml chloroform, transfer to a round bottom flask, and at a water bath temperature of 40°C, the rotation speed is 150r / min, and the organic solvent is evaporated under reduced pressure to form a film. After formation, the organic solvent was completely removed by nitrogen gas for several minutes. Weigh the prescription amount of solanine and Tween-80 and dissolve it in 100ml of phosphate buffered saline solution, transfer the buffer solution into a flask, spin and wash the membrane at room temperature and normal pressure until the membrane completely falls off, hydrate for 30min, and then sonicate After 20 minutes of treatment, s...

Embodiment 3

[0181] Example 3. Solanine liposome preparation.

[0182] Party:

[0183] Australian solanine 0.1g

[0184] Soy Lecithin for Injection 1.5g

[0185] Cholesterol 0.4g

[0186] Poloxamer F-68 0.2g

[0187] pH=4.9 phosphate buffered saline solution 100ml

[0188] Weigh the prescribed amount of soybean lecithin for injection and cholesterol, dissolve in 300ml ether, dissolve poloxamer F-68, and Australian solanine in 100ml phosphate buffered saline solution, mix the organic phase and the aqueous phase evenly, and heat in a water bath to 35°C, sonicate for 15 minutes, evaporate the organic solvent under reduced pressure until there is no ether smell, and then disperse it by sonication to obtain solanine liposomes with an encapsulation efficiency of 70.5%.

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Abstract

The invention relates to solamargine liposome, which is characterized in that the liposome comprises the following raw materials: 1 part by weight of solamargine, 8 to 80 parts by weight of phospholipid, 2 to 20 parts by weight of cholesterol and 1 to 10 parts by weight of emulsifier. The invention also discloses a preparation method of the solamargine liposome. The invention has the advantages that the solamargine is coated between the two phospholipid layers of the liposome so that the water solubility is enhanced; the physical stability of the solamargine liposome is good; and the solamargine liposome can be stored for a longer time. The preparation method of the solamargine liposome is simple and mature, and is convenient to industrial production.

Description

technical field [0001] The invention relates to an alkaloid liposome, in particular to a solanine liposome; the invention also relates to a preparation method and application of the solanine liposome. Background technique [0002] Australian solanine, English name: solamargine, molecular formula: C 45 h 73 NO 15 , the structural formula: [0003] [0004] Australian solanine is a white powder, insoluble in water, soluble in methanol, and can be extracted and refined from the dry aerial part of Solanaceae Solanum nigrum L. through any extraction process disclosed in the prior art. It can be purchased from the market, and the content of solanine in Australia is preferably more than 95%. The content of Australian solanine in the whole plant of Solanum solanum is the most in the immature fruit, which can reach 4.2%. [0005] Solanum nigrum is the dry aerial part of Solanum nigrum L., a plant of the Solanaceae family. It tastes bitter, slightly sweet, and cold in nature. ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/706A61K36/81A61P1/16A61P35/00A61P11/00
Inventor 萧伟徐连明曹亮张岩唐朝辉李娜
Owner JIANGSU KANION PHARMA CO LTD
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