Liposome preparation of teniposide phospholipid complexes and preparing method thereof

A technique of teniposide phospholipid and paraside phospholipid is applied in the field of medicine to achieve the effects of improving lipophilicity, improving solubility and improving toxicity

Inactive Publication Date: 2011-03-23
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] After literature search, there is no report on the use of teniposide phospholipid complexes to improve the encapsulation efficiency of teniposide liposome preparations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Weigh 6.56g of teniposide and 7.5g of soybean lecithin, add them to tetrahydrofuran, heat and reflux at 30°C for 30 minutes until the solution is clear, remove tetrahydrofuran by volatilizing the solvent with a rotating thin film method, and obtain light yellow crystals Teniposide phospholipid complex. Take 5.0 g of teniposide phospholipid complex, 10 g of soybean lecithin, and 5 g of cholesterol, add them to chloroform, and remove the chloroform by evaporation at 40 °C by the method of rotating thin film evaporation solvent, add PBS (pH7.4) buffer solution and fully water Then add 50g of sucrose to fully dissolve it, and the obtained liposome suspension is homogenized under high pressure, then subpackaged and freeze-dried to obtain the teniposide liposome freeze-dried preparation.

Embodiment 2

[0038] Weigh 65.6g of teniposide and 75g of soybean lecithin, add them into acetone, and heat under reflux for 60 minutes at 40°C until the solution is clear, then volatilize and remove the acetone by the method of rotating thin film to evaporate the solvent, and obtain light yellow crystal substitute Niposide phospholipid complex. Take 50g of teniposide phospholipid complex, 100g of soybean lecithin, and 50g of cholesterol, add them to chloroform, and remove the chloroform at 40°C by the method of rotating thin film evaporation solvent, add PBS (pH7.4) buffer solution to fully hydrate , followed by adding 750 g of trehalose to make it fully dissolved, and the obtained liposome suspension was homogenized under high pressure, then subpackaged and freeze-dried to obtain the teniposide liposome freeze-dried preparation.

Embodiment 3

[0040] Weigh 131.2 g of teniposide and 150 g of dimyristoylphosphatidylcholine, add them into tetrahydrofuran, and heat under reflux at 50°C for 120 minutes until the solution is clear, and remove tetrahydrofuran by volatilization by the method of rotating thin film to evaporate the solvent to obtain Pale yellow crystalline teniposide phospholipid complex. Take 100g of teniposide phospholipid complex, 200g of soybean lecithin, and 100g of cholesterol, add them to chloroform, and remove the chloroform at 40°C by the method of rotating thin film evaporation solvent, and add PBS (pH6.8) buffer solution to fully hydrate , followed by adding 1500 g of trehalose to make it fully dissolved, and the obtained liposome suspension was homogenized under high pressure, then subpackaged and freeze-dried to obtain the teniposide liposome freeze-dried preparation.

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PUM

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Abstract

The invention relates to a liposome preparation of teniposide phospholipid composite and the preparation method thereof. Clinical experiments prove that teniposide has a more broad-spectrum of anti-tumor activity, but the existing preparations in the process of use cause severe allergic reactions due to a large number of surfactants CremophorEL contained in the prescriptions. The invention provides a liposome preparation of teniposide phospholipid composite, which comprises the following components by weight percentages: 0.1-10 percent of the teniposide phospholipid composite, 0-80 percent ofthe phospholipid and 0-50 percent of cholesterol, wherein, the teniposide phospholipid composite is compounded by the teniposide and the phospholipid. The invention also provides the preparation method of the liposome preparation of teniposide phospholipid composite, as well as a lyophilized preparation, and not only overcomes the shortcomings of existing teniposide preparations in toxicity and allergy, but also improves the hydrophilicity and / or the lipotropy of the teniposide and enhance the entrapment rate and the stability of the liposome preparation thereof at the same time. The method is a novel drug sustained-release targeted preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a teniposide phospholipid complex liposome preparation and a preparation method thereof. Background technique [0002] Teniposide (Teniposide, Vumon, VM-26) aliases: Teniposide, Wittner, Vierm 26, Podophylloside, Podophylloside, Podophyllothiophene Glycoside, podophylloside. Teniposide is a biological ester base with anti-cancer effect proposed from the genus A. tricuspidus, which can inhibit the synthesis of eukaryotic protein, depolymerize polyribosomes, and interfere with the function of protein ribosomes. Teniposide is a cycle-specific cytotoxic drug that acts on the late S2 and G2 phases of the cell cycle by preventing cell mitosis. It can also cause single-strand and double-strand breaks of DNA bonds, and its mechanism of action may be caused by the inhibition of type II topoisomerase. Teniposide has a remarkable curative effect, and clinical data show that teniposide has...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K9/127A61K47/24A61P35/00
Inventor 陈建明张扬邓莉吴忠斌张悦郭丹李莹杨秋霞孙靖郑肖利刘薇顾芃
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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