Liposome preparation of teniposide phospholipid complexes and prepraring method thereof

A technology 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: 2008-10-29
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 phospholipi

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 it to tetrahydrofuran, heat and reflux for 30 minutes at 30°C, until the solution is clear, evaporate and remove tetrahydrofuran by rotating thin film evaporation solvent method to obtain light yellow crystals Teniposide Phospholipid Complex. Take 5.0g of teniposide phospholipid complex, 10g of soy lecithin, and 5g of cholesterol, add it to chloroform, at 40℃, use rotating film to evaporate the solvent to remove the chloroform, add PBS (pH7.4) buffer to water After that, 50 g of sucrose is added to make it fully dissolved, and the resulting liposome suspension is homogenized under high pressure, and then divided and lyophilized to obtain a teniposide liposome lyophilized preparation.

Embodiment 2

[0038] Weigh 65.6g of teniposide and 75g of soy lecithin, add them to acetone, heat and reflux for 60 minutes at 40°C, until the solution is clear, evaporate and remove the acetone by a rotating film evaporation solvent method to obtain a pale yellow crystal. Niposide Phospholipid Complex. Take 50g of teniposide phospholipid complex, 100g of soy lecithin, and 50g of cholesterol, add them to chloroform, and evaporate and remove the chloroform at 40℃ by rotating the thin film solvent method, and add PBS (pH7.4) buffer to fully hydrate Then, 750g of trehalose was added to fully dissolve it, and the resulting liposome suspension was homogenized under high pressure, and then subpackaged and lyophilized to obtain a teniposide liposome lyophilized preparation.

Embodiment 3

[0040] Weigh 131.2g of teniposide and 150g of dimyristoylphosphatidylcholine, add them to tetrahydrofuran, heat and reflux for 120 minutes at 50°C, until the solution is clear, evaporate and remove the tetrahydrofuran by the method of evaporating the solvent on a rotating film to obtain Light yellow crystalline teniposide phospholipid complex. Take 100g of teniposide phospholipid complex, 200g of soybean lecithin, and 100g of cholesterol, add it to chloroform, at 40℃, use rotating film to volatilize the solvent to remove the chloroform, add PBS (pH6.8) buffer to fully hydrate Then, 1500g of trehalose was added to fully dissolve it, and the resulting liposome suspension was homogenized under high pressure, and then subpackaged and lyophilized to obtain a teniposide liposome lyophilized preparation.

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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 of the 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, velvet, vietnam 26, podosulfuryl methylene glucoside, Banglai, podophylloside, podophylloside thiophene Glycoside, Methylpodophylloside. Teniposide is an anti-cancer alkaloid proposed from plants of the genus Cephalotaxus. It can inhibit the synthesis of eukaryotic proteins, depolymerize polyribosomes, and interfere with the function of protein ribosomes. Teniposide is a cycle-specific cytotoxic drug that acts in the late S2 and G2 phases of the cell cycle, and works by preventing cell mitosis. It can also cause single-stranded and double-stranded breaks in DNA bonds, and its mechanism of action may be caused by the inhibition of type II topoisomerase. Teniposide has a significant curative effect, and clinical ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7048A61K47/24A61P35/00
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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