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Oxaliplatinum liposome glucose preparation and its preparation method and application

A technology of oxaliplatin and liposome, applied in the field of oxaliplatin liposome glucose preparation and preparation thereof, can solve the problems of easy decomposition, low solubility, etc., so as to improve the anticancer effect, reduce pain, and improve the Effects on quality of life

Active Publication Date: 2008-01-16
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nanoparticles with a particle size of less than 200nm can remain stable in the blood for a long time, effectively enter the cancer tissue for a long time, achieve the anti-cancer effect of passive targeting, and solve the problem of the solubility of oxaliplatin non-liposomal preparations in the blood Low, easy to be decomposed, while reducing the side effects of oxaliplatin, greatly improving the anticancer efficacy of oxaliplatin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] (Recipe 1)

[0021] Hydrogen Phosphate 30g

[0022] Cholesterol 30g

[0023] DSPE-PEG2000 30g

[0024] Oxaliplatin 7.2g

[0025] Weigh hydrogenated phospholipids, cholesterol, DSPE-PEG2000, mix and add 900ml of tert-butanol and stir to dissolve, pre-cool to -35°C, after 12 hours of freeze-drying, add 900ml of 4% glucose oxaliplatin saturated aqueous solution , under the heating condition of 45°C, stir, dissolve and emulsify through a milk homogenizer, and prepare a liposome solution through a homogenizer, a nano extruder (equipped with a 100-200nm microporous filter membrane), etc. Then it is separated and refined through a filter column to prepare an oxaliplatin liposome glucose solution. After being sterilized by filtration through a 0.22 μm microporous membrane, the filtrate was divided into 30 ml vials, 25 ml per bottle, stoppered, plugged, packaged, and prepared into a solution for injection.

[0026] The oxaliplatin liposome glucose solution prepared above wa...

Embodiment 2

[0029] (Recipe 2)

[0030] Hydrogen Phosphate 50g

[0031] Cholesterol 20g

[0032] DSPE-PEG2000 20g

[0033] Oxaliplatin 14.4g

[0034] Weigh hydrogenated phospholipids, cholesterol, DSPE-PEG2000, mix and add 900ml of tert-butanol, stir to dissolve, pre-cool to -38°C, after 18 hours of freeze-drying, add 7% glucose oxaliplatin saturated aqueous solution 1800ml , under the condition of heating at 55°C, stir, dissolve and emulsify through a milk homogenizer, and prepare a liposome solution through a homogenizer, a nano extruder (equipped with a 100-200nm microporous filter membrane), etc. Then it is separated and refined through a filter column to prepare an oxaliplatin liposome glucose solution. After being sterilized by filtration through a 0.22 μm microporous membrane, the filtrate was divided into 30 ml vials, 25 ml per bottle, stoppered, plugged, packaged, and prepared into a solution for injection.

[0035] The oxaliplatin liposome glucose solution prepared above was...

Embodiment 3

[0038] (Recipe 3)

[0039] Hydrogen Phosphate 50g

[0040] Cholesterol 5g

[0041] DSPE-PEG2000 10g

[0042] Oxaliplatin 15.6g

[0043] Weigh hydrogenated phospholipids, cholesterol, DSPE-PEG2000, mix and add 900ml of tert-butanol and stir to dissolve, pre-cool to -40°C, after 24 hours of freeze-drying, add 10% glucose oxaliplatin saturated aqueous solution 1950ml , under the condition of heating at 60°C, stir, dissolve and emulsify through a milk homogenizer, and prepare a liposome solution through a homogenizer, a nano extruder (equipped with a 100-200nm microporous filter membrane), etc. Then it is separated and refined through a filter column to prepare an oxaliplatin liposome glucose solution. After being sterilized by filtration through a 0.22 μm microporous membrane, the filtrate was dispensed into 30 ml vials, 25 ml per bottle, stoppered, tamped, and packaged to prepare a solution for injection.

[0044] The oxaliplatin liposome glucose solution prepared above was s...

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Abstract

The invention discloses an oxaliplatin liposome glucose preparation and the preparation method and application, relating to an oxaliplatin liposome glucose solution preparation used for tumor resistance and the preparation method and application. An oxaliplatin liposome glucose preparation is formed by liposome which prepared by oxaliplatin, hydrogenated phosphorus, cholesterol and DSPE-PEG2000, and is dissolved in glucose solution; wherein the weight ratio of the hydrogenated phosophorus and the oxaliplatin is 1:1-50; the weight ratio of the hydrogenated phosophorus, cholesterol and the DSPE-PEG2000. The preparation method is that the hydrogenated phosophorus, cholesterol and the DSPE-PEG2000 are weighed according to proportioning by weight in a description and then fixed together; tertiary butyl alcohol is added into the fixture for the fixture to be stirred and dissolved, then the fixture is precooled; the oxaliplatin saturated water solution with 4-10 percent of glucose after cooling and drying is stirred, dissolved and emulsified by an emulsion balancing machine and then prepared into liposome solution by a homogenizer and a nanometer extruder, separated and refined through a filter column to prepare the oxaliplatin liposome glucose solution.

Description

technical field [0001] The invention relates to an oxaliplatin liposome glucose preparation and its preparation method and application, and relates to an anti-tumor oxaliplatin liposome glucose solution preparation and its preparation method and application. Background technique [0002] Oxaliplatin, as a derivative of the anti-tumor drug cisplatin, has been widely used in the treatment of various tumors. Compared with cisplatin, oxaliplatin has the characteristics of milder inhibition of bone marrow function, weaker gastrointestinal reaction, lower renal toxicity, and no cross-resistance with cisplatin. However, as an antineoplastic drug, oxaliplatin still has disadvantages such as low solubility, easy to be decomposed and destroyed, bone marrow suppression and renal toxicity. [0003] Liposomes are often used to reduce the toxicity of drugs, increase the concentration of poorly soluble drugs in the blood, and maintain long-term effective drug concentrations, especially in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/282A61K9/127A61K9/19A61K47/24A61P35/00
Inventor 陈祥峰蔡课霞
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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