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New formulation oxaliplatin liposome

A technology of oxaliplatin and liposomes, which is applied in the field of medicine, can solve the problems of preparations such as high irritation, poor quality, and high production costs, and achieve the effects of improving curative effect and poor oral absorption

Inactive Publication Date: 2006-05-24
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

[0012] Preparation of oxaliplatin liposomes by ethanol injection method: take soybean phospholipids, cholesterol, VE and add absolute ethanol to dissolve and inject into oxaliplatin aqueous solution, stir at constant temperature and high speed, evaporate under reduced pressure to remove ethanol, pass through a microporous membrane for sizing , to obtain oxaliplatin liposomes, and the encapsulation efficiency can reach 72.8%.

Embodiment 2

[0014] Preparation of oxaliplatin liposomes by film dispersion method: take soybean lecithin, cholesterol, VE and dissolve them in 150ml eggplant-shaped bottle with 15ml chloroform, form a film under reduced pressure on a rotary thin film evaporator and remove all organic solvents, add 10ml oxaliplatin The oxaliplatin liposome is obtained by hydrating the aqueous solution of the liposome, passing through a microporous membrane to obtain the liposome, and the encapsulation efficiency can reach 70.1%.

Embodiment 3

[0016] Prepare oxaliplatin liposomes by reverse-phase evaporation: weigh soybean lecithin, cholesterol, VE and add 5ml chloroform to dissolve, then add 10ml ether, then add 15ml oxaliplatin in phosphate buffer, bath ultrasonic A homogeneous single-phase system was formed, and the chloroform ether was evaporated under reduced pressure to form a gel. Continue to evaporate under reduced pressure for 5 to 10 minutes, and vortex until the aqueous suspension, that is, liposome, was formed. Encapsulation efficiency can reach 37.5%.

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PUM

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Abstract

The present invention relates to a new-type preparation-oxalibol liposome and its preparation method. It is a liposome or precursor liposome prepared by using oxalibol and auxiliary materials of phospholipid and cholesterol, in which the auxiliary materials of supporting agent, etc. also can be added. The film material phospholipid can adopt natural phospholipid or synthetic phospholipid, and the weight ratio of phospholipid and medicine is 0.1:1-50:1. Its preparation method can adopt ethyl alcohol injection method, film dispersion method, inverted evaporation method, extrusion method and mechanical method, and the supporting agent can be sorbitol, mannitol, cane sugar, sodium chloride, water soluble starch, dextran, glucose and lactose, and the ratio of supporting agent and phospholipid is 0.01:1-500:1. The oxalibol can be used for patient with carcinoma of colon and rectal carcinoma.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an oxaliplatin 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] Oxaliplatin Oxaliplatin did not appear the nephrotoxicity of cisplatin, nor the bone marrow toxicity of carboplatin. Belonging to a new platinum derivative, it acts on DNA by producing alkylated conjugates to form intra...

Claims

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Application Information

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IPC IPC(8): A61K31/555A61K9/127A61P35/00
Inventor 胡才忠
Owner 胡才忠
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