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Oxaliplatin liposome, preparation method and application thereof

A technology of oxaliplatin and liposomes, which is applied in the field of oxaliplatin liposomes and its preparation, can solve the problems of poor popularity, harsh conditions in the fusion process of reversed micelles and blank liposome membranes, and Issues such as low sealing rate

Inactive Publication Date: 2010-12-01
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The acidic phospholipids used in this patent are synthetic phospholipids, which are expensive; the prepared drug-phospholipid conjugate reversed-phase micelles can remain stable above 50°C, and a large amount of precipitation will rapidly occur below 50°C; reversed-phase micelles and The membrane fusion process of blank liposomes is under harsh conditions, and precipitation is easily produced after the two are mixed.
The technical requirements of the whole process are relatively high, and the popularity is not strong
In addition, Yang Meiyan's doctoral thesis "Oxaliplatin long-cycle thermosensitive liposome research" used the freeze-thaw cycle process to try to improve the encapsulation efficiency of liposomes, but the result was only to increase the encapsulation efficiency to 30%, which was not very good. Good solution to the problem of low encapsulation rate

Method used

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preparation example Construction

[0058] The invention provides a method for preparing oxaliplatin liposomes, which is to make the reverse micelles spontaneously transform into liposomes by removing the organic solvent in the reverse micelles composition on the basis of preparing the reverse micelles composition.

[0059] The preparation method of reverse micelles comprises the following steps:

[0060] (1) mixing cholesterol, phospholipids and an organic solvent to obtain an organic phase;

[0061] (2) Oxaliplatin and buffer are mixed to obtain an aqueous phase; and

[0062] (3) Mix the organic phase and the aqueous phase obtained in steps (1) and (2) to obtain reversed-phase micelles.

[0063] The weight ratio of oxaliplatin and phospholipid is 1:3-20; the weight ratio of cholesterol and phospholipid is 1:2-10; the organic solvent is selected from chloroform, ether, or a mixture thereof; the mixture of chloroform and ether The volume ratio of the two is 1:4-4:1.

[0064] The buffer solution has a pH of 5....

Embodiment 1

[0087] Preparation of stable reverse micelles I

[0088]

[0089] cholesterol

[0090] Preparation method: Take natural egg yolk phospholipids (purity is 90%) and cholesterol according to the prescription amount, place them in an eggplant-shaped bottle, add 10ml of chloroform / ether mixed solvent (4:1, v / v) to dissolve them; weigh 4.0 mg oxaliplatin was dissolved in 1 ml of acetic acid-sodium acetate buffer (0.05M, pH 5.0), and then added to the lipid solution. After vortex mixing, short-term ultrasonication in an ice bath forms a stable reversed-phase micelle I, which exists stably at room temperature for more than 30 minutes.

Embodiment 2

[0092] Preparation of stable reverse micelles II

[0093] Oxaliplatin

[0094] Preparation method: Take natural egg yolk phospholipids (purity is 75%) and cholesterol according to the prescription, place them in eggplant-shaped bottles, add 3ml of chloroform / ether mixed solvent (1:4, v / v) to dissolve them; weigh 8.0 mg oxaliplatin was dissolved in 1 ml of citric acid-sodium citrate buffer (1M, pH 6.2), and then added to the lipid solution. After vortex mixing, short-time ice-bath sonication forms a stable reversed-phase micelle II, which exists stably at room temperature for more than 30 minutes.

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Abstract

The invention discloses an oxaliplatin liposome, a preparation method and application thereof. The oxaliplatin liposome contains oxaliplatin, phospholipid and cholesterol, wherein, based on the total weight of the phospholipid, the phospholipid comprises the following components in percentage by weight: 75 to 90 percent of phosphatidylcholine (PC), and 10 to 25 percent of phosphatidyl glycerol (PG) and phosphatidic acid (PA); the weight ratio of the oxaliplatin to the phospholipid is 1:3-20, and the weight ratio of the cholesterol to the phospholipid is 1:2-10.

Description

technical field [0001] The invention relates to the field of drug liposomes, in particular to an oxaliplatin liposome and a preparation method and application thereof. Background technique [0002] Oxaliplatin is the third-generation platinum anticancer drug, researched and developed by Debi opharm in Switzerland, produced and sold by Sanofi in France, and first launched in France in October 1996. In 2004, the FDA approved oxaliplatin for injection in combination with 5-fluorouracil and folinic acid for the first-line treatment of advanced colorectal cancer. The currently marketed oxaliplatin preparations include aqueous injection and freeze-dried powder injection. Oxaliplatin has a significant effect on advanced colorectal cancer, but with the extensive clinical application of oxaliplatin, its adverse reactions have been continuously discovered and reported. Neurotoxicity is the most common dose-limiting toxicity of oxaliplatin, about 85%-95% of patients have acute and tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/282A61K31/194A61P35/00
Inventor 陶涛贺宁
Owner SHANGHAI INST OF PHARMA IND CO LTD
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