Gemcitabine or salt liposome thereof, and preparation method and application thereof

A gemcitabine and liposome technology, applied in the field of gemcitabine or its salt liposome and its preparation, can solve the problem of poor stability of gemcitabine liposome or nano-microsphere, adverse effects of drug stability and bioavailability, stability It can improve the encapsulation rate and stability, reduce the pain of medication, and reduce the effects of toxic and side effects.

Active Publication Date: 2012-11-21
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN101444485B discloses a kind of gemcitabine liposome, and this liposome comprises gemcitabine, phospholipid, cholesterol, but the encapsulation efficiency and dispersibility of this liposome all perform poorly, all have unfavorable to the stability of medicine and bioavailability influences
CN101926779A discloses a gemcitabine solid lipid nanoparticle and a preparation method thereof. The preparation still has the problems of low drug encapsulation efficiency and poor stability, and the drug is partially degraded after storage for about 3 months
[0007] Judging from the current research results, gemcitabine liposomes or nanospheres prepared by existing methods have problems such as poor stability, easy aggregation in aqueous solution, overall erosion or surface degradation, and cannot be practically applied in clinical practice.

Method used

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  • Gemcitabine or salt liposome thereof, and preparation method and application thereof
  • Gemcitabine or salt liposome thereof, and preparation method and application thereof
  • Gemcitabine or salt liposome thereof, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027]

[0028] Preparation:

[0029] Step 1, preparation of gemcitabine hydrochloride oil solution. Under the protection of an inert gas, add 10 g of gemcitabine hydrochloride to 150 g of soybean oil for injection, stir at a high speed for 20 min in a constant temperature water bath at 40°C, transfer the mixed solution to a high-pressure homogenizer and homogenize for 15 min until the average particle size is below 100 nm .

[0030] Step 2, preparation of blank liposomes. Weigh 600g of soybean lecithin and 100g of cholesterol and dissolve them in an appropriate amount of ether, add an appropriate amount of ammonium sulfate solution with a concentration of 200mmol / L to the above lipid solution under stirring, and ultrasonicate in a water bath under stirring until a stable W / O emulsion is formed Then transfer it to a round-bottomed flask, and remove part of the ether by rotary evaporation at 50°C under reduced pressure.

[0031] Step 3, preparation of gemcitabine hydrochl...

Embodiment 2

[0033] The composition of the prescription, the content of each component, and the preparation method are the same as in Example 1, except that during the preparation of the gemcitabine hydrochloride oil solution, the mixture was stirred at a high speed for 10 minutes in a constant temperature water bath at 40°C, and the mixed solution was transferred to a high-pressure homogenizer to homogenize the mixture. For 15min, until the average particle size is below 120nm.

Embodiment 3

[0035] The composition of the prescription, the content of each component, and the preparation method are the same as in Example 1, except that during the preparation of the gemcitabine hydrochloride oil solution, the mixture was stirred at a high speed for 45 minutes in a constant temperature water bath at 40°C, and the mixed solution was transferred to a high-pressure homogenizer to homogenize the mixture. For 20min, until the average particle size is below 50nm.

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Abstract

The present invention relates to a gemcitabine or a salt sodium liposome thereof, and a preparation method and application thereof. The liposome comprises gemcitabine or the salt thereof, injection oil, phospholipid and cholesterol in a mass ratio of 1:1-20:50-70:5-30. The injection has good encapsulation efficiency, better stability, and lower side effect.

Description

technical field [0001] The invention relates to a novel preparation of gemcitabine or its salt and a preparation method thereof, in particular to a liposome of gemcitabine or its salt, its preparation method and application. Background technique [0002] Gemcitabine is a difluoronucleoside antimetabolite anticancer drug that disrupts cell replication. It is a water-soluble analog of deoxycytidine and is an inhibitory substrate for ribonucleotide reductase. , this enzyme is critical for the generation of deoxynucleotides required during DNA synthesis and repair. It has the characteristics of broad anti-tumor spectrum, unique mechanism of action, no cross-resistance with other chemotherapy drugs, and no superposition of toxic reactions. [0003] As a prodrug, gemcitabine is a good substrate for deoxythymidine kinase phosphorylation in the cell, and is converted into the following metabolites under the action of the enzyme: gemcitabine monophosphate (dFdCMP), gemcitabine dipho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7068A61P35/00
Inventor 宋阳张春红吕爱锋
Owner JIANGSU HANSOH PHARMA CO LTD
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