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A kind of docetaxel composite sustained release agent and preparation method thereof

A technology of docetaxel and sustained-release preparations, which is applied in the field of pharmaceutical anti-tumor drug preparations, can solve the problems of limited application, and achieve the effects of high drug loading, good stability and low toxicity

Active Publication Date: 2020-11-06
昌吉市威特医用材料科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the toxicity of DTX to the heart, lungs and other organs has also been reported, and these toxic and side effects greatly limit its application.

Method used

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  • A kind of docetaxel composite sustained release agent and preparation method thereof
  • A kind of docetaxel composite sustained release agent and preparation method thereof
  • A kind of docetaxel composite sustained release agent and preparation method thereof

Examples

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preparation example Construction

[0026] The present invention relates to a kind of preparation method of docetaxel composite sustained-release agent, comprising the following steps:

[0027] S1: Dissolve docetaxel powder and lecithin in a tetrahydrofuran solvent, and react in a water bath at 45°C for 3 hours to obtain a docetaxel-phospholipid complex solution;

[0028] S2: removing aprotic tetrahydrofuran, which is easy to form complexes, in the docetaxel-phospholipid complex solution by rotary evaporation to obtain the docetaxel-phospholipid complex;

[0029] S3: putting the above docetaxel phospholipid complex into n-hexane solvent, and collecting the docetaxel phospholipid complex in n-hexane solvent by filtration;

[0030] S4: Remove the n-hexane in the docetaxel phospholipid complex by rotary evaporation (docetaxel is insoluble in n-hexane), and obtain a pale yellow docetaxel phospholipid complex by drying;

[0031] S5: putting the above light yellow docetaxel phospholipid complex, cholesterol, and polo...

Embodiment 1

[0046] A preparation method of docetaxel composite slow-release agent, comprising the following steps:

[0047] S1: dissolving docetaxel powder and soybean lecithin (mass ratio: 1:5) in an aprotic tetrahydrofuran solvent that is easy to form a complex, and reacting in a water bath at 45°C for 3 hours to obtain a docetaxel-phospholipid complex solution;

[0048] S2: removing tetrahydrofuran in the docetaxel-phospholipid complex solution by rotary evaporation to obtain the docetaxel-phospholipid complex;

[0049] S3: putting the above docetaxel phospholipid complex into n-hexane solvent, and collecting the docetaxel phospholipid complex in n-hexane solvent by filtration;

[0050] S4: remove n-hexane in the docetaxel phospholipid complex by rotary evaporation, and obtain a light yellow docetaxel phospholipid complex by drying;

[0051] S5: Put the above light yellow docetaxel phospholipid complex, cholesterol and poloxamer into tetrahydrofuran to obtain an organic solution conta...

Embodiment 2

[0057] A method for preparing the docetaxel composite slow-release preparation as described in Example 1, wherein the mass ratio of docetaxel powder and soybean lecithin in S1 is: 1:4.

[0058] The average particle size of the docetaxel composite slow-release agent prepared by this method is about 130nm, and the drug loading is 14.42%.

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Abstract

The invention relates to the field of pharmaceutical antitumor drug preparations, in particular to a docetaxel composite slow-release agent and a preparation method thereof. The docetaxel composite slow-release agent is prepared by: compositing docetaxel powder and lecithin via tetrahydrofuran, washing via n-hexane, performing vacuum rotary evaporation, ultrafiltering, and lyophilizing. The docetaxel composite slow-release agent related herein has good stability; compared with docetaxel liposomes, the docetaxel composite slow-release agent has the advantages of high carrying capacity, long cycle, low toxicity, good treatment effect and the like since docetaxel and phospholipids take effect not through simple encapsulating of drug in a vesical via phospholipids but through weak interaction.

Description

technical field [0001] The invention relates to the field of pharmaceutical antitumor drug preparations, in particular to a docetaxel composite slow-release agent and a preparation method thereof. Background technique [0002] Docetaxel (DTX), CAS number 33069-62-4, Mr 807.8792, also known as docetaxel. It is a paclitaxel derivative, an anti-cancer drug directly extracted from the leaves or needles of the natural plant yew yew. DTX is white or off-white crystalline powder with a melting point of 213°C. It has good fat solubility, easily soluble in ethanol, acetone, ether, benzene and other organic solvents, very insoluble in water and n-hexane. [0003] Mechanism of DTX: The pharmacological effects of DTX are similar to those of other paclitaxel derivatives. Microtubules are an important component of eukaryotic cells, which are formed by microtubule dimers composed of two similar polypeptide subunits. Under normal conditions, there is a dynamic equilibrium between microt...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/337A61K47/24A61K47/26A61P35/00
CPCA61K9/5123A61K31/337A61K47/26
Inventor 侯振清范仲雄侯鲁
Owner 昌吉市威特医用材料科技有限公司
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