Docetaxel long-circulating liposome and preparation method thereof

A long-circulating liposome and docetaxel technology, which is applied in the directions of liposome delivery, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve problems such as systemic toxicity, damage, and clinical application limitations, and achieve increased curative effect. , avoid phagocytosis, increase the effect of stability

Inactive Publication Date: 2010-11-17
SHANGHAI GENE CELL BIO MEDICAL TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a cytotoxic antineoplastic drug, docetaxel has systemic toxicity, especially immune system toxicity such as neutropenia, which has caused great damage to the patient's body and mind, and its clinical application has also been limited.

Method used

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  • Docetaxel long-circulating liposome and preparation method thereof
  • Docetaxel long-circulating liposome and preparation method thereof
  • Docetaxel long-circulating liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Dissolve 1.0 mg of docetaxel, 100.0 mg of soybean lecithin, and 8.0 mg of cholesterol in 10 ml of ethanol to obtain solution A.

[0024] Film A was formed into a film by rotary evaporation in a water bath at 40°C to obtain film B.

[0025] Dissolve 200 mg of poloxamer in 5 ml of phosphate buffer at pH=6.8 to obtain solution C.

[0026] Add solution C to membrane B, refrigerate at below 4°C for 30 minutes to fully hydrate the membrane, and then vortex for 15 minutes to prepare the product.

[0027] Apply Sephadex column to separate liposome and unencapsulated free drug, add methanol to dissolve, take methanol solution and apply high performance liquid chromatography to measure peak area, substitute peak area into regression equation to find concentration, calculate encapsulation The sealing rate is 90.3%.

[0028] Take about 10.0mg of the raw material drug, weigh it accurately, put it in a 10ml measuring bottle, add methanol to dissolve it ultrasonically, let it cool d...

Embodiment 2

[0033] Dissolve 4 mg of docetaxel, 80 mg of phosphatidylcholine, and 10 mg of cholesterol in 10 ml of ethanol and chloroform mixture (1:1, volume ratio) to obtain solution A.

[0034] Film A was formed into a film by rotary evaporation in a water bath at 40°C to obtain film B.

[0035] Dissolve 200 mg of poloxamer in 5 ml of pH=9 phosphate buffer to obtain solution C.

[0036] Add solution C to membrane B, refrigerate below -4°C for 30 minutes to fully hydrate the membrane, and then vortex and mix for 15 minutes to prepare the product.

Embodiment 3

[0038] By tail vein administration of embodiment 1 and docetaxel injection, measure two kinds of dosage forms median lethal dose (LD 50 ), using the modified Cole’s method to calculate, the results are as follows: the acute toxicity of docetaxel long-circulation liposome is significantly less than that of docetaxel injection, LD 50 The dose is more than twice that of docetaxel injection, indicating that the prepared long-circulating liposome of docetaxel can reduce the toxicity of the drug. The results are shown in the table below:

[0039] Docetaxel Injection and Docetaxel Long Circulation Liposome LD 50 (x±s)

[0040]

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Abstract

The invention aims to provide a method for preparing a docetaxel long-circulating liposome. The method comprises the following steps of: dissolving docetaxel and carrier materials such as phospholipid, cholesterol and the like together in an organic solvent; forming a film through rotary evaporation in a 40 to 70 DEG C water bath; adding buffer solution which contains a surfactant and performing refrigeration at the temperature of below 4 DEG C for 10 to 60 minutes to fully hydrate the film; and then mixing or stirring to obtain the docetaxel liposome. The liposome of 70 to 500nm is prepared from the docetaxel and can be prepared into docetaxel long-circulating liposome frozen powder for injection by lyophilization.

Description

technical field [0001] The invention relates to a docetaxel preparation and a preparation method thereof. Background technique [0002] Docetaxel is a taxane antineoplastic drug, which is semi-synthesized from the extract from the needle leaves of Taxus baccata, Europeyew or from the precursor compound extracted from the regenerable taxus needle-shaped organisms Come. The dosage form currently on the market is an injection, which first dissolves the drug in Tween 80. Before clinical use, it is diluted to 1 mg / ml with 13% ethanol aqueous solution, and when administered, it is further diluted with 5% glucose solution to make the final When the drug concentration reaches 0.3-0.9 mg / L, the diluted injection should be used within 4 hours, otherwise precipitation may occur. The study found that the transient moderate hypersensitivity induced by Tween-80 was related to the possible fluid retention caused by Tween-80. Therefore, antihistamines and phenanthrene anti-inflammatory d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/28A61P35/00
Inventor 奉建芳罗远黄盼华
Owner SHANGHAI GENE CELL BIO MEDICAL TECH
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