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Cabazitaxel lipid microsphere injection and preparation method thereof

A technology of cabazitaxel and lipid microspheres, which is applied in the field of medicine to achieve high dilution resistance, excellent market prospects, and good dilution resistance

Inactive Publication Date: 2015-01-28
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] After patent and literature search, there is no report on the study of lipid microsphere preparations involving cabazitaxel cholesterol complexes and amphiphilic polyamino acids

Method used

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  • Cabazitaxel lipid microsphere injection and preparation method thereof
  • Cabazitaxel lipid microsphere injection and preparation method thereof
  • Cabazitaxel lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of cabazitaxel cholesterol complex

[0057] Place 0.1 g of cabazitaxel and 0.3 g of cholesterol in a round-bottomed flask, slowly add ether to immerse the cholesterol and drugs in the ether, and heat and reflux for 2 hours at 60°C to obtain a clear reaction solution, which is dried under reduced pressure to remove Solvent, namely cabazitaxel cholesterol complex.

Embodiment 2

[0059] Preparation of cabazitaxel cholesterol complex

[0060] Place 0.1 g of cabazitaxel and 0.2 g of cholesterol in a round-bottomed flask, slowly add ethyl acetate to immerse the cholesterol and the drug in the ethyl acetate, and heat and reflux at 50°C for 1 hour to obtain a clear reaction solution. Rotary evaporation is used to evaporate the dry solvent to obtain cabazitaxel cholesterol complex.

Embodiment 3

[0062] Preparation of cabazitaxel cholesterol complex

[0063] Place 0.1g of cabazitaxel and 0.25g of cholesterol in a round-bottomed flask, slowly add chloroform to immerse the cholesterol and the drug in the chloroform, heat and reflux for 1 hour at 60°C to obtain a clear reaction solution, and evaporate the dry solvent , That is, cabazitaxel cholesterol complex.

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Abstract

The invention relates to a cabazitaxel lipid microsphere injection and a preparation method thereof. The injection comprises the following components in percentage by weight: 0.01% to 1 % of cabazitaxel cholesterol complex (based on cabazitaxel), 5% to 30% of oil for injection; 1% to 6% of phospholipid for injection, 0.2% to 0.7% of auxiliary emulsifier, 0.05% to 1.0% of amphiphilic polyamino, 2.0% to 3.5% of osmotic pressure modifier, the balance being water for injection. The cabazitaxel lipid microsphere injection is prepared by using phospholipid as an emulsifier, a surfactant as a coemulsifier, and high-purity cabazitaxel as an active ingredient, and adding cholesterol, amphiphilic polyamino acids, an osmotic pressure modifier and water for injection through an ultrahigh pressure microjet nano-dispersion technology. By means of the unique interaction of cholesterol and drugs, the chemical stability of cabazitaxel in lipid microspheres is improved, and the thermodynamic stability of cabazitaxel in the lipid microspheres is also improved. The stability of a preparation is further enhanced by adding the amphiphilic polyamino acids provided by the invention.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a cabazitaxel lipid microsphere injection and a preparation method thereof. Background technique [0002] Cancer is a serious threat to human life and health. With the increase of industrialization, the increase of environmental pollution and the general extension of human life, the incidence of cancer is increasing year by year. According to the World Health Organization (WHO), there are currently 24.6 million cancer patients worldwide; by 2020, it is estimated that it will reach 30 million. In 2005, 7.6 million people died of cancer, accounting for 13% of the 58 million deaths in the world. By 2020, cancer could cause more than 10 million deaths each year. If this trend continues, the estimated number of new cases each year is expected to increase from 10.9 million in 2002 to 16 million in 2020. There were nearly 1.9 million cancer deaths in China in 2005, and 1.2 mill...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/42A61K31/337A61P35/00
Inventor 唐星张宇张岩蔡翠芳
Owner SHENYANG PHARMA UNIVERSITY
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