A kind of cabazitaxel lipid microsphere injection and preparation method thereof

A technology of cabazitaxel and lipid microspheres, applied in the field of medicine, to achieve the effect of prolonging the half-life, meeting the needs of medication, and avoiding drug waste

Inactive Publication Date: 2017-08-04
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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  • A kind of cabazitaxel lipid microsphere injection and preparation method thereof
  • A kind of cabazitaxel lipid microsphere injection and preparation method thereof
  • A kind of cabazitaxel lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of Cabazitaxel Cholesterol Complex

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

Embodiment 2

[0059] Preparation of Cabazitaxel Cholesterol Complex

[0060] Put 0.1 g of cabazitaxel and 0.2 g of cholesterol in a round-bottomed flask, slowly add ethyl acetate, immerse the cholesterol and the drug in ethyl acetate, heat and reflux at 50°C for 1 hour to obtain a clear reaction solution, The solvent was dried by rotary evaporation to obtain the cholesterol complex of cabazitaxel.

Embodiment 3

[0062] Preparation of Cabazitaxel Cholesterol Complex

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

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Abstract

A cabazitaxel lipid microsphere injection and a preparation method thereof belong to the technical field of medicine. The components of the injection are by weight percentage: 0.01% to 1% of cabazitaxel cholesterol complex (calculated as cabazitaxel); Oil for injection 5% to 30%; phospholipids for injection 1% to 6%; auxiliary emulsifier 0.2% to 0.7%; amphiphilic polyamino 0.05% to 1.0%; osmotic pressure regulator 2.0% to 3.5%; the rest is Water for Injection. The preparation method uses phospholipids as emulsifiers, surfactants as auxiliary emulsifiers, high-purity cabazitaxel as active ingredients, and adding cholesterol, amphiphilic polyamino acids, osmotic pressure regulators and water for injection, using ultra-high pressure It is constructed by micro-fluidic nano-dispersion technology. The invention not only improves the chemical stability of the cabazitaxel in the lipid microsphere, but also improves the thermodynamic stability of the cabazitaxel lipid microsphere by virtue of the unique interaction between the cholesterol and the drug. The addition of the amphiphilic polyamino acid described in the present invention further increases the stability of the preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular 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 improvement of industrialization, the aggravation of environmental pollution and the general extension of human life expectancy, the incidence of cancer is increasing year by year. According to the report of the World Health Organization (WHO), there are currently 24.6 million cancer patients in the world; 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 worldwide. By 2020, cancer will cause more than 10 million deaths per year. If this trend continues, the estimated number of new cases per year is expected to increase from 10.9 million in 2002 to 16 million in 2020. In 2005, the number of cancer deaths in ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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