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Method for preparation of ultrasound micro bubbles carrying docetaxel lipid

A technology of docetaxel and ultrasonic microbubbles is applied in the field of preparing docetaxel-loaded lipid ultrasonic microbubbles, which can solve the problems of poor water solubility and limited, and achieve the effects of uniform distribution, improved ablation effect, and neat and round shape.

Inactive Publication Date: 2015-02-25
张悦
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility and good fat solubility of docetaxel, its clinical application is limited.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Take 2 mg of docetaxel, 1 mg of DPPC reagent, 2 mg of DPPE reagent, 5 mg of DSPA reagent and an appropriate amount of cholesterol, add an organic solvent to fully dissolve, cool to room temperature, add 450 μl of PBS solution with a pH value of 5.0, 50 μl of glycerin, and an appropriate amount of cholesterol, and mix thoroughly Seal it, incubate it in a constant temperature device at 50°C to form a thin film, fill it with perfluoropropane to replace the air in the airtight container, place it in an amalgam blender and vibrate for 30 seconds, and it is ready.

Embodiment 2

[0023] Take 1 mg of docetaxel, 0.5 mg of DPPC reagent, 1 mg of DPPE reagent, 3 mg of DSPA reagent and appropriate amount of cholesterol, add organic solvent to fully dissolve, cool to room temperature, add 200 μl of PBS solution with pH value less than 4.0, 40 μl of glycerin, appropriate amount of cholesterol, and mix well After sealing, place it in a constant temperature device at 60°C to incubate to form a thin film, fill it with perfluoropropane to replace the air in the airtight container, place it in an amalgam blender and vibrate for 35 seconds to obtain the product.

Embodiment 3

[0025] Take 5 mg of docetaxel, 2 mg of DPPC reagent, 4 mg of DPPE reagent, 10 mg of DSPA reagent and appropriate amount of cholesterol, add an organic solvent to fully dissolve, cool to room temperature, add 800 μl of PBS solution with a pH value less than 3.0, 60 μl of glycerin, and appropriate amount of cholesterol, and mix thoroughly Seal it, place it in a constant temperature device at 40°C to incubate to form a thin film, fill it with perfluoropropane to replace the air in the closed container, place it in an amalgam blender and vibrate for 40 seconds, and you get it.

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Abstract

The invention relates to a method for preparation of ultrasound micro bubbles carrying docetaxel lipid, main chemical reagent used in the method are DPPC (dipalmitoyl phosphatidylcholine), DPPE (dipalmitoyl phosphoethanolamine), DSPA, cholesterol and PBS solution, and a novel and efficient drug administration route for the treatment of liver cancer is ultimately provided.

Description

technical field [0001] The invention relates to a method for preparing docetaxel-loaded lipid ultrasonic microbubbles, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Primary liver cancer is the sixth most common malignant tumor in the world. There are about 1 million new patients with liver cancer every year worldwide. The 5-year survival rate of patients is less than 10%. The median survival time of patients who lose the chance of surgery is only For 4-6 months, the prognosis is extremely poor, ranking third in the cause of death caused by cancer. Due to the high infection rate of HBV and HCV in our population, the morbidity and mortality of liver cancer rank first in the world. Therefore, research on the treatment of liver cancer is particularly important and necessary. Surgical resection is still the preferred treatment for liver cancer at present, however, only 10%-15% of patients have the opportunity for surgery when they...

Claims

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Application Information

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IPC IPC(8): A61K49/22A61K41/00A61K31/337A61K9/00A61P1/16A61P35/00
Inventor 张悦
Owner 张悦
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