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Method for preparing etoposide ultrafine particles by supercutical fluid technology

A technology of etoposide and ultra-fine particles, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, powder delivery, etc. It can solve the problems of organic solvent residues, wide product particle size distribution, variability, etc., and achieve solubility Improved effect

Active Publication Date: 2015-11-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used drug micronization techniques include grinding method, spray drying method, recrystallization method, jet milling method, freeze drying method, etc., but these methods have disadvantages such as organic solvent residue, wide particle size distribution of the product, and variability.

Method used

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  • Method for preparing etoposide ultrafine particles by supercutical fluid technology
  • Method for preparing etoposide ultrafine particles by supercutical fluid technology
  • Method for preparing etoposide ultrafine particles by supercutical fluid technology

Examples

Experimental program
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Embodiment

[0028] Weigh 100 mg of etoposide raw material, dissolve in 10 mL of acetone to form a solution. Set the pressure in the crystallization tank to 10MPa, the temperature to 40°C, and remove the air in the tank. After the pressure and temperature are constant, adjust the flow control valve to keep the CO 2 The exhaust speed is 10L / min, start the high-efficiency liquid phase pump, and the solution is input into the crystallization kettle at a speed of 1mL / min. After the solution completely enters the crystallization kettle, keep the gas in and out for more than 30min. Subsequent shutdown of the CO 2 Inlet valve, depressurize and remove sample.

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PUM

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Abstract

The invention relates to a method for preparing etoposide ultrafine particles by a supercutical anti-solvent crystallization technology. The method can prepare the etoposide ultrafine particles with improved solubility. Through change of drug solvent types, a solution concentration, crystallization pressure, a crystallization temperature and a solution sample introduction flow velocity, drug particle sizes are effectively controlled in a range of 1-10 microns. The prepared etoposide ultrafine particles have a high dissolution rate.

Description

technical field [0001] The invention relates to a method for preparing etoposide ultrafine particles, in particular to a method for preparing etoposide ultrafine particles using supercritical fluid crystallization technology. Background technique [0002] Etoposide is a cell cycle specific anti-tumor drug, generally used in the treatment of small cell lung cancer, non-small cell lung cancer, malignant lymphoma, gastric cancer, ovarian cancer and esophageal cancer. Etoposide belongs to the semi-synthetic derivatives of podophyllin lipids, and its water solubility is poor (the solubility at room temperature is 58.7mg / L, and the solubility at 37°C is 148-153mg / L), and its dissolution rate is also very slow, low At 0.01mg / (min·cm 2 ). The solubility and absorbability of drug active ingredients in the digestive juice of the gastrointestinal tract determine the bioavailability of oral medication, and poorly soluble or water-insoluble drugs cannot be effectively dissolved in the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/7048A61P35/00
Inventor 王志祥程月颜庭轩黄德春缪虹刚
Owner CHINA PHARM UNIV