Super-critical anti-solvent preparation for water-soluble nano camptothecin powder

A supercritical anti-solvent, camptothecin technology, applied in the directions of medical preparations containing active ingredients, powder delivery, pharmaceutical formulations, etc., can solve the problems of destroying the drug structure, wide particle distribution, difficult to make medicine, etc., and achieve powder quality. High, narrow particle size distribution, easy operation

Inactive Publication Date: 2008-09-17
NORTHEAST FORESTRY UNIVERSITY +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Conventional drug nanopowder preparation methods are generally ball milling and jet milling. Although the particle size of the drug can be achieved, it has the disadvantages of high energy consumption, low efficiency, wide particle distribution, easy pollution, unsafe, easy to degrade and destroy the structure of the drug, etc. difficult to drug

Method used

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  • Super-critical anti-solvent preparation for water-soluble nano camptothecin powder

Examples

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Comparison scheme
Effect test

example 1

[0021] Accurately weigh 1g of camptothecin, dissolve it in 100ml DMSO, open the valve 3, start the high-pressure liquid pump 4, pressurize the high-pressure crystallization kettle to 20Mpa, heat up to 55°C, adjust the flow control valve 10, start the high-pressure liquid pump 6, and pass Nozzle 9 sprays the camptothecin DMSO solution into the high-pressure crystallization chamber. Close valve 10 and valve 3, run for 50 minutes to relieve pressure, and obtain camptothecin powder with an average particle size of 600nm.

example 2

[0023] Accurately weigh 1g of camptothecin, dissolve it in 150ml DMF, open the valve 3, start the high-pressure liquid pump 4, pressurize the high-pressure crystallization kettle to 15Mpa, heat up to 46°C, adjust the flow control valve 10, start the high-pressure liquid pump 6, and pass Nozzle 9 sprays the camptothecin DMSO solution into the high-pressure crystallization chamber. Close valve 10 and valve 3, run for 50 minutes to relieve pressure, and obtain camptothecin powder with an average particle size of 800nm.

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Abstract

The invention relates to a supercritical anti-solvent preparation method of water-soluble nanoparticlization camptothecin powder, which is characterized in that, starting CO2 high-pressure pump, injecting CO2 in a high-pressure crystallizing reactor at a flow speed of 5L/h to 20L/h, stabilizing the temperature of the high-pressure crystallizing reactor between 32 DGR C and 75 DGR C, stabilizing the pressure between 7.5MPa and 25MPa, reaching a supercriticality; injecting DMSO or DMF solution with a camptothecin concentration of 1mg/ml to 5mg/ml in the high-pressure crystallizing reactor at a flow speed of 1ml/min to 30ml/min through a nozzle with a pore diameter of 20um to 1000um, dissolving out camptothecin powder with an average grain diameter of 100nm to 800nm, making CO2 circulate in the high-pressure crystallizing reactor for at least half an hour to dry the formed nanoparticlization camptothecin powder; separating DMSO or DMF solution from CO2 in a separation reaction in a pressure of 5MPa to 6.5MPa at temperature of 25 DGR C to 50 DGR C, recycling and reusing DMSO or DMF, making CO2 circulate directly for use. The nanoparticlization camptothecin powder has the advantages of smooth surface, uniform particle size distribution, good water solubility, no solvent remnant, non-pollution manufacturing technique, low cost, high yield, and easy industrialization.

Description

technical field [0001] The invention relates to a method for preparing drug nano-powder, in particular to a method for preparing anti-cancer drug camptothecin nano-powder by supercritical anti-solvent. technical background [0002] Camptothecin (CPT for short) is an alkaloid that was first extracted by American chemists from Camptotheca chinensis in China in 1966. Experiments have shown that camptothecin has obvious curative effects on various malignant tumors such as head and neck tumors, gastric cancer, intestinal cancer, lung cancer, liver cancer, ovarian cancer, bladder cancer and leukemia. [0003] Camptothecin is insoluble in water, so it is not convenient for direct clinical use. And the water-soluble sodium salt of camptothecin, because the ring-opening form of its lactone ring leads to the reduction of anticancer activity and the toxicity is greatly enhanced, it can cause serious adverse reactions such as bone marrow suppression, diarrhea, and hemorrhagic cystitis ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/4745A61P35/00A61J3/02
Inventor 祖元刚赵修华祖柏实杨磊李庆勇朱磊祖纯林张宝友
Owner NORTHEAST FORESTRY UNIVERSITY
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