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Preparation method of ultrafine artesunate sterile powder

The technology of artesunate and fine artesunate is applied in the field of preparation of ultra-fine artesunate sterile powder, which can solve the problems of wide product particle size distribution, narrow particle size distribution and high equipment cost, and achieves easy dissolving speed, The effect of simple and easy control and low production cost

Inactive Publication Date: 2013-06-26
GUILIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although jet milling and ball milling are commonly used methods to reduce the particle size of drugs, they generally have the disadvantages of high energy consumption, low efficiency, wide product particle size distribution, and easy structural damage and degradation of thermally unstable drugs. Will cause problems such as dust pollution and static electricity safety
Although spray drying and supercritical fluid technology can produce micronized drugs with narrow particle size distribution, the cost of equipment is high
However, there is no report on the micronization of artesunate by anti-solvent crystallization method

Method used

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  • Preparation method of ultrafine artesunate sterile powder
  • Preparation method of ultrafine artesunate sterile powder

Examples

Experimental program
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Effect test

Embodiment 1

[0030] 1) Get 2g of artesunate raw drug, dissolve it in ethanol at 20°C to make a concentration of 0.05g / ml (5% of the concentration of artesunate sterile powder in ethanol under this temperature condition) About 40ml of the bulk drug solution is placed in the bulk drug solution storage tank 1, and 400ml of deionized water is placed in the anti-solvent storage tank 2;

[0031] 2) Through the bulk drug solution advection pump 3 and the anti-solvent advection pump 4, the bulk drug solution and water are pumped into the microreactor 5 substantially simultaneously through the solution inlet and the anti-solvent inlet respectively for recrystallization, and the slurry obtained by the recrystallization is produced by the microreaction The output pipeline of the device 5 is collected to the slurry storage tank 6; the flow rate of the bulk drug solution is 1ml / min, the flow rate of the deionized water is 10ml / min, and the recrystallization temperature is 10°C;

[0032] 3) Filter the s...

Embodiment 2

[0036] 1) Get 10.0g of artesunate raw drug, dissolve it in ethanol at 20°C to make a concentration of 0.2g / ml (that is, 20% of the concentration of artesunate sterile powder in ethanol under this temperature condition) About 50ml of bulk drug solution is placed in bulk drug solution storage tank 1, and 1250ml deionized water is placed in antisolvent storage tank 2;

[0037] 2) Through the bulk drug solution advection pump 3 and the anti-solvent advection pump 4, the bulk drug solution and water are pumped into the microreactor 5 substantially simultaneously through the solution inlet and the anti-solvent inlet respectively for recrystallization, and the slurry obtained by the recrystallization is produced by the microreaction The output pipeline of the device 5 is collected to the slurry storage tank 6; the flow rate of the bulk drug solution is 4ml / min, the flow rate of the deionized water is 20ml / min, and the recrystallization temperature is 15°C;

[0038] 3) The slurry obta...

Embodiment 3

[0041]1) Take 8.0kg of artesunate raw drug, dissolve it in ethanol at 20°C to make a concentration of 0.2kg / L (that is, 20% of the saturated concentration of artesunate sterile powder in ethanol under this temperature condition). %) of the crude drug solution 40L, placed in the crude drug solution storage tank 1, get 1200L deionized water and placed in the anti-solvent storage tank 2;

[0042] 2) Through the bulk drug solution advection pump 3 and the anti-solvent advection pump 4, the bulk drug solution and water are pumped into the microreactor 5 substantially simultaneously through the solution inlet and the anti-solvent inlet respectively for recrystallization, and the slurry obtained by the recrystallization is produced by the microreaction The output pipeline of the device 5 is collected to the slurry storage tank 6; the flow rate of the bulk drug solution is 4ml / min, the flow rate of the deionized water is 60ml / min, and the recrystallization temperature is 15°C;

[0043...

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Abstract

The invention discloses a preparation method of an ultrafine artesunate sterile powder, which comprises the following steps: 1) preparing a 1-20% (w / v) active pharmaceutical ingredient solution; 2) simultaneously adding the active pharmaceutical ingredient solution and a counter solvent into a microreactor by a constant-flux pump respectively through a solution inlet and a counter solvent inlet, and recrystallizing at 10-15 DEG C, wherein the volume ratio of the active pharmaceutical ingredient solution to the counter solvent is 1:(10-30), the flow rates of the active pharmaceutical ingredient solution and counter solvent entering the microreactor are respectively 1-80 ml / minute, and the flow rate ratio is 1:(5-25); and 3) filtering the recrystallized slurry, washing and drying to obtain the artesunate sterile powder with the particle size of 0.3-30 mu m prepared by a distribution method. The artesunate sterile powder has the advantages of narrow particle size distribution, high water solubility and high solution rate.

Description

technical field [0001] The invention relates to a preparation method of ultrafine artesunate aseptic powder, which belongs to the technical field of chemical industry and pharmacy. Background technique [0002] Artemisinin-like drugs are artemisinin monomers extracted from Artemisia annua, which are currently effective drugs in the antimalarial market, especially artesunate, one of the artemisinin derivatives obtained by structurally modifying the parent artemisinin, Its curative effect can be increased by about 5 times compared with artemisinin, but artesunate has low solubility in water and is an insoluble drug. Currently, 5% bicarbonate is used in the use of artesunate freeze-dried powder injection. Sodium solution was added to artesunate sterile powder, shaken to dissolve and then injected intravenously. [0003] In injection powder drugs, there are certain requirements for the particles of the drug: (1) particle size: the smaller the particle size, the larger the speci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/357
Inventor 胡伟松潘梅郑清四
Owner GUILIN PHARMA
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