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Artesunate nanoemulsion drug composition and preparation method thereof

A technology of artesunate and nanoemulsion, which is applied in the direction of drug combination, pharmaceutical formula, anti-infective drugs, etc. It can solve the problems of poor stability of sodium salt and poor water solubility of artesunate, and achieve long shelf life and clear appearance , good anti-corrosion and anti-mildew effect

Inactive Publication Date: 2010-01-13
LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the present invention, artesunate is made into nanoemulsion, which greatly enhances the effectiveness of artesunate, and also solves the disadvantages of artesunate, such as poor water solubility and poor stability of sodium salt, etc.

Method used

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  • Artesunate nanoemulsion drug composition and preparation method thereof
  • Artesunate nanoemulsion drug composition and preparation method thereof
  • Artesunate nanoemulsion drug composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] 1) Weigh 6 g of ethyl oleate, 22 g of Tween-80, 11.5 g of n-butanol, 3 g of artesunate, and 57.5 g of ultrapure water;

[0054] 2) At room temperature, place the ethyl oleate, Tween-80, n-butanol, and artesunate of the above weight on a constant temperature magnetic stirrer at 200-400rpm and stir until the drug is dissolved in the system middle.

[0055] 3) Slowly add ultrapure water to the mixture, and stir while adding; at the beginning, the viscosity of the system is small, and as the water volume increases to 16ml, the system gradually becomes viscous, and at this time the system may appear liquid crystal phase or W / O (Water-in-oil type) nano-emulsion, continue to drop and stir continuously, when the water volume reaches 32ml, the system will suddenly become clear and thin, and the O / W type nano-emulsion will be produced at this time, add ultra-pure water to 57.5ml, the fluidity of the system is good, and it is prepared into a clear and transparent O / W nanoemulsion...

Embodiment 2

[0057] 1) Weigh 4.6g of ethyl oleate, 13.2g of Tween-80, 8.7g of n-butanol, 2g of artesunate and 71.5g of ultrapure water for each drug component.

[0058] 2) At room temperature, place the ethyl oleate, Tween-80, n-butanol, ultrapure water, and artesunate of the above-mentioned weight on a constant temperature magnetic stirrer at 200 to 400rpm and stir until evenly mixed. The drug is dissolved in the above system.

[0059] 3) Slowly add ultra-pure water to the mixture, and stir while adding; at the beginning, the viscosity of the system is small, and as the amount of water increases, the system gradually becomes viscous. At this time, the system may appear liquid crystal phase or W / O (oil-in-oil Water-type) nano-emulsion, continue to drop and stir continuously, when the water volume reaches 50ml, the system will suddenly become clear and thin, at this time, the O / W-type nano-emulsion is produced, add ultra-pure water to 71.5ml, The fluidity of the system is good, and it is p...

Embodiment 3

[0061] 1) Weigh 6 g of ethyl oleate, 24 g of Tween-80, 11.5 g of n-butanol, 53.5 g of ultrapure water, and 5 g of artesunate for use as spare parts.

[0062] 2) At room temperature, place the ethyl oleate, Tween-80, n-butanol, ultrapure water, and artesunate of the above-mentioned weight on a constant temperature magnetic stirrer at 200 to 400rpm and stir until evenly mixed. The drug is dissolved in the above system.

[0063] 3) Slowly add ultrapure water to the mixture, and stir while adding; at the beginning, the viscosity of the system is small, and as the amount of water increases, the system gradually becomes viscous. At this time, the system may appear liquid crystal phase or W / O (oil Water-containing type) nanoemulsion, continue to drop and stir continuously, when the water volume reaches 28ml, the system will suddenly become clear and thin, and the O / W type nanoemulsion will be produced at this time, add ultra-pure water to 53.5ml , the fluidity of the system is good,...

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Abstract

The invention discloses an Artesunate nanoemulsion drug that is an O / W (oil-in-water type) nanoemulsion system consisting of ethyl oleate, Tween-80, normal butanol, ultrapure water and Artesunate. The nanoemulsion drug effectively overcomes the first-pass effect of traditional tablets in liver, causes no sense of pain in injection and greatly improves the insecticidal and helminthic effect of original Artesunate. Meanwhile, the nanoemulsion system has high drug-loading rate, is stable when stored, has certain slow release function compared with merchant Artesunate injection, and further is convenient for administration, thus greatly improving the bioavailability. Besides, shown by acute toxicity tests and clinical drug effect tests on mice, the nanoemulsion has no obvious toxic or side effect and is a safe, reliable and high-efficiency nano level antiparasitic drug.

Description

technical field [0001] The invention belongs to the field of veterinary medicines, and relates to an antiparasitic medicine for efficiently killing malaria parasites and theileria theilera, in particular to an artesunate nanoemulsion medicine and a preparation method thereof. Background technique [0002] Artesunate (Artesunate), the chemical name is dihydroartemisinin-1,2-α-succinic acid monoester, which is a derivative of antimalarial artemisinin with a sesquiterpene structure, in the form of colorless crystals or White crystalline powder, odorless, almost tasteless. Slightly soluble in water, easily soluble in ethanol, acetone, chloroform. As an effective antimalarial drug, artesunate is effective against vivax malaria, falciparum malaria, and cerebral malaria. In veterinary medicine, it is mainly used to treat cattle and sheep theileriasis and double-bud pyrozoosis. The traditional tablet of artesunate cannot overcome the first-pass effect of the liver, and the commer...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/557A61P33/06A61P33/14A61K47/26
Inventor 张继瑜李剑勇周绪正吴培星胡宏伟牛建荣魏小娟李金善
Owner LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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