Veterinary compound diminazene aceturate and artemisinin preparation and preparation technology thereof

A compound triazamidine and preparation process technology, which can be applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc. Toxic and other problems, to achieve the effects of fast absorption, high bioavailability, and reduced toxic and side effects

Active Publication Date: 2012-09-05
HUBEI WUDANG ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The process route of the triazine raw material drug with industrial production value must produce p-nitrobenzonitrile, which is highly toxic to humans and seriously pollutes th

Method used

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  • Veterinary compound diminazene aceturate and artemisinin preparation and preparation technology thereof
  • Veterinary compound diminazene aceturate and artemisinin preparation and preparation technology thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Take the leaves of Artemisia annua that produce artemisinin content of more than 0.2% in the Yunxi area of ​​Hubei Province, put them in a drying box and dry them at 40°C, and TLC The law distinguishes its authenticity. Crush and pass through a 60-mesh-0.25mm sieve. According to the literature (Li Chunli et al., [J], Journal of Chongqing Medical University, 2007, 32 (4), 413), the content of artemisinin was determined by ultraviolet spectrophotometry, and the content of artemisinin was required to be more than 0.2%.

[0046] Weigh about 10Kg of powder into the extraction tank group, such as figure 2 shown, press figure 1 Process and process parameters countercurrent extraction (extraction tank adopts extraction temperature 50°C; extraction time 60min; stirring speed 200-400 rpm; extraction solvent is 50°C petroleum ether; the solid-liquid ratio of the leaves and flower buds of Artemisia annua to the extraction solvent is 1 :9). The solvent rich in active ingredient...

Embodiment 2

[0051] Example 2 follows the same operating method and process conditions as in Example 1, except that artemisinin is replaced by artemisinin extract.

Embodiment 3

[0052] Example 3 is the same operating method and process conditions as in Example 1, except that it is composed of the following composition and mass percentage: triazamidine 15%; artemisinin or artemisinin extract 55%; β-cyclodextrin 30% (both are mass percentages), prepared, mixed, potted and sterilized to make compound triazamidine and artemisinin injection powders with specifications of 0.5-4g / bottle.

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PUM

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Abstract

The invention relates to a veterinary compound diminazene aceturate and artemisinin preparation, which is a powder injection comprising the following medicinal components in percentage by mass: 10 to 85 percent of diminazene aceturate, 5 to 60 percent of artemisinin or artemisinin extract, and 2 to 30 percent of beta-cyclodextrin. The preparation is prepared by the following steps of: 1) refining the diminazene aceturate; 2) preparing a water-soluble inclusion complex of the artemisinin or the artemisinin extract; and 3) proportioning, mixing, sterilizing and filling the preparation. The veterinary compound diminazene aceturate and artemisinin preparation has the advantages that the preparation is quick in absorption and high in bioavailability in subcutaneous or intramuscular injection; by combined utilization of the artemisinin and the diminazene aceturate which serve as active Chinese medicinal ingredients, a synergistic effect of Chinese medicaments can be achieved, and the toxic or side effect of the diminazene aceturate is reduced; the artemisinin, particularly the artemisinin extract is cheaper than dihydroartemisinin, artemether and artesunate; and the preparation is suitable to be produced in injection workshops of animal pharmaceutical factories with good manufacturing practice (GMP) conditions, and does not require to update the investment.

Description

technical field [0001] The invention relates to a veterinary compound triazine and artemisinin preparation, which belongs to the field of pharmaceutical preparations. Background technique [0002] Triazamidine, also known as Bernier and Xuechongjing, realized industrial scale production in my country in the 1970s. Triazamidine and its injections have been included in the Veterinary Pharmacopoeia of the People's Republic of China. For trypanosomiasis and equine disease caused by trypanosomes. The mechanism of action of this product is to selectively block the DNA synthesis and replication of trypanosome kinetosomes, and irreversibly combine with the nucleus, so that the kinetosomes of trypanosomes disappear and cannot divide and reproduce, so as to achieve the purpose of treatment. However, its toxicity is high, and its safety range is small, and the application of therapeutic doses may also cause animal muscle tremors, restlessness in standing and lying, frequent urination...

Claims

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Application Information

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IPC IPC(8): A61K31/655A61K31/366A61K9/08A61K47/48A61P33/06A61P33/00A61P31/00
Inventor 陈国明
Owner HUBEI WUDANG ANIMAL PHARMA
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