Ivermectin mixed micelle injection and preparation method thereof

A technology of ivermectin and mixed micelles, which is applied in the directions of drug combinations, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve problems such as adverse reactions in animals and affect the effect of ivermectin, and achieve a small dispersion index. , uniform particle size, reducing the effect of toxic and side reactions

Active Publication Date: 2011-06-29
四川吉星动物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although ivermectin is also a poorly soluble drug, due to the high requirements for ivermectin injection preparations in the prior art, the non-natural solubilizing ingredients in the preparation may cause adverse reactions in animals. In theory, bile salts The phospholipids / bile salts and other substances contained in the phospholipid / phospholipid mixed micelle system can affect the effect of ivermectin, and even cause severe local reactions in cattle, sheep, pigs, reindeer, especially dogs and horses. Therefore, this Those skilled in the art have never thought of using mixed micelles to prepare ivermectin injection preparations, and there is no record in the prior art

Method used

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  • Ivermectin mixed micelle injection and preparation method thereof
  • Ivermectin mixed micelle injection and preparation method thereof
  • Ivermectin mixed micelle injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Weigh 50mg of soybean lecithin, 70mg of sodium cholate and 25mg of ivermectin, place them in a 50ml round-bottomed flask, add 10ml of absolute ethanol, stir to dissolve, remove the organic solvent by rotary evaporation under reduced pressure, and the temperature of the water bath is 40°C. Form a layer of transparent film, and then disperse with 2.5ml of 0.9% NaCl aqueous solution to obtain a drug-containing mixed micelles solution, then filter and sterilize with a 0.22 μm microporous membrane, potting, and obtain ivermectin mixed micelles for injection liquid. Recording its ivermectin content is 9.6mg / ml.

Embodiment 2

[0045] Weigh 50mg of egg yolk lecithin, 50mg of sodium deoxycholate and 20mg of ivermectin into a 50ml round bottom flask, add 10ml of methanol-chloroform (5:5) solution, stir to dissolve, and remove the organic solvent by rotary evaporation under reduced pressure. The temperature of the water bath is 40°C to form a layer of transparent film, and then disperse with 2.5ml of water for injection to obtain a drug-containing mixed micelles solution, then filter and sterilize it with a 0.22 μm microporous membrane, and pot it to obtain ivermectin Mixed micellar injection. It is measured that its ivermectin content is 7.3mg / ml.

Embodiment 3

[0047] Weigh 50mg of polyene phosphatidylcholine, 40mg of sodium glycinate cholate and 25mg of ivermectin into a 50ml round bottom flask, add 10ml of ethanol-ethyl acetate (8:2) solution, stir to dissolve, spin down under reduced pressure Evaporate to remove the organic solvent, the temperature of the water bath is 50°C, form a layer of transparent film, then disperse with 2.5ml of pH 7.4 phosphate buffer solution to obtain the drug-containing mixed micelles solution, then filter and sterilize with a 0.22 μm microporous membrane, pour Seal, promptly obtain ivermectin mixed micelle injection. It is measured that its ivermectin content is 9.6mg / ml.

[0048]

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Abstract

The invention provides Ivermectin mixed micelle injection for reducing poisoning incidence and local reaction probability during the killing of livestock parasites and a preparation method thereof. The micelle injection is prepared by taking Ivermectin as active ingredients and adopting a cholate/phosphatide mixed micelle system, so the problem that the Ivermectin is difficult to dissolve in water is solved effectively, the medicine-carrying dose of the micelle injection is improved greatly. The mixed micelle injection prepared by the method has a simple preparation process, and can reduce the probability of toxic and side reactions during the killing of the livestock parasites.

Description

technical field [0001] The invention relates to an injection containing ivermectin, in particular, the invention relates to a mixed micelle injection containing ivermectin, which belongs to the field of pharmaceutical preparations. Background technique [0002] Ivermectin is a semi-synthetic macrolide multicomponent antibiotic produced by the fermentation of Streptomyces avermitilis, which is almost insoluble in water. Ivermectin is a new type of broad-spectrum, high-efficiency, and low-toxicity antibiotic antiparasitic drug, which has a good killing effect on internal and external parasites, especially nematodes and arthropods. The insecticidal mechanism is that the drug binds to a specific high-affinity site on the target insect cell, which affects the permeability of the cell membrane to Clˉ, and then causes nematode nerve cells and arthropod muscle cells to inhibit the neurotransmitter γ- The release of aminobutyric acid (GABA) is increased, and the Clˉ channel controll...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/7048A61K47/28A61P33/14
Inventor 龚照墉刘振谧
Owner 四川吉星动物药业有限公司
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