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Method for preparing diclazuril microemulsion

A technology of diclazuril and microemulsion, which is applied in the fields of emulsion delivery, anti-infective drugs, and active ingredients of heterocyclic compounds, etc. It can solve the problems of strong toxic and side effects, short duration of drug effect, poor stability of diclazuril solution, etc. problems, to achieve the effect of high drug loading, obvious targeting, and reduced drug dosage

Inactive Publication Date: 2016-01-06
南阳农业职业学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a diclazuril microemulsion for oral use, which can effectively solve the problems of poor stability of diclazuril solution, short duration of drug effect, strong toxic and side effects, etc. The preparation method of submicroemulsion

Method used

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  • Method for preparing diclazuril microemulsion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) Formulation:

[0045] Diclazuril 0.1g, tea oil 4ml, Tween-605ml, propylene glycol 2ml, vitamin E0.3ml, methyl p-hydroxybenzoate 0.1g, sodium carboxymethyl cellulose 0.2g, dimethyl sulfoxide 3ml, ethanolamine 0.5 ml, ethanol 2ml, and purified water to 100ml.

[0046] (2) Preparation process:

[0047] ①Take dimethyl sulfoxide, heat to 50°C, add diclazuril, stir evenly, add ethanolamine, stir to dissolve completely, set aside;

[0048] ②Take vitamin E and Tween-60, add them to camellia oil respectively, stir evenly, make oil phase, set aside;

[0049] ③Add sodium carboxymethylcellulose into purified water, control the water temperature at 80-90°C, stir to make it dissolve evenly, then add propylene glycol, stir evenly, and make a water phase for later use;

[0050] ④ First add the liquid described in ② into the colloid mill, grind for 5 minutes at a speed of 5000 rpm, then put the liquid described in ③ into it, mix and grind for 5 minutes, then add the liquid descri...

Embodiment 2

[0054] (1) Formulation:

[0055] Diclazuril 0.5g, soybean oil 6ml, Tween-808ml, glycerol 5ml, vitamin E0.4ml, ethyl p-hydroxybenzoate 0.1g, sodium carboxymethylcellulose 0.4g, dimethyl sulfoxide 4ml, Add 0.6ml of triethanolamine, 2ml of ethanol, and purified water to 100ml.

[0056] (2) Preparation process:

[0057] ①Take dimethyl sulfoxide, heat to 50°C, add diclazuril, stir evenly, add triethanolamine, stir to dissolve completely, set aside;

[0058] ②Take vitamin E and Tween-80, add them to soybean oil respectively, stir evenly, make oil phase, set aside;

[0059] ③Add sodium carboxymethyl cellulose to purified water, control the water temperature at 80-90°C, stir to dissolve evenly, then add glycerin, stir evenly, and make a water phase for later use;

[0060] ④ First add the liquid described in ② into the colloid mill, grind for 5 minutes at a speed of 5000 rpm, then put the liquid described in ③ into it, mix and grind for 5 minutes, then add the liquid described in ① ...

Embodiment 3

[0064] (1) Formulation:

[0065] Diclazuril 0.6g, cottonseed oil 6ml, Tween-608ml, glycerol 5ml, vitamin E0.4ml, methyl p-hydroxybenzoate 0.2g, sodium carboxymethylcellulose 0.4g, dimethyl sulfoxide 4ml, Add 0.6ml of ethanolamine, 2ml of ethanol, and purified water to 100ml.

[0066] (2) Preparation process:

[0067] ①Take dimethyl sulfoxide, heat to 50°C, add diclazuril, stir evenly, add ethanolamine, stir to dissolve completely, set aside;

[0068] ②Take vitamin E and Tween-60, add them to cottonseed oil respectively, stir evenly, make oil phase, and set aside;

[0069] ③Add sodium carboxymethyl cellulose to purified water, control the water temperature at 80-90°C, stir to dissolve evenly, then add glycerin, stir evenly, and make a water phase for later use;

[0070] ④ First add the liquid described in ② into the colloid mill, grind for 5 minutes at a speed of 5000 rpm, then put the liquid described in ③ into it, mix and grind for 5 minutes, then add the liquid described ...

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Abstract

The invention discloses a method for preparing a diclazuril microemulsion. The diclazuril microemulsion is characterized by being prepared from the following components in every milliliter: 1-20mg / mL of diclazuril, 50-200mg / mL of plant oil for injection, 8-24mg / mL of an emulsifying agent, 1-20mg / mL of a co-emulsifying agent, 0.1-3mg / mL of a stabilizing agent, 0.8mg / mL of an antioxidant vitamin E and 22.5mg / mL of an isoosmotic adjusting agent glycerinum. The diclazuril microemulsion is a veterinary preparation for animals, and has the advantages of simple preparation method, long drug efficacy duration period, small toxic or side effect and wide application prospect. According to the method, the existing novel equipment and novel process are used, and the existing traditional production process is improved, so that the production process is efficient and quick, and is convenient to popularize.

Description

technical field [0001] The invention relates to the field of veterinary drug preparations, in particular to a preparation method of diclazuria microemulsion. Background technique [0002] Diclazuril (Diclazuril) is a triazine phenylacetonitrile compound of the genus Diclazuril. It is a new type, high-efficiency, and low-toxicity anticoccidial drug, and is widely used in chicken coccidiosis. [0003] The mechanism of action of diclazuril against coccidia is still unclear. The peak period of the main action on coccidia varies with different species of coccidia, such as the main action point on Eimeria tenella is in the sexual cycle of the second generation schizont coccidia. But the giant, Eimeria brucei schizont invalid. The point of action on Eimeria maxima is at the zygote stage of Eimeria brucei; it is highly effective on the microgametophyte stage of Eimeria brucei. Diclozolid also inhibited the formation of sporulated oocysts. [0004] At present, commercially availa...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/53A61P33/02
Inventor 王国强布登付张天伟李伟李泳袁录贾荣玲杜军王小建刘建成王世江郝光辉杨灵杰
Owner 南阳农业职业学院