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High-efficiency water-solubility toltrazuril solution and preparation method thereof

A toltrazuril and water-soluble technology, applied in the field of water-soluble toltrazuril solutions and preparation methods, can solve the problem of accelerating the elimination speed of the triazinone drug market, the inability of sick animals to drink drugs, and the development of drug resistance in sick animals and other problems, to achieve the effect of reducing adverse pharmacological effects, improving bioavailability, and solving the problem of dilution and precipitation

Inactive Publication Date: 2010-07-07
QINGDAO ZHONGREN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, although there are similar products on the market in China, most of their production processes are dissolved in pure organic solvents, such as DMF, etc., the production cost is high, and the drug is very irritating and has obvious adverse pharmacological effects.
[0009] At present, similar products on the market are commonly diluted and crystallized during clinical application, the drug is dispersed unevenly, and the drug sedimentation speed is fast, so that sick animals cannot drink a sufficient amount of the drug, and the bioavailability is low.
If this product is used for a long time, the sick animals will quickly develop drug resistance, and toltrazuril is also prone to cross-resistance with drugs such as diclazuril, which in disguise accelerates the market elimination of triazone drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] A kind of component weight ratio of efficient water-soluble toltrazuril solution and preparation method are as follows

[0052] Toltrazuril 2.5%

[0053] Beta-Cyclodextrin 3%

[0054] Sodium Lauryl Sulfate 1%

[0055] Tween 80 10%

[0056] Span 80 2%

[0057] Isopropyl myristate 3%

[0058] Alpha-Pyrrolidone 40%

[0059] Glycerin Methylal 10%

[0060] Triethanolamine 1%

[0061] Carving white powder 1%

[0062] Purified water balance

[0063] (1) Take 2.5% of Toltrazuril, 3% of clathrate agent β-cyclodextrin, and 1% of antistatic agent sodium lauryl sulfate, mix evenly, put it in a planetary ball mill and grind for 1 hour, and the obtained powder is passed through an 80-mesh sieve , make material A, standby;

[0064] (2) Take 40% of α-pyrrolidone, 10% of glycerol methylal, 2% of Span 80, and 1% of triethanolamine, mix evenly, add 1% of anti-oxidant carving white powder, heat to 60°C in water bath, add material A, stir to dissolve Mixture B is obtained;

[0065...

Embodiment 2

[0068] A kind of component weight ratio of efficient water-soluble toltrazuril solution and preparation method are as follows

[0069] Toltrazuril 2%

[0070] Beta-Cyclodextrin 3%

[0071] Sodium Lauryl Sulfate 1%

[0072] Tween 80 5%

[0073] Span 80 2%

[0074] Isopropyl myristate 2%

[0075] Alpha-Pyrrolidone 30%

[0076] Glycerin Methylal 10%

[0077] Triethanolamine 1%

[0078] Carving white powder 1%

[0079] Purified water balance

[0080] (1) Take 2% of Toltrazuril, 3% of inclusion agent β-cyclodextrin, and 1% of antistatic agent sodium lauryl sulfate, mix evenly, put it in a planetary ball mill and grind for 1 hour, and the obtained powder is passed through an 80-mesh sieve , make material A, standby;

[0081] (2) Take 30% of α-pyrrolidone, 10% of glycerol methylal, 2% of Span 80, and 1% of triethanolamine and mix evenly, add 1% of anti-oxidant carving white powder, heat to 60°C in water bath, add material A, stir to dissolve Mixture B is obtained;

[0082...

Embodiment 3

[0085] A kind of component weight ratio of efficient water-soluble toltrazuril solution and preparation method are as follows

[0086] Toltrazuril 3%

[0087] Beta-Cyclodextrin 4%

[0088] Sodium Lauryl Sulfate 1%

[0089] Tween 80 10%

[0090] Span 80 2%

[0091] Isopropyl myristate 3%

[0092] Alpha-Pyrrolidone 45%

[0093] Glycerin Methylal 10%

[0094] Triethanolamine 2%

[0095] Carving white powder 1%

[0096] Purified water balance

[0097] (1) Take 3% of Toltrazuril, 4% of inclusion agent β-cyclodextrin, and 1% of antistatic agent sodium lauryl sulfate, mix evenly, put it in a planetary ball mill and grind for 1 hour, and the obtained powder is passed through an 80-mesh sieve , make material A, standby;

[0098] (2) Take 45% of α-pyrrolidone, 10% of glycerol methylal, 2% of Span 80, and 2% of triethanolamine, mix evenly, add 1% of anti-oxidant carving white powder, heat to 60°C in water bath, add material A, stir to dissolve Mixture B is obtained;

[0099] ...

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Abstract

The invention relates to a high-efficiency water-solubility toltrazuril solution which comprises the following components in percentage by weight: 2-6 percent of toltrazuril, 2-10 percent of inclusion agent, 1 percent of antistatic agent, 7-17 percent of composite emulsifying agent, 1-3 percent of pH regulator, 1 percent of antioxidant, 35-70 percent of composite organic solvent and the balance of purified water. In the invention, an advanced microemulsion preparation process is adopted, and the water insoluble toltrazuril is prepared into a water-insoluble microemulsion solution which can be mixed with water in any proportion, therefore, the dilution and precipitation problems are effectively solved, the bioavailability of the product is improved, and the medicine consumption is reduced; and compared with the prior art, the invention reduces the consumption of the organic solvent and the harmful pharmacological action, saves the cost and improves the security.

Description

technical field [0001] The invention relates to a medicine and a preparation method thereof, in particular to a water-soluble toltrazuril solution prepared by using medicine inclusion technology and microemulsion preparation technology and a preparation method thereof. Background technique [0002] Chicken coccidiosis is an acute epidemic parasitic disease caused by one or more unicellular parasites of the genus Eimer. my country has listed it as a second-class animal disease. Among various chicken diseases, the incidence of coccidiosis is the highest, accounting for about 1 / 6-1 / 5, especially the chicks within 3 months of age are the most susceptible to infection, and the mortality rate can reach 70%, and the recovered chicks are often several It is not easy to recover health within a month. Most adult chickens are also carriers. Other poultry such as ducks, turkeys, pigeons, crane quails, etc. can be infected, which seriously affects the development of my country's breed...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/48A61K31/53A61K47/40A61P33/02A61K47/61
Inventor 姜宪华张述智姜继光
Owner QINGDAO ZHONGREN PHARMA
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