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Method for preparing water-soluble ethopabate and application thereof

A kind of ethopabate, water-soluble technology, applied in the direction of pharmaceutical formulations, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problems of poor bioavailability, low dissolution rate, affecting drug efficacy, etc. Achieve the effect of easy operation, good absorption and simple method

Inactive Publication Date: 2010-07-07
PU LIKE BIO ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After chickens get sick, the feed intake often decreases. It is difficult to reach the effective concentration of the drug due to the decrease of the feed intake when the premix is ​​used. Moreover, for most medium and small farms, there is no drug mixing ability, so that the drug can be mixed in the feed. Can not be mixed evenly, thus affecting the efficacy of the medicine
[0004] The most widely used dosage form of ethopabate is mainly a premix. Due to its poor solubility in water and low dissolution rate, resulting in poor bioavailability, it is difficult for the drug to reach the blood concentration required for treatment.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The preparation of embodiment 1 water-soluble ethopabate:

[0022] 1) Take 160 g of hydroxypropyl-β-cyclodextrin and add 6 times the amount of water, and stir evenly to prepare an aqueous solution of hydroxypropyl-β-cyclodextrin;

[0023] 2) Take 16g of ethopabate, add 0.125g of polyvinylpyrrolidone and 25ml of ethanol to dissolve;

[0024] 3) Slowly add 2) into the hydroxypropyl-β-cyclodextrin aqueous solution while stirring, ultrasonically treat for 60 minutes, concentrate under reduced pressure to a viscous state, refrigerate and stand for 12 hours, then filter, and dry the filter cake at 60°C. Instantly. The measured yield was 91.1%, and the encapsulation efficiency was 94.2%.

Embodiment 2

[0025] The preparation of embodiment 2 water-soluble ethopabate:

[0026] 1) Take 160 g of hydroxypropyl-β-cyclodextrin and add 3 times the amount of water, and stir evenly to prepare an aqueous solution of hydroxypropyl-β-cyclodextrin;

[0027] 2) Dissolve 8 g of ethopabate in 20 ml of ethanol;

[0028] 3) Slowly add 2) to the aqueous solution of hydroxypropyl-β-cyclodextrin while stirring, heat and stir at 60°C for 2 hours, concentrate under reduced pressure to a viscous state, refrigerate and stand for 16 hours, then filter, and the filter cake 60 ℃ drying, that is. The measured yield was 93.5%, and the encapsulation efficiency was 95.0%.

Embodiment 3

[0029] The preparation of embodiment 3 water-soluble ethopabate:

[0030] 1) Take 520 g of β-cyclodextrin polymer and add 3 times the amount of water, and stir evenly to prepare an aqueous solution of β-cyclodextrin polymer;

[0031] 2) Dissolve 8 g of ethopabate in 20 ml of ethanol;

[0032] 3) Slowly add 2) into the β-cyclodextrin polymer aqueous solution while stirring, heat and stir at 60°C for 4 hours, concentrate under reduced pressure to a viscous state, refrigerate and stand for 12 hours, then filter, and filter cake at 60°C Dry and serve. The measured yield was 90.4%, and the encapsulation efficiency was 92.7%.

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Abstract

The invention, belonging to a method for preparing water-soluble ethopabate and an application thereof, relates to an anticoccidial veterinary drug, wherein, ethopabate and Beta-cyclodextrin derivative or water-soluble cyclodextrin polymer by weight ratio of 1:10-65 are prepared into an inclusion compound according to ultrasonic sound or a hot stirring method, and the resulting inclusion compoundcan be directly used for preparing liquid or solid anticoccidial medicines. Due to inclusion technology, the solubility of ethopabate in water is obviously increased.

Description

【Technical field】 [0001] The invention relates to an anticoccidial veterinary drug, in particular to a preparation method and application of water-soluble ethopabate. 【Background technique】 [0002] Chicken coccidiosis is an important and common disease in the poultry industry. It is very harmful to chicken production. According to statistics, the annual cost of medicines for the prevention and treatment of chicken coccidiosis in my country reaches hundreds of millions of yuan, accounting for 100 million yuan of chicken coccidiosis. nearly one-third of all disease prevention and treatment costs. The growth of coccidiosis-prevalent chickens is seriously retarded, and other diseases, such as colibacillosis and mycoplasma disease, are subsequently induced. As early as the 1940s, people discovered that sulfa drugs could be used to prevent and treat coccidiosis, and later found that other drugs such as furans, alkaloids, ionophores and other drugs could be used to prevent and tre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/245A61K47/40A61P33/02A61K31/506A61K31/635A61K31/505
Inventor 张晓会李兴国杜丽丽
Owner PU LIKE BIO ENG
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