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Diclazuril liposome and preparation method thereof

A technology of diclazuril and zuril fat, which is applied in the direction of liposome delivery, freeze-drying delivery, anti-infective drugs, etc., can solve the problems of insignificant effect, difficult to mix, low solubility, etc., and reduce the amount of clinical use , good stability, guarantee the effect of safe conversion

Inactive Publication Date: 2015-03-11
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is that at present, diclazuril mainly includes premixes, suspension powders, etc. on the market, but the solubility of these products is extremely low, and the drug will settle, resulting in insufficient drug dosage in the body. , the effect is not significant, the bioavailability is low, and the cost is wasted; if the mixture is used, the clinical dosage is low, and it is not easy to mix, which affects the effect of preventing and treating coccidia. In order to solve the above problems, a diclazuril liposome and its preparation are provided. method

Method used

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  • Diclazuril liposome and preparation method thereof
  • Diclazuril liposome and preparation method thereof
  • Diclazuril liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A liposome of diclazuril, made of the following raw materials in parts by weight: 3-4 parts of diclazuril, 10-20 parts of α-pyrrolidone, 30-50 parts of soybean lecithin, 1-10 parts of glycerin formal 10-20 servings of cholesterol.

[0023] Specific steps are as follows:

[0024] 1) Weigh 3-4 parts of diclazuril raw powder, dissolve it in the mixture of propylene glycol and ethanol, then add PBS buffer solution to fully dissolve it, and make a water phase with a concentration of 3mg / mL for later use ;

[0025] 2) Weigh α-pyrrolidone, soybean lecithin, glycerol formal, and cholesterol in proportion, and use an ultrasonic breaker at normal temperature for 2-5s with an interval of 2-5s to fully dissolve them to obtain the oil phase;

[0026] 3) Evaporate the oil phase under reduced pressure to form a blank phospholipid film, wash and hydrate the blank phospholipid film with ammonium sulfate solution to obtain blank liposomes, filter through a filter membrane, and set asid...

Embodiment 2

[0035] A diclazuril liposome is prepared from the following raw materials in parts by weight: 30 g of diclazuril, 100 g of α-pyrrolidone, 300 g of soybean lecithin, 10 g of glycerin formal, and 100 g of cholesterol.

[0036] Specific steps are as follows:

[0037] 1) Weigh 30g of diclazuril raw powder, dissolve it in a mixture of propylene glycol and ethanol, the volume ratio of propylene glycol and ethanol is 2:1, and then add PBS buffer solution with a pH value of 6.8-7.2 to make it Fully dissolve to make an aqueous phase with a concentration of 3mg / mL for later use;

[0038] 2) Weigh α-pyrrolidone, soybean lecithin, glycerol formal, and cholesterol in proportion, and act with an ultrasonic crusher at normal temperature for a short time, the action time is 2s, and the interval time is 2s, so that they are fully dissolved and the oil phase is obtained;

[0039] 3) Evaporate the oil phase under reduced pressure to form a blank phospholipid film, wash the blank phospholipid fi...

Embodiment 3

[0043] A diclazuril liposome is prepared from the following raw materials in parts by weight: 32 g of diclazuril, 120 g of α-pyrrolidone, 340 g of soybean lecithin, 30 g of glycerin formal, and 120 g of cholesterol.

[0044] Specific steps are as follows:

[0045] 1) Weigh 32g of diclazuril raw powder, dissolve it in a mixture of propylene glycol and ethanol, the volume ratio of propylene glycol and ethanol is 1:1, and then add PBS buffer solution with a pH value of 6.8-7.2 to make it Fully dissolve to make an aqueous phase with a concentration of 3mg / mL for later use;

[0046] 2) Weigh α-pyrrolidone, soybean lecithin, glycerol formal, and cholesterol in proportion, and act with an ultrasonic breaker at normal temperature for a short time, the action time is 3s, and the interval time is 3s, so that they are fully dissolved to obtain the oil phase;

[0047] 3) Evaporate the oil phase under reduced pressure to make a blank phospholipid film, wash the blank phospholipid film wit...

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Abstract

The invention discloses a diclazuril liposome which is prepared by the following raw materials in parts by weight: 3-4 parts of diclazuril, 10-20 parts of alpha-pyrrolidone, 30-50 parts of soybean lecithin, 1-10 parts of glycerolformal and 10-20 parts of cholesterol. Compared with the prior art, the diclazuril liposome disclosed by the invention has good stability, solubility and sustained-release property and solves the problem of use methods of the diclazuril; the drug property of the diclazuril can be effectively utilized, and the clinical usage amount can be reduced, so that the safe conversion of the drug in a human body is ensured.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and in particular relates to a diclazuril liposome and a preparation method thereof. Background technique [0002] Diclazuril is a chicken coccidiosis control drug. There are mainly premixes and suspension powders on the market. The solubility of these products is extremely low, and the drug will settle, resulting in insufficient drug dosage in the body and poor efficacy. Not significant, low bioavailability, waste of cost; if used as a mixture, the clinical dosage is low, not easy to mix, affecting the effect of coccidial control. [0003] Diclazuril belongs to the triazine benzyl nitrile compound. It is a new type, high-efficiency, and low-toxicity anticoccidiosis drug, which is widely used in chicken coccidiosis. etc. have an excellent killing effect, and the antibiotic indices against the above five coccidia are 200, 200, 197, 193, and 183, respectively. In addition to effective...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K31/53A61P33/02
Inventor 李建正徐进郭俊清
Owner ZHENGZHOU HOUYI PHARMA
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