Veterinary enrofloxacin taste-masking sustained-release granule and preparation method thereof

A technology of slow-release granules and enrofloxacin, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve problems such as incomplete taste masking of coatings, and achieve improved Oral bioavailability, reduced release, reduced irritation effects

Inactive Publication Date: 2019-03-01
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, coating technology has been widely used in improving the palatability of drugs and preparing targeted drug release delivery systems, but incomplete taste masking by simple coatings is also common in production.

Method used

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  • Veterinary enrofloxacin taste-masking sustained-release granule and preparation method thereof
  • Veterinary enrofloxacin taste-masking sustained-release granule and preparation method thereof
  • Veterinary enrofloxacin taste-masking sustained-release granule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Formula 1 of veterinary enrofloxacin taste-masking sustained-release granules and its cumulative release in vitro

[0059] The formula 1 of enrofloxacin taste-masking sustained-release granules for veterinary use is shown in Table 1, and the enrofloxacin nanosuspension prepared by formula 1 and the enrofloxacin taste-masking sustained-release granules for veterinary cumulative release tests in vitro The results are shown in Table 2.

[0060] Table 1 The formula 1 of veterinary enrofloxacin taste-masking sustained-release granules

[0061]

[0062] Preparation steps of veterinary enrofloxacin taste-masking sustained-release granules:

[0063] (1) Add 6 g of enrofloxacin after heating and dissolving 20 g of stearic acid, and stir to dissolve enrofloxacin in the molten stearic acid to obtain solution 1;

[0064] (2) Preheat 80ml of 5% polyvinyl alcohol solution to 100°C, add it into solution 1 of step (1), and use ultrasonic emulsification (technical conditi...

Embodiment 2

[0071] Example 2 Formula 2 of veterinary enrofloxacin taste-masking sustained-release granules and its cumulative release in vitro

[0072] The formulation 2 of enrofloxacin taste-masking sustained-release granules for veterinary use is shown in Table 3, and the cumulative release in vitro of the enrofloxacin nanosuspension prepared by formula 2 and the enrofloxacin taste-masking sustained-release granules for veterinary use is shown in Table 3. Table 4.

[0073] Table 3 The formula 2 of veterinary enrofloxacin taste-masking sustained-release granules

[0074]

[0075] The preparation steps are as follows:

[0076] (1) Add 7g of enrofloxacin after heating and dissolving 25g glyceryl behenate and 5g nonanoic acid, stir to make enrofloxacin dissolve in the molten oil phase;

[0077] (2) Preheat 80ml of 2.5% Tween-80 and sodium lauryl sulfate solution to 100°C, add it to the above solution (1), and perform ultrasonic emulsification (technical conditions: 6mm probe, ultrasoni...

Embodiment 3

[0084] Example 3 Formula 3 of veterinary enrofloxacin taste-masking sustained-release granules and its cumulative release in vitro

[0085] The design of formulation 3 of enrofloxacin taste-masking sustained-release granules for veterinary use is shown in Table 5. Table 6 shows the in vitro cumulative release of enrofloxacin nanosuspension and veterinary enrofloxacin taste-masked sustained-release granules prepared in formula 3.

[0086] The design of the formula 3 of table 5 veterinary enrofloxacin taste-masking sustained-release granules

[0087]

[0088] The preparation steps are as follows:

[0089] (1) Add 15g of enrofloxacin after heating and dissolving 30g of capric acid, stir to make enrofloxacin dissolve in the molten oil phase;

[0090] Table 6. In vitro release of granules at different pH values ​​in Example 3

[0091]

[0092] (2) Preheat 80m of 3.75% polyvinyl alcohol solution to 100°C, add it to the solution of the above step (1), and perform ultrasonic ...

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Abstract

The invention belongs to the field of preparation of veterinary medicine preparations, and particularly relates to a veterinary enrofloxacin taste-masking sustained-release granule and a preparation method thereof. The granule is prepared through the following step that lipid matrix nanocrystallization, wet granulation and film coating are combined; the granule is prepared by mixing, by mass, 2.5-15.0% of enrofloxacin, 5.0-35.0% of lipid matrix, 1.0-5.0% of a surfactant, 20.0-40.0% of a diluent; 10.0 %-20.0% of a flavoring agent and 5.0%-20.0% of a coating material. The invention provides an optimized formulation and a preparation method. The granule has the advantages that the appearance is white or light yellow, the particle size is 0.2-2 mm, and the loss on drying is less than 2%; the dissolution rate is less than 30% in simulated gastric juice when the pH value is equal to 2, and the dissolution rate in 30 min is less than 60% in the simulated gastric juice when the pH value is equal to 8.

Description

technical field [0001] The invention belongs to the field of preparation of veterinary drug preparations, and in particular relates to a veterinary enrofloxacin taste-masking sustained-release granule and a preparation method thereof. Background technique [0002] Enrofloxacin is a new fluoroquinolone drug for animals. Because of its unique antibacterial mechanism of interfering with bacterial transcription and replication, it has good oral bioavailability to a variety of monogastric animals and is widely distributed in the body, which is beneficial to systemic infection and deep tissue The treatment of infection, long elimination half-life and other advantages are widely used in veterinary clinics for Klebsiella, E. Treatment of infections caused by bacteria such as Staphylococcus aureus. Currently, enrofloxacin dosage forms on the market include enrofloxacin injection, enrofloxacin soluble powder, enrofloxacin suspension and enrofloxacin tablets. Because enrofloxacin has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/496A61K47/38A61K47/32A61K47/12A61K47/14A61P31/04
CPCA61K9/5026A61K9/5042A61K31/496A61K47/12A61K47/14A61P31/04
Inventor 谢书宇袁宗辉周凯翔李超陈冬梅潘源虎陶燕飞
Owner HUAZHONG AGRI UNIV
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