Enteric long-acting compound amoxicillin powder for veterinary use and preparation method thereof

Abstract

The invention relates to enteric long-acting compound amoxicillin powder for veterinary use and a preparation method thereof. Every 100g of the enteric long-acting compound amoxicillin powder for veterinary use comprises the following components by weight: 8-10g of amoxicillin, 2-3g of potassium clavulanate, 8-10g of probenecid, 20-40g of beta-cyclodextrin, 10-20g of micropowder silica gel, 1-5% of acrylic resin and the balance of glucose. The main drug amoxicillin of the preparation is kept stable in a strong acid environment in the upper portion of the stomach and is not damaged by the strong acid; when the pH of the lower portion of the stomach is close to 6, amoxicillin is released after an enteric material is dissolved; potassium clavulanate can reduce degradation of beta-lactamase generated by sensitive bacteria, and probenecid can prolong discharge of amoxicillin in kidneys, so that the blood concentration is effectively prolonged. According to the product, the bioavailability of amoxicillin is improved greatly, the treatment course of livestock diseases is shortened, the treatment cost of farmers is lowered, and a high quality preventing drug is provided for animal husbandry.

Description

technical field [0001] The invention belongs to the field of veterinary medicine, relates to veterinary enteric-coated long-acting compound amoxicillin powder, and also relates to a preparation method of veterinary enteric-coated long-acting compound amoxicillin powder. Background technique [0002] Amoxicillin is a β-lactam semi-synthetic broad-spectrum antibiotic with strong bactericidal effect and strong ability to penetrate cell walls. After oral administration, the lactam group in the drug molecule is immediately hydrolyzed to form a peptide bond, which is quickly combined with the transpeptidase in the bacteria to inactivate it, cutting off the only way for the bacteria to rely on the transpeptidase to synthesize glycopeptides to build the cell wall, making the bacteria The cells quickly become spherical and rupture and dissolve, and the bacteria eventually swell and die due to the loss of cell walls and continuous water penetration. For most pathogenic G + bacteria ...

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Problems solved by technology

However, there are still some problems in its practical application: 1. The blood elimination half-life (t1 / 2β) of amoxicillin is 1 to 1.3 hours, and about 24% to 33% of the dose is metabolized in the liver after taking the drug, and 45% of the drug is metabolized in 6 hours. ~68% of the dose is excreted from the urine with the original drug; ②Although amoxicillin is relatively stable under acidic conditions, its β-lactam ring is still relatively easy to hydrolyze and open in the environment of about pH 2 in the upper part of the stomach, thus Loss of activity; ③The β-lactamase produced by some sensitive bacteria will degrade amoxicillin, resulting in its inactivity; ④Amoxicillin is relatively stable to water, but potassium clavulanate is sensitive to water and hygroscopic It is highly resistant, and it is easy to degrade after moisture absorption during production and storage. Studies by Xue Jing and others at the China Institute of Food and Drug Control have shown that moisture is more sensitive to the stability of potassium amoxicillin and clavulanate particles. Under high humidity conditions After being left open for 1 day, potassium clavulanate could no longer be detected in some samples

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