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Compound doxycycline-hydrochloride florfenicol sustained-release microsphere suspension injection for veterinary use

A technology of doxycycline hydrochloride and suspension injection, which is applied in the directions of tetracycline active ingredients, liquid delivery, and pharmaceutical formulations, which can solve the problems of liver and kidney toxicity, strong irritation, and side effects, and achieve improved sustained release Performance, increased half-life, improved stability effects

Active Publication Date: 2016-02-03
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These organic solvents are irritating to the injection site and have varying degrees of toxic and side effects on the body.
In particular, dimethylformamide and dimethylacetamide are irritating to the eyes, skin and respiratory tract, and are highly irritating. After invading the body, they may cause certain toxic and side effects to the liver and kidneys.

Method used

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  • Compound doxycycline-hydrochloride florfenicol sustained-release microsphere suspension injection for veterinary use
  • Compound doxycycline-hydrochloride florfenicol sustained-release microsphere suspension injection for veterinary use
  • Compound doxycycline-hydrochloride florfenicol sustained-release microsphere suspension injection for veterinary use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The prescription of a kind of veterinary compound doxycycline hydrochloride and florfenicol sustained-release microsphere suspension injection is shown in Table 1, and the preparation steps include:

[0037] (1) Weigh 15g of hydroxypropyl-β-cyclodextrin into a round bottom flask, add an appropriate amount of ethanol to it and stir on a stirrer to completely dissolve the hydroxypropyl-β-cyclodextrin, and weigh 5g of them accurately Add doxycycline hydrochloride and florfenicol to the round bottom flask, seal and continue to stir for 4-6h to form clathrate molecules;

[0038] (2) Accurately weigh 2.5g polyvinylpyrrolidone K 30Add it into the above-mentioned round-bottom flask, and then use a rotary evaporator to evaporate and remove the organic solvent ethanol at 50°C until the powdery microspheres completely remain on the wall of the round-bottom flask to obtain powdery microspheres A;

[0039] (3) Draw 50 mL of deionized water into a 200 mL beaker, add 0.2 g of hydroxy...

Embodiment 2

[0046] A composition of veterinary compound doxycycline hydrochloride and florfenicol sustained-release microsphere suspension injection is shown in Table 2, and the preparation steps include:

[0047] (1) Weigh 30g of β-cyclodextrin in a round bottom flask, add appropriate amount of ethanol to it and stir on a stirrer to completely dissolve the β-cyclodextrin, and accurately weigh 5g of doxycycline hydrochloride and 20g of fluorobenzene Nicotine was added to the round bottom flask, sealed, and continued to stir for 4-6h to form clathrates;

[0048] (2) Accurately weigh 7.5g of polyvinyl alcohol and add it to the above-mentioned round-bottomed flask, and use a rotary evaporator to evaporate and remove the organic solvent ethanol at 50°C until the powdery microspheres completely remain on the wall of the round-bottomed flask. Microsphere A;

[0049] (3) Draw 40 mL of deionized water into a 200 mL beaker, add 2 g of hydroxypropyl methylcellulose, 0.25 g of sodium formaldehyde s...

Embodiment 3

[0057] A composition of veterinary compound doxycycline hydrochloride and florfenicol sustained-release microsphere suspension injection is shown in Table 3, and the preparation steps include:

[0058] (1) Weigh 15g of hydroxypropyl-β-cyclodextrin and 10g of β-cyclodextrin in a round bottom flask, add an appropriate amount of ethanol to it and stir on a stirrer to make hydroxypropyl-β-cyclodextrin and β-cyclodextrin -The cyclodextrin is completely dissolved, and accurately weigh 20g of doxycycline hydrochloride and 5g of florfenicol respectively and add them into the round bottom flask, seal it, and continue to stir for 4-6h to form an inclusion compound;

[0059] (2) Accurately weigh 5g polyvinylpyrrolidone K 30 and 2.5g of polyvinyl alcohol were added to the above-mentioned round bottom flask, and then the organic solvent ethanol was evaporated and removed with a rotary evaporator at 50°C until the powdery microspheres remained on the wall of the round bottom flask completel...

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Abstract

The invention belongs to the technical field of veterinary drug preparation, and relates to a compound doxycycline-hydrochloride florfenicol sustained-release microsphere suspension injection for veterinary use. The suspension injection is produced through a preparation technology combining an inclusion technology, a microcapsule technology and a high-pressure homogenization technology. The suspension injection comprises the following ingredients according to W / V: 10-30% of an inclusion material, 5-20% of doxycycline hydrochloride, 5-20% of florfenicol, 2.5-7.5% of a high-molecular capsule material, 0.2-1% of a suspending agent, 0.25-1% of an anti-oxidant, 0.05-0.2% of a metal chelator, 0.1-0.4% of an antiseptic, and the balance injection water. The active ingredients in the injection possess synergic antibacterial effects and obvious sustained release effect, clinic dosing frequency is reduced, the injection does not contain organic solvents, does not stimulate target animals, is small in toxic and side effects, and is capable of controlling respiratory diseases caused by streptococcus suis, actinobacillus pleuropneumoniae, pasteurella multocida, haemophilus parasuis, mycoplasma and the like.

Description

technical field [0001] The invention relates to the field of preparation of new veterinary drug preparations, in particular to a veterinary compound doxycycline hydrochloride florfenicol sustained-release microsphere suspension injection and a preparation method and application thereof. Background technique [0002] Porcine respiratory disease is a kind of infectious disease that is extremely harmful in the intensive pig industry at present. The secondary infection and mixed infection of various pathogens such as mycoplasma have caused huge economic losses and harm to the pig industry in my country. Doxycycline hydrochloride and florfenicol are widely used in veterinary clinics to treat porcine respiratory diseases caused by sensitive bacteria, but they have a short half-life, rapid metabolism in the body, and require frequent administration of high doses, which not only affect the The treatment effect also increases the stress intensity of animals and the labor intensity an...

Claims

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Application Information

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IPC IPC(8): A61K31/65A61K9/10A61P31/04A61K31/165
Inventor 袁宗辉谢书宇李先强王玉莲潘源虎黄玲利瞿伟陈冬梅程古月刘振利谢长清
Owner HUAZHONG AGRI UNIV
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