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Amoxicillin biodegradable microsphere long-acting sustained-release preparation and preparation method thereof

A technology of amoxicillin and biodegradation, applied in the field of amoxicillin biodegradable microsphere long-acting sustained-release preparations and its preparation, can solve the problems of inability to maintain effective blood drug concentration, instability of β-lactam ring, short half-life, etc. problems, to achieve the effects of obvious sustained-release effect, no toxic side effects, and low burst release dose

Inactive Publication Date: 2017-12-22
王荻
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But amoxicillin in animals T 1 / 2 The half-life is short, and the effective blood drug concentration cannot be maintained for a long time, and because the β-lactam ring in the amoxicillin molecule is unstable, it can be used in aqueous solution under the action of acid, alkali, certain metal ions or oxidants. The β-lactam ring opens, molecular rearrangement occurs, and a series of degradation products are produced

Method used

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  • Amoxicillin biodegradable microsphere long-acting sustained-release preparation and preparation method thereof
  • Amoxicillin biodegradable microsphere long-acting sustained-release preparation and preparation method thereof
  • Amoxicillin biodegradable microsphere long-acting sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Long-acting sustained-release preparation of amoxicillin biodegradable microspheres with a drug concentration of 10%

[0028] The preparation method is as follows:

[0029] (1) Slowly add 1 g of PLGA into 10 ml of triacetin and heat to 50°C, stir slowly until it is completely dissolved to obtain a viscous liquid and let it stand at room temperature.

[0030] (2) Add 12g of amoxicillin raw material (95% amoxicillin content) into 10ml of polyethylene glycol 400, and add 1ml of Tween 80, stir rapidly to make it fully mixed.

[0031] (3) Slowly add the suspension solution obtained in (2) into the viscous liquid described in (1), and stir at high speed for 15-20 minutes, so that all the drugs are mixed evenly, and the paste-like semi-solid drug dispersion phase I is obtained at room temperature.

[0032] (4) Heat 70g of polyethylene glycol 4000 in a water bath to the molten state at 50°C as the continuous phase II, slowly add the drug dispersion phase I obtained in (3) into...

Embodiment 2

[0036] Long-acting sustained-release preparation of amoxicillin biodegradable microspheres with a drug concentration of 20%

[0037] The preparation method is as follows:

[0038] (1) Slowly add 2g of PLGA and 1g of PLA into 10ml of triacetin and heat to 50°C, stir slowly until they are completely dissolved to obtain a viscous liquid and let it stand at room temperature.

[0039] (2) Add 22g of amoxicillin raw material (95% amoxicillin content) into 12ml of polyethylene glycol 400, and add 1ml of Tween 80, stir rapidly to make it fully mixed.

[0040] (3) Slowly add the suspension solution obtained in (2) into the viscous liquid described in (1), and stir at high speed for 15-20 minutes, so that all the drugs are mixed evenly, and the paste-like semi-solid drug dispersion phase I is obtained at room temperature.

[0041] (4) Heat 50g of polyethylene glycol 6000 in a water bath to the molten state at 55°C as the continuous phase II, slowly add the drug dispersion phase I obtai...

Embodiment 3

[0045] Long-acting sustained-release preparation of amoxicillin biodegradable microspheres with a drug concentration of 15%

[0046] The preparation method is as follows:

[0047] (1) Slowly add 1g of PLGA and 1g of PLA into 10ml of ethyl acetate, heat to 50°C, stir slowly until all are dissolved, obtain a viscous liquid and let it stand at room temperature.

[0048] (2) Add 18g of amoxicillin raw material (95% amoxicillin content) into 12ml of polyethylene glycol 400, and add 1ml of Tween 80, stir rapidly to make it fully mixed.

[0049] (3) Slowly add the suspension solution obtained in (2) into the viscous liquid described in (1), and stir at high speed for 15-20 minutes, so that all the drugs are mixed evenly, and the paste-like semi-solid drug dispersion phase I is obtained at room temperature.

[0050] (4) Heat 60g of polyethylene glycol 6000 in a water bath to the molten state at 60°C as the continuous phase II, slowly add the drug dispersion phase I obtained in (3) in...

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Abstract

The invention discloses an amoxicillin biodegradable microsphere long-acting sustained-release preparation, which is prepared by mixing a drug dispersion phase I and a continuous phase II, wherein the drug dispersion phase I comprises polyester, acetate, amoxicillin, polyethylene glycol A and Tween, and the continuous phase II is polyethylene glycol B. According to the present invention, the amoxycillin is subjected to microsphere encapsulation by using the polyester as the skeleton material, and the skeleton material encapsulated biodegradable microsphere is subjected to phase dispersion by using polyethylene glycol with good water dispersion property as the continuous phase; and the prepared amoxicillin drug preparation has the microsphere encapsulation structure, can drive the drug to be slowly released along with the entering of the water in the microsphere in the body, and is suitable for the drinking administration of animal populations under the dispersion effect of the polyethylene glycol continuous phase.

Description

technical field [0001] The invention relates to a veterinary amoxicillin pharmaceutical preparation applied to drinking water for animals, in particular to a long-acting sustained-release preparation of amoxicillin biodegradable microspheres and a preparation method thereof. Background technique [0002] Amoxicillin is a semi-synthetic acid-resistant broad-spectrum penicillin drug. Its antibacterial spectrum and antibacterial activity are basically the same as ampicillin, but its acid resistance is stronger than that of ampicillin, and its bactericidal effect is also faster than ampicillin. , especially against Salmonella and Enterococcus. It is widely used in the treatment of bacterial diseases in the process of animal breeding. In the process of animal breeding, group administration usually adopts the method of adding drugs to drinking water, so there are certain requirements for the water dispersibility of pharmaceutical preparations. [0003] The chemical structure of a...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K47/10A61K47/14A61K47/26A61K31/43A61P31/04
Inventor 王荻
Owner 王荻
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