Preparation method of ceftiofur microspheres

A technology of ceftiofur and microspheres, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of strong hydrophobicity and unfavorable release of insoluble drugs, and achieve load High drug dosage, good biocompatibility, and low energy consumption

Active Publication Date: 2021-02-12
山东华辰制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] PLA microspheres are not conducive to the release of insoluble drugs due to their strong hydrophobicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: A preparation method of ceftiofur microspheres, the polylactic acid-polyethylene glycol block copolymer is dissolved in an organic solvent as a carrier material, and the drug ceftiofur is dispersed in the carrier material solution through ultrasonic waves. Mix to form a dispersed phase, and the mass percentage of the carrier material and the drug ceftiofur is 1:5. At a temperature of 25°C, add the above-mentioned dispersed phase into water, add Tween as an emulsifier, and stir with a constant temperature magnetic force at a speed of 3000rpm to fully emulsify to obtain an O / W (O: represents the oil phase; W: represents the water phase) type emulsion. The volume ratio of the dispersed phase to the continuous phase is 1:10; quickly stir the emulsion at a temperature of 40°C for 1 hour to evaporate and remove part of the organic solvent, add an appropriate amount of water to the emulsion, and rapidly extract the initially dried microspheres to form a hard film, an...

Embodiment 2

[0029] Example 2: A preparation method of ceftiofur microspheres, dissolving polylactic acid-polyethylene glycol block copolymer as a carrier material in an organic solvent, and dispersing the drug ceftiofur in the carrier material solution through ultrasonic waves. The dispersed phase is prepared by mixing, and the mass percentage of the carrier material and the drug ceftiofur is 1:10. At a temperature of 25°C, add the above dispersed phase into water, add Tween and monocaprate as emulsifiers, stir with constant temperature magnetic force, and rotate at a speed of 2000rpm to fully emulsify to obtain O / W (O: represents the oil phase; W: represents the water phase) type emulsion, the volume ratio of the dispersed phase to the continuous phase is 1:5; the emulsion is rapidly stirred at a temperature of 40°C for 1 hour to evaporate and remove part of the organic solvent, and an appropriate amount of water is added to the emulsion to rapidly extract and form the initially dried mic...

Embodiment 3

[0034] Example 3: A preparation method of ceftiofur microspheres, dissolving the polylactic acid-polyethylene glycol block copolymer as a carrier material in an organic solvent, and dispersing the drug ceftiofur in the carrier material solution through ultrasonic waves. The dispersed phase is prepared by mixing, and the mass percentage of the carrier material and the drug ceftiofur is 1:10. At a temperature of 25°C, add the above-mentioned dispersed phase to water, add Tween as an emulsifier, stir with a constant temperature non-magnetic machine, and rotate at a speed of 3000rpm to fully emulsify to obtain an O / W (O: represents the oil phase; W: represents the water phase) type emulsion liquid, the volume ratio of the dispersed phase to the continuous phase is 1:5; quickly stir the emulsion at a temperature of 40°C for 1 hour to evaporate and remove part of the organic solvent, add an appropriate amount of water to the emulsion, and rapidly extract the initially dried microsphe...

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Abstract

The invention discloses a preparation method of ceftiofur microspheres, and relates to the field of veterinary drugs, and the preparation method comprises the following steps: 1, dissolving a polylactic acid-polyethylene glycol segmented copolymer as a carrier material in an organic solvent; 2, adding ceftiofur, and stirring and mixing to prepare a dispersion phase; 3, adding the dispersion phaseinto water, adding an emulsifier, and magnetically stirring and emulsifying to obtain an emulsion; 4, rapidly stirring the emulsion for a period of time T1, supplementing water, and continuously stirring for a period of time T2 until the organic solvent is completely volatilized; and 5, centrifuging, washing, collecting and drying in vacuum to obtain the ceftiofur microsphere. According to the ceftiofur sustained-release microsphere disclosed by the invention, a drug is more uniformly dispersed in a carrier material, the drug loading capacity is high, a dispersion system of drug particles is reduced by virtue of a nanoscale microsphere technology, and the ceftiofur sustained-release microsphere has better needle permeability, so that the drug has a stronger sustained-release effect and a longer sustained drug effect.

Description

technical field [0001] The invention relates to the field of veterinary medicine, in particular to a preparation method of ceftiofur microspheres. Background technique [0002] Ceftiofur is the third-generation cephalosporin for animals. It is widely used all over the world because of its strong antibacterial activity, broad antibacterial spectrum, excellent pharmacokinetic characteristics, small toxic and side effects, and low residue. [0003] At present, the ceftiofur-related preparations that have been marketed in China mainly include ceftiofur injection, ceftiofur sodium powder injection, and ceftiofur hydrochloride injection. Since ceftiofur is not well absorbed orally, it is mainly used by injection. To reach the effective therapeutic concentration, multiple injections are required, usually once a day for 3 to 5 consecutive days, which is very inconvenient in the clinical application process. In order to reduce the animal stress response caused by frequent injection ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/34A61P31/04
CPCA61K9/1641A61K9/1694A61K31/546A61P31/04
Inventor 王建国王少娟刘海王春梅周愉淇匡宝晓
Owner 山东华辰制药有限公司
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