Lung targeted cefquinome sulfate PLGA microspheres and preparation method thereof

A technology of cefquinol sulfate and cefquinol, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., to achieve high reproducibility, mild preparation conditions, and simple operation methods Effect

Active Publication Date: 2017-11-03
QINGDAO AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are still some defects in the preparation of lung-targeting cefquinol sulfate PLGA microspheres, and the application effect needs to be further improved

Method used

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  • Lung targeted cefquinome sulfate PLGA microspheres and preparation method thereof
  • Lung targeted cefquinome sulfate PLGA microspheres and preparation method thereof
  • Lung targeted cefquinome sulfate PLGA microspheres and preparation method thereof

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preparation example Construction

[0025] The present invention is achieved through the following measures: a lung-targeted cefquinol sulfate PLGA microsphere, the preparation method comprising the following steps:

[0026] The raw material drug and the dispersant are mixed according to the ratio of 1g: 2-5ml, put into a frequency conversion planetary ball mill, and ball milled. The milling time is ball milling for 1-3h, with an interval of 0.5-1.5h, and then ball milling for 1-3h, and the liquid is evaporated to obtain Processed raw material drug cefquinol; take PLGA and PLA in proportion as carrier, and the carrier is dissolved in the mixed solvent of 200ml dichloromethane and methanol, after completely dissolving, add cefquinol raw material drug in proportion, and then Add glidant, mix by ultrasonic wave, ultrasonic 1-1.5min with low power 300-400w, ultrasonic 0.5-1min with high power 800-1000w, then spray dry with two-fluid spray dryer, and carry out magnetic stirring at the same time, spray dry The sample ...

Embodiment 1

[0154] The preparation method comprises the following steps:

[0155] Mix 3.7g of bulk drug with 15ml of dispersant, put into frequency conversion planetary ball mill, ball mill, milling time is ball mill 2h, intermittent 1h, ball mill again 2h, evaporate the liquid, obtain the treated bulk drug cefquinol; weigh PLGA and PLA is used as a carrier, and the carrier is dissolved in a mixed solvent of 200ml of dichloromethane and methanol. After it is completely dissolved, the raw material of cefquinol is added, and then 0.15g of glidant is added. 1min, high-power 800w ultrasonic 0.5min, and then use a two-fluid spray dryer for spray drying, and magnetic stirring at the same time, the injection speed of spray drying is 8ml / min, and then obtain lung targeting cefquinol sulfate PLGA micro Ball microspheres.

[0156] Wherein, in the dispersant, the volume ratio of ethanol:isopropanol:dichloromethane is 5:2:1.

[0157] Wherein, the grinding machine used is a frequency conversion plan...

Embodiment 2

[0164] The preparation method comprises the following steps:

[0165] Mix 4g of the raw material with 20ml of the dispersant, put it into a variable frequency planetary ball mill, and mill it. The milling time is 2 hours, with an interval of 1 hour, and then ball milled for 2 hours, and evaporate the liquid to obtain the treated raw drug cefquinol; weigh 10g of PLGA according to the proportion and PLA2g as carrier, the carrier is dissolved in the mixed solvent of 200ml dichloromethane and methyl alcohol, after dissolving completely, add cefquinol bulk drug in proportion, then add 0.3g flow aid, by ultrasonic mixing, low Ultrasound at 350w for 1min, high power at 900w for 1min, and then use a two-fluid spray dryer for spray drying with magnetic stirring at the same time. PLGA Microspheres Microspheres.

[0166] Wherein, in the dispersant, the volume ratio of ethanol:isopropanol:dichloromethane is 5:2:1.

[0167] Wherein, the grinding machine used is a frequency conversion pla...

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Abstract

The invention provides lung targeted cefquinome sulfate PLGA microspheres and a preparation method thereof and belongs to the technical field of antibiotics targeted preparations for animals. The preparation method comprises the following steps: uniformly mixing a bulk drug with a dispersant, performing ball-milling, and completely evaporating liquid to obtain treated bulk drug cefquinome; weighing PLGA and PLA as carriers, dissolving the carriers in a mixed solvent, adding the bulk drug after complete dissolution, then adding a flow aid, performing spray-drying through ultrasonic mixing, meanwhile, performing magnetic stirring, and then adopting a vortex separator to obtain the microspheres. The microsphere encapsulation ratio is 95% or above, the drug loading capacity is 20% or above, and 85% or more microspheres have the grain sizes of 10-25 [mu]m; the operation method is simple and convenient, the microsphere preparation efficiency is high, and the obtained microspheres are good in dispersity and have a favorable slow-release effect and lung targeting characteristic. An established tissue Chinese herbal medicine detection method is good in specificity, high in sensitiveness and recovery rate and excellent in degree of precision.

Description

technical field [0001] The invention relates to the technical field of antibiotic targeting preparations, in particular to a lung-targeting cefquinol sulfate PLGA microsphere and a preparation method thereof. Background technique [0002] Cefquinome, also known as cefquinome, is the first fourth-generation cephalosporin antibiotic for animals developed by Hoechst Roussel Vet in Germany. It is widely used at home and abroad to treat respiratory diseases of livestock. [0003] The research and development of cefquinol and its preparations in my country is relatively late. At present, only cefquinol sulfate raw material and its injection (suspension injection, injection powder injection) have been approved by the Ministry of Agriculture for production and sales, which matches There are fewer types of dosage forms. Oral absorption of cefquinol is not good, injection absorption is relatively rapid, and the half-life in the body is short, only 1 to 3 hours. In order to achieve a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/34A61P31/04A61P11/00
CPCA61K9/0002A61K9/1641A61K31/546
Inventor 郝智慧曲少奇戴存春
Owner QINGDAO AGRI UNIV
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