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A kind of lung targeting cefquinol sulfate gelatin microspheres and preparation method thereof

A quinol gelatin and lung-targeting technology, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, and medical preparations containing active ingredients. No problem, inconvenient clinical application, etc., to achieve the effect of high reproducibility, easy control of microsphere particle size, and excellent precision

Active Publication Date: 2020-05-05
QINGDAO AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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 an effective therapeutic concentration, multiple injections are required, which brings great inconvenience to clinical application.

Method used

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  • A kind of lung targeting cefquinol sulfate gelatin microspheres and preparation method thereof
  • A kind of lung targeting cefquinol sulfate gelatin microspheres and preparation method thereof
  • A kind of lung targeting cefquinol sulfate gelatin microspheres and preparation method thereof

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preparation example Construction

[0027] The present invention is achieved through the following measures: a lung targeting cefquinol sulfate gelatin microspheres, the preparation method comprising the following steps:

[0028] In the first step, the raw material drug and the dispersant are mixed according to the ratio of 1g: 2-5ml, put into the frequency conversion planetary ball mill, ball mill for 1-3h, intermittently for 0.5-1.5h, and then ball mill for 1-3h, evaporate the liquid, and get the treatment Subsequent raw materials;

[0029] In the second step, weigh gelatin and sodium alginate as carriers, dissolve them in double distilled water at 40-50°C, heat and stir until they are completely dissolved, then add cefquinol raw materials in proportion, and mix them evenly by ultrasonic waves. 300-400w ultrasonic for 1-2min, high power 600-1000w ultrasonic for 1-2min, add flow aid, mix well to form a mixture, then add glutaraldehyde solution, and then use double-flow spray dryer for spray drying, and magnetic...

Embodiment 1

[0158] The preparation method comprises the following steps:

[0159] In the first step, mix 3.3g of raw material medicine with 16ml of dispersant, put it into a frequency conversion planetary ball mill, ball mill for 2 hours, intermittently for 1 hour, ball mill for another 2 hours, and evaporate the liquid to obtain the treated raw medicine;

[0160] In the second step, weigh 10g of gelatin and 3.3g of sodium alginate as carriers, dissolve them in 250ml of double-distilled water at 50°C, heat and stir until completely dissolved, then add the cefquinol raw material, and mix them evenly by ultrasonic waves. 400w ultrasonic for 1min, high power 1000w ultrasonic for 1min, add 0.133g flow aid, mix to form a mixture, then add glutaraldehyde solution, then spray dry with double-flow spray dryer, and need magnetic stirring at the same time, spray dry to get microspheres.

[0161] Wherein, in the dispersant, the volume ratio of ethanol:isopropanol:dichloromethane is 5:2:1.

[0162] ...

Embodiment 2

[0169] The preparation method comprises the following steps:

[0170] In the first step, mix 1.1g of raw material medicine with 5ml of dispersant, put it into a frequency conversion planetary ball mill, ball mill for 1 hour, intermittently for 0.5 hour, ball mill for another 1 hour, and evaporate the liquid to obtain the treated raw material medicine;

[0171] In the second step, weigh 10g of gelatin and 1g of sodium alginate as the carrier, dissolve them in 250ml of double distilled water at 50°C, heat and stir until completely dissolved, then add the cefquinol raw material, mix well by ultrasonic wave, low power 400w Ultrasonic for 2 minutes, high power 1000w ultrasonic for 2 minutes, add 0.33g flow aid, mix to form a mixture, then add glutaraldehyde solution, and then use a double-flow spray dryer for spray drying, while requiring magnetic stirring, and spray drying to obtain microspheres.

[0172] Wherein, in the dispersant, the volume ratio of ethanol:isopropanol:dichloro...

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Abstract

The invention provides a lung-targeted cefquinome sulfate gelatin microsphere and a preparation method thereof, and belongs to the technical field of animal antibiotic targeting preparations, the preparation method comprises the following steps: evenly mixing a raw material medicine and a dispersing agent, performing ball-milling, volatilizing until the liquid is dried to obtain a processed raw material medicine; weighing gelatin and sodium alginate as carriers, dissolving the gelatin and the sodium alginate in double distilled water at 40-50DEG C, heating and stirring until the gelatin and the sodium alginate are completely dissolved, adding cefquinome, adding a glidant, mixing evenly, adding a glutaraldehyde solution, using a double flow spray dryer for spray drying, magnetically stirring, spraying and drying to obtain the microsphere. The encapsulation efficiency of the microsphere is 90% or more, the drug loading capacity is 20% or more, the particle size of 90% or more of the microsphere is distributed in the range of 10-25um, the preparation method has the advantages of simple operation, high efficiency of preparation of the microspheres, the microsphere has good sustained-release effect and targeting property; the established organization drug detection method has good specificity, high sensitivity and recovery rate and good precision.

Description

technical field [0001] The invention relates to the technical field of antibiotic targeting preparations, in particular to a lung-targeting cefquinol sulfate gelatin 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 achiev...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/42A61K47/36A61K31/546A61P31/04A61P11/00
CPCA61K9/0002A61K9/1652A61K9/1658A61K31/546
Inventor 郝智慧曲少奇戴存春
Owner QINGDAO AGRI UNIV
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