Composite cefquinome microsphere gel preparation and preparation method thereof

A technology of cefquinome and compound preparations, which is applied in the field of cefquinome microsphere gel compound preparations and its preparation, can solve the problems of personnel and drug waste, reduce the frequency of administration, etc., and achieve improved drug efficacy, reduced exposure, and prolonged The effect of entry time

Active Publication Date: 2017-03-08
RINGPU TIANJIN BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Therefore the subject of the present invention is to study how to develop the lung-targeted sustained-release preparation of cefquinome, aiming at improving the drug concentration at t

Method used

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  • Composite cefquinome microsphere gel preparation and preparation method thereof
  • Composite cefquinome microsphere gel preparation and preparation method thereof
  • Composite cefquinome microsphere gel preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The cefquinome microsphere gel composite preparation of the present invention is prepared by weight from the following raw materials:

[0032]

[0033] Preparation method:

[0034] 1. Take polylactic acid-glycolic acid copolymer, add it to ethyl acetate, then add 100g of cefquinome micropowder, shear and stir to form a uniform suspension, at an inlet temperature of 40°C, a feed rate of 100ml / h, Under the conditions of pressure 0.4MPa and power 20Hz, carry out spray drying to obtain microsphere powder for future use;

[0035] 2. Take 3g of sodium hyaluronate (molecular weight: 2 million), add 900g of water for injection, make it infiltrate and swell to form a transparent gel matrix, mix the gel matrix and microsphere powder, and stir until uniform.

Embodiment 2

[0037] The veterinary cefquinoxime microsphere gel composite preparation of the present invention is prepared by weight from the following raw materials:

[0038]

[0039]

[0040] Preparation method:

[0041] 1. Take polylactic acid-glycolic acid copolymer, add it to acetone, then add 100g of cefquinome micropowder, and shear and stir to form a uniform suspension. Carry out spray drying under KPa, power 40Hz parameter condition, obtain microsphere powder, standby;

[0042] 2. Take 10g of sodium hyaluronate (molecular weight: 1,000,000), add 900g of water for injection, and make it infiltrate and swell to form a transparent gel matrix. Mix the gel base and the microsphere powder, stir until uniform, and obtain.

Embodiment 3

[0044] The veterinary cefquinoxime microsphere gel composite preparation of the present invention is prepared by weight from the following raw materials:

[0045]

[0046] Preparation method:

[0047] 1. Take polylactic acid-glycolic acid copolymer, add it to chloroform, then add 100g of cefquinome micropowder, and shear and stir to form a uniform suspension. Carry out spray drying under KPa, power 30Hz parameter condition, obtain microsphere powder, standby;

[0048] 2. Take 90g of sodium hyaluronate (molecular weight: 100,000) and add 900g of water to make it infiltrate and swell into a transparent gel matrix. Mix the gel base and the microsphere powder, stir until uniform, and obtain.

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Abstract

The invention discloses a composite cefquinome microsphere gel preparation and a preparation method thereof, and belongs to the technical field of medicines. The composite cefquinome microsphere gel preparation for veterinary use is prepared by adopting a spray drying method to prepare microspheres, adopting cefquinome as the medicine for the microspheres, adopting polylactic acid/polylactic acid-glycolic acid as a coating carrier material, and adopting hyaluronic acid and water as gel bases to prepare the composite cefquinome microsphere gel preparation. The microspheres are of 5-30umd in grain size, which is beneficial to lung targeting of the main medicine cefquinome, the cefquinome can easily gather at a target organ, blood clearance is reduced, long-time circulation is benefited, and pharmacological efficacy is improved. In addition, by the aid of the gel bases, contact of the medicine and interstitial fluid is reduced, the time of the medicine flowing into a bloodstream is prolonged, and a slow-release effect of the preparation is further increased.

Description

technical field [0001] The invention relates to a cefquinome microsphere gel composite preparation and a preparation method thereof. The preparation is mainly used for subcutaneous administration and for the treatment of pigs and cattle respiratory diseases and cow mastitis, and belongs to the field of pharmaceutical preparations. Background technique [0002] Cefquinoxime has another name called cefquinol and cefquinome. It is currently the only fourth-generation cephalosporin antibiotic for animals. It has the following advantages: 1. It is highly stable to β-lactamase. 2. Its intrinsic antibacterial activity is stronger than that of the third-generation cephalosporin ceftiofur. Compared with the third-generation cephalosporins, the plasma half-life of the fourth-generation cephalosporins is longer and has no nephrotoxicity. 3. It has strong antibacterial activity, which is effective against Staphylococcus aureus, Streptococcus, Pseudomonas aeruginosa, Enterobacteriaceae ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/06A61K31/546A61K47/36A61K47/34A61P31/04
Inventor 张珺聂丽娜李旭东刘爱玲刘桂兰井丁丁夏雪林
Owner RINGPU TIANJIN BIOLOGICAL PHARMA
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