Lung-targeting gelatin microsphere agent containing cefquinome sulfate and preparation method of lung-targeting gelatin microsphere agents

A cefquinol sulfate, lung-targeting technology, applied in the direction of bulk delivery, respiratory diseases, inactive components of polymer compounds, etc. Inconvenient clinical application and other problems, to achieve the effect of reducing toxic side effects, prolonging residence time, and improving curative effect

Inactive Publication Date: 2015-11-11
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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  • Lung-targeting gelatin microsphere agent containing cefquinome sulfate and preparation method of lung-targeting gelatin microsphere agents
  • Lung-targeting gelatin microsphere agent containing cefquinome sulfate and preparation method of lung-targeting gelatin microsphere agents
  • Lung-targeting gelatin microsphere agent containing cefquinome sulfate and preparation method of lung-targeting gelatin microsphere agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0187] Accurately weigh 0.60g of gelatin and dissolve it in 3mL of water at 50°C to obtain an aqueous solution with a gelatin concentration of 20%; accurately weigh 0.20g of cefquinol sulfate, add it to the gelatin solution, and use a probe to ultrasonically disperse for 5 cycles. Power 600W, ultrasonic 4s, stop 5s, as the final water phase; Measure 20mL of liquid paraffin, add 0.4mL emulsifier span-80, mix well, preheat to 50°C, stir at 800rpm, mix the above water phase (drug Gelatin solution) was slowly added dropwise to the oil phase, stirred and emulsified for 15 minutes; the emulsion was placed in an ice bath at 4°C for 20 minutes, stirred at a low speed, and 1.0 mL of 50% glutaraldehyde aqueous solution was slowly added dropwise, and the reaction crosslinked for 1.5 hours; cold isopropanol was added 25mL, dehydrated for 25min, and filtered through a 0.45um membrane to obtain microspheres; wash the microspheres once with ether, twice with acetone, and vacuum-dry at room te...

Embodiment 2

[0190] Accurately weigh 0.40g gelatin, 0.05g chitosan, put in 2% acetic acid aqueous solution water 3mL and dissolve at 50 ℃, make the aqueous solution that carrier material concentration is 15%; Accurately weigh 0.225g cefquinol sulfate, add to In the carrier material solution, use the probe to ultrasonically disperse 5 cycles, ultrasonic power 600W, ultrasonic 4s, stop 5s, as the final water phase; measure 20mL of liquid paraffin, add 0.4mL emulsifier span-80, mix well, and preheat to 50°C, under stirring at 800rpm, slowly drop the above water phase into the oil phase, stir and emulsify for 15min; place the emulsion in ice bath at 4°C for 20min, stir at low speed, slowly add 1.5mL of 50% glutaraldehyde aqueous solution dropwise, and the reaction Add 25 mL of cold isopropanol, dehydrate for 25 min, and filter through a 0.45 μm membrane to obtain microspheres; wash the microspheres once with ether, twice with acetone, and vacuum-dry at room temperature to obtain drug-loaded mic...

Embodiment 3

[0193] 1) Take 0.09g gelatin, 0.66g chitosan, 0.006g N,N-dimethylacetamide, 0.001g N-[3-(aminomethyl)benzyl]carbamate tert-butyl ester and 0.043g formamide, add 3.2ml of water at 40°C was used as a 20% carrier solution, and 0.2g of cefquinol sulfate was dispersed into the carrier solution with an ultrasonic probe in 5 cycles of ultrasonic power of 600W, ultrasonic for 5s, and stop for 5s to form an aqueous phase;

[0194] 2) Take 20ml of liquid paraffin and 0.67ml of sorbitan oleate, mix well to form an oil phase, take the water phase obtained in step 1), preheat to 50°C, stir at 800rpm, slowly drop the water phase Add to the oil phase, stir and emulsify for 20min;

[0195] 3) The emulsion obtained in step 2) was placed in an ice bath at 4°C for 30 minutes, stirred at a low speed, and 2 mL of a 50% glutaraldehyde solution of a crosslinking agent was slowly added dropwise, and the reaction crosslinked for 1.5 hours;

[0196] 4) Add 30 mL of isopropanol to the reactant obtained...

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Abstract

The invention discloses a lung-targeting gelatin microsphere agent containing cefquinome sulfate and a preparation method of the lung-targeting gelatin microsphere agent. According to the lung-targeting gelatin microsphere agent, cefquinome sulfate is taken as the active ingredient, gelatin or gelatin-chitosan compound is taken as a carrier, and the weight ratio of the active ingredient to the carrier is 1 to 2-6. The invention further provides the preparation method of the lung-targeting gelatin microsphere agent. The encapsulation efficiency of the prepared microspheres is 65% or above, the particle sizes of 80% or more of the microspheres are distributed within 7-35 um, so that the microsphere agent can gather to the lung in a targeted manner, the therapeutic effect of the medicine is effectively improved, the toxic and side effects of the medicine are reduced, meanwhile, the retaining time of the medicine in the lug is prolonged, the concentration of the blood concentration is kept stable, and the long-term effect is achieved.

Description

technical field [0001] The invention relates to the technical field of veterinary preparations, in particular to a cefquinol sulfate lung-targeting gelatin microsphere preparation and a preparation method thereof. Background technique [0002] Cefquinol is the first fourth-generation cephalosporin antibiotic for animals. It is widely used at home and abroad to treat respiratory diseases of livestock because of its strong antibacterial activity, broad antibacterial spectrum and low drug resistance. [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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/42A61P31/04A61P11/00
Inventor 郝智慧丁兆鹏王仕文高明星曲少奇
Owner QINGDAO AGRI UNIV
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