Lung-targeted PLGA (polylactic-co-glycolic-acid) microsphere preparation of cefquinome sulfate and preparation method of lung-targeted PLGA microsphere preparation

A technology of cefquinol sulfate and lung targeting, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., and can solve the short-term, only 1 to 3 hours, cefquinol Poor absorption, inconvenient clinical application and other problems, to achieve the effect of reducing toxic and 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

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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 or

Method used

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  • Lung-targeted PLGA (polylactic-co-glycolic-acid) microsphere preparation of cefquinome sulfate and preparation method of lung-targeted PLGA microsphere preparation
  • Lung-targeted PLGA (polylactic-co-glycolic-acid) microsphere preparation of cefquinome sulfate and preparation method of lung-targeted PLGA microsphere preparation
  • Lung-targeted PLGA (polylactic-co-glycolic-acid) microsphere preparation of cefquinome sulfate and preparation method of lung-targeted PLGA microsphere preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0187] Accurately weigh 45 mg of cefquinol sulfate, add it to 0.4 mL of a 15% gelatin solution (W / V), and uniformly disperse cefquinol sulfate with probe ultrasound as the inner water phase W1; weigh 450 mg of PLGA (molecular weight: 100,000), vortex Spin and dissolve into 3 mL of dichloromethane (DCM) to make a 15% concentration (W / V) PLGA solution in dichloromethane as oil phase O; ultrasonically emulsify the above-mentioned inner water phase W1 into oil phase O to form W1 / O-type colostrum; quickly transfer the colostrum to 35mL of 1% (W / V) PVA aqueous solution W2, shear and emulsify it with a high-speed shearing machine for 30s at 3000rpm to form a W1 / O / W2 type double emulsion; The double-emulsion solution was added to 150 mL of 0.25% (W / V) PVA aqueous solution containing 1% NaCl, placed on a magnetic stirrer and stirred at low speed for 3 hours, and evaporated at room temperature to remove dichloromethane; The microspheres were washed three times with pure water and freez...

Embodiment 2

[0190] Accurately weigh 60 mg of cefquinol sulfate, add it to 0.4 mL of a 10% gelatin solution (W / V), and disperse cefquinol sulfate evenly with probe ultrasound as the inner aqueous phase W 1 ; Take 450mg PLGA (molecular weight 100,000), dissolve in the mixed solvent of 2.7mL dichloromethane and 0.3mL ethyl acetate by vortex, make the PLGA solution of 15% concentration (W / V) as oil phase O; Internal water phase W 1 phacoemulsification into oil phase O to form W 1 / O-type colostrum; this colostrum was quickly transferred to 35 mL of 1% (W / V) PVA in water containing 1% NaCl W 2 , at 3200rpm, shear and emulsification with a high-speed shearing machine for 30s to form W 1 / O / W 2 type double emulsion; add the double emulsion solution to 150 mL of 0.25% (W / V) PVA aqueous solution containing 1% NaCl, place it on a magnetic stirrer and stir at low speed for 3 hours, and volatilize at room temperature to remove dichloromethane and ethyl acetate; The microspheres were collected by c...

Embodiment 3

[0193] Accurately weigh 60 mg of cefquinol sulfate, add it to 0.4 mL of a 10% gelatin solution (W / V), and disperse cefquinol sulfate evenly with probe ultrasound as the inner aqueous phase W 1 Weigh 450mg PLGA (molecular weight 100,000), dissolve in 450mg organic solvent by vortex, and the PLGA solution of 15% concentration (W / V) is used as oil phase O; The above-mentioned inner water phase W 1 phacoemulsification into oil phase O to form W 1 / O type colostrum; this colostrum was quickly transferred to 35mL of 1% (W / V) PVA water solution W 2 , at 3200rpm, shear and emulsification with a high-speed shearing machine for 30s to form W 1 / O / W 2 type double emulsion; add the double emulsion solution to 150 mL of 0.25% (W / V) PVA aqueous solution, place it on a magnetic stirrer and stir at low speed for 3 hours, and volatilize and remove the organic solvent at room temperature; The microspheres were washed three times with pure water and freeze-dried to obtain a PLGA microsphere p...

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Abstract

The invention discloses a lung-targeted PLGA (polylactic-co-glycolic-acid) microsphere preparation of cefquinome sulfate. The lung-targeted PLGA microsphere preparation is prepared by cefquinome sulfate serving as an active pharmaceutical ingredient and PLGA serving as a carrier according to a weight ratio of 1:5-20. The invention further provides a preparation method of the lung-targeted PLGA microsphere preparation. The lung-targeted PLGA microsphere preparation and the preparation method have the advantages that encapsulation efficiency of prepared microspheres is higher than 60%, and grain diameter of more than 85% of the microspheres ranges from 7um to 35um, so that the microsphere preparation can be gathered in a lung in a targeted manner, curative effect of the microsphere preparation is improved effectively, and toxic and side effect of the microsphere preparation is lowered; detention time of the microsphere combination in the lung can be increased, and blood-drug concentration can be maintained stable to realize long-acting effect.

Description

technical field [0001] The invention relates to the technical field of veterinary preparations, in particular to a lung-targeted PLGA microsphere preparation of cefquinol sulfate and a preparation method thereof. Background technique [0002] Cefquinol is the first 4th generation cephalosporin antibiotic for animals. It is widely used at home and abroad to treat respiratory diseases of livestock due to 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 materials and its injections (suspension injection, injection powder injection) have been approved by the Ministry of Agriculture for production and sales, which matches with it. There are fewer types of dosage forms. Oral absorption of cefquinol is not good, injection absorption is relatively rapid, and the half-life in vivo is short, only 1 to 3...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/546A61K47/34A61P11/00A61P31/04
Inventor 郝智慧丁兆鹏王仕文高明星曲少奇
Owner QINGDAO AGRI UNIV
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