Preparation method of long-acting injection containing danofloxacin mesylate

A dafloxacin mesylate and injection technology, which is applied in the field of long-acting injections, can solve the problems of affecting animal growth, wasting manpower and financial resources, etc., and achieve the effects of good histocompatibility, reducing irritation and being easy to use

Inactive Publication Date: 2014-01-29
中农华威制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Multiple injections waste human and financial resources, and each injection triggers a different degree of stress response in animals, which affects animal growth

Method used

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  • Preparation method of long-acting injection containing danofloxacin mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1, preparation 30% dafloxacin mesylate injection

[0024] Preparation composition: 150g of dafloxacin mesylate, 125g of SAIB, 4.5g of aluminum stearate, 0.05g of BHA, 0.05g of BHT, 0.025g of PG, 100ml of benzyl benzoate, and 500ml of ethyl oleate.

[0025] Preparation method: (1) Add aluminum stearate to ethyl oleate, stir and heat (95-100°C) to prepare oil gel; (2) Dissolve SAIB in benzyl benzoate to prepare SAIB / benzene Benzyl formate solution; (3) Mix danofloxacin mesylate with SAIB / benzyl benzoate solution, grind it with a sand mill until the particle size of dafloxacin mesylate is less than 5 μm, and then mix it with oil gel, And adding an antioxidant, using a high-shear homogenizer under the condition of 15000-21000rpm for multiple times of homogenization, to prepare dafloxacin mesylate injection with a particle size of less than 5 μm.

Embodiment 2

[0026] Embodiment 2, preparation 15% dafloxacin mesylate injection

[0027] Preparation composition: dafloxacin mesylate 150g, SAIB 170g, aluminum stearate 11g, BHA 0.1g, BHT 0.2g, benzyl benzoate 300ml, IPM added to 1000ml.

[0028] Preparation method: (1) Add aluminum stearate to IPM, stir and heat (95-100°C) to prepare oil gel; (2) Dissolve SAIB in benzyl benzoate to prepare SAIB / benzyl benzoate solution; (3) mix danofloxacin mesylate with oil gelatin, pass through a colloid mill and grind until the particle size of dafloxacin mesylate is less than 20 μm, then mix it with SAIB / benzyl benzoate solution, and add antioxidant Dafloxacin mesylate injection was prepared by using a high-shear homogenizer under the condition of 15000-21000rpm for multiple times of homogenization and then passing through a sand mill.

Embodiment 3

[0029] Embodiment 3, preparation 20% dafloxacin mesylate injection

[0030] Preparation composition: Dafloxacin mesylate 200g, SAIB110g, HCO3g, Span-808g, BHA0.1g, BHT0.1g, PG0.05g, ethyl oleate added to 1000ml.

[0031] Preparation method: (1) Add HCO and Span-80 into ethyl oleate, stir and heat (80-90°C) to prepare HCO-containing colloidal liquid; (2) Dissolve SAIB in the colloidal liquid, Prepare HCO and SAIB / ethyl oleate solution; (3) Mix dafloxacin mesylate with about half the amount of HCO and SAIB / ethyl oleate solution, and grind it with a sand mill until dafloxacin mesylate The star particle size is less than 5 μm, then add antioxidant and the remaining solution, and use a high-shear homogenizer under the condition of 15000-21000 rpm for several times to obtain dafluxa mesylate with a particle size of less than 5 μm Star Injection.

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Abstract

The invention relates to an application of sucrose acetate iso-butyrate to preparation of an oil injection for livestock, and in particular relates to a method used for preparing a long-acting injection containing danofloxacin mesylate by combining sucrose acetate iso-butyrate and hydrogenated castor oil or aluminium stearate. A dispersion medium of the preparation is isopropyl myristate, benzyl benzoate, ethyl oleate or a mixture of more than one of isopropyl myristate, benzyl benzoate and ethyl oleate. The preparation has good sustained release effects, stable characters and good tissue compatibility and is easy to prepare.

Description

technical field [0001] The invention belongs to the preparation technology of veterinary drug preparations, and in particular relates to the combination of dafloxacin mesylate and a slow-release carrier to prepare a long-acting injection with slow-release effect. Background technique [0002] Dafloxacin mesylate is a special fluoroquinolone antibacterial drug for animals. It has a broad-spectrum bactericidal effect and can kill both Gram-negative bacteria and Gram-positive bacteria, mycoplasma and chlamydia. Currently commercially available products include oral preparations (soluble powders) and injections. The solvent of the injection is mainly water, and the concentration of the active ingredient is 1% or 2.5%. The preparation needs to be injected once a day, and a course of treatment needs to be administered continuously for 3-5 days. Therefore, the current commercially available injections have short drug effect maintenance time, many administration times, and due to t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/4709A61K47/44A61K47/26A61K47/12A61P31/04
Inventor 王玉万潘贞德戴晓曦任雅楠徐飞沈力
Owner 中农华威制药股份有限公司
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