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Marbofloxacin micro-capsule and preparation method thereof

The technology of mabrofloxacin and solution is applied in the field of mabrofloxacin microcapsules and its preparation, which can solve the problems of low solubility, restrict the development and application of mabrofloxacin preparations, etc. light-sensitive effect

Active Publication Date: 2015-06-17
XINCHANG GUOBANG CHEM IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the solubility of Mabofloxacin is extremely special, its state is solid, and the solubility of Mabofloxacin in oil is low
Restricting the development and application of marbofloxacin preparations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Starch Sodium Octenylsuccinate 40%

[0023] Mabofloxacin 60%

[0024] Preparation:

[0025] Dissolve starch sodium octenyl succinate in purified water to prepare a wall material solution with a concentration of 10%. Dissolve Mabofloxacin in a mixed solution of dichloromethane / absolute ethanol (9:1 ratio) to prepare a core material solution with a concentration of 20%. At a shear rate of 5000r / min, slowly drop the core material solution into the wall material solution, and at the same time carry out vacuum distillation to recover the mixed solution of dichloromethane / absolute ethanol. The system temperature is 10°C and the vacuum degree is 0.07Mpa. The time was 2 hours, and the distillation under reduced pressure was continued for 2 hours after the dropwise addition was completed. The emulsion is spray-dried, the inlet air temperature is 180°C, and the outlet air temperature is 80°C.

[0026] The appearance of the obtained powder oil is light yellow, good fluidity, a...

Embodiment 2

[0028] Starch Sodium Octenyl Succinate 90%

[0029] Mabofloxacin 10%

[0030] Preparation:

[0031] Dissolve starch sodium octenyl succinate in purified water to prepare a wall material solution with a concentration of 30%. Dissolve Mabofloxacin in a mixed solution of dichloromethane / absolute ethanol (3:2) to prepare a core material solution with a concentration of 50%. At a shear rate of 10000r / min, slowly drop the core material solution into the wall material solution, and carry out vacuum distillation at the same time to recover the dichloromethane / absolute ethanol mixed solution. The system temperature is 40°C and the vacuum degree is 0.01Mpa. The time was 0.5 hour, and the vacuum distillation was continued for 2 hours after the dropwise addition was completed. The emulsion is spray-dried, the inlet air temperature is 220°C, and the outlet air temperature is 120°C.

[0032] The appearance of the obtained powder oil is light yellow, good fluidity, and dissolves in water...

Embodiment 3

[0034] Starch Sodium Octenylsuccinate 70%

[0035] Mabofloxacin 30%

[0036] Preparation:

[0037] Dissolve starch sodium octenyl succinate in purified water to prepare a wall material solution with a concentration of 20%. Dissolve Mabofloxacin in a mixed solution of dichloromethane / absolute ethanol (19:3) to prepare a core material solution with a concentration of 35%. At a shear rate of 7500r / min, slowly drop the core material solution into the wall material solution, and at the same time carry out vacuum distillation to recover the mixed solution of dichloromethane / absolute ethanol. The system temperature is 25°C and the vacuum degree is 0.04Mpa. The time was 1.25 hours, and the distillation under reduced pressure was continued for 2 hours after the dropwise addition was completed. The emulsion is spray-dried, the inlet air temperature is 200°C, and the outlet air temperature is 100°C.

[0038] The appearance of the obtained powder oil is light yellow, good fluidity, an...

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PUM

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Abstract

The invention relates to a marbofloxacin micro-capsule and a preparation method of the marbofloxacin micro-capsule. The preparation method comprises the following steps: (1) preparing a wall material solution, (2) preparing a core material solution, (3) carrying out emulsification and reduced pressure distillation: slowly dropwise adding the core material solution prepared in Step (2) into the wall material solution prepared in Step (1) under a high-speed shearing condition, carrying out the reduced pressure distillation at the same time, recovering a dichloromethane / absolute ethyl alcohol mixed solution, and continuing the reduced pressure distillation after dropwise adding, and (4) carrying out spray drying, wherein the system temperature is 10-40 DEG C; a vacuum degree is 0.01-0.07Mpa; the dropwise adding time is 0.5-2h; and the shearing speed is 5000-10000 r / min. The sensitivity of marbofloxacin to light can be reduced; the drug efficacy is prolonged; an unpleasant odor is covered; the solubility is improved; in addition, various preparations, such as powder, a tablet, a capsule and controlled-release agent can be prepared very conveniently; and animal administration is facilitated.

Description

technical field [0001] The invention relates to a marbofloxacin microcapsule and a preparation method thereof, belonging to the field of veterinary drug preparations. Background technique [0002] Mabofloxacin is another third-generation quinolone antibacterial drug for animals after enrofloxacin, dafloxacin, sarafloxacin, and difloxacin. It is mainly antibacterial by inhibiting the activity of bacterial topoisomerase. Mabaofloxacin was first created by Roche in Switzerland and further developed by Vetoquinol. It was first listed in the UK in 1995, and then in France, the United States and Europe. Mabaofloxacin has a wide antibacterial spectrum and strong bactericidal power. It has strong activity against Gram-negative and positive bacteria, and is even effective against some molds and anaerobic bacteria. Strong tissue penetration, rapid and complete absorption in the body and wide distribution, long elimination half-life, bioavailability close to 100%; wide range of safe ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/5395A61K47/36A61P31/04
Inventor 姜应新侯仲轲郑立斌邱家军
Owner XINCHANG GUOBANG CHEM IND
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