A kind of sustained-release sarafloxacin hydrochloride microcapsule and preparation method thereof

A technology of salafloxacin hydrochloride and microcapsules is applied in the directions of microcapsules, capsule delivery, pharmaceutical formulations, etc., and achieves the effects of simple preparation method, good palatability and low cost

Active Publication Date: 2017-11-03
山西沃德华兽生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to solve the problems existing in the existing oral powder of sarafloxacin hydrochloride, and provide a kind of intestine-targeted slow-release sarafloxacin hydrochloride microcapsules to improve its palatability and curative effect

Method used

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  • A kind of sustained-release sarafloxacin hydrochloride microcapsule and preparation method thereof
  • A kind of sustained-release sarafloxacin hydrochloride microcapsule and preparation method thereof
  • A kind of sustained-release sarafloxacin hydrochloride microcapsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Add 40Kg of sarafloxacin hydrochloride to a 500L reactor, then add 400Kg of purified water and 5Kg of Span-80, and stir vigorously for 1 to 2 hours; keep stirring, add 8Kg of methyl methacrylate and 1Kg of allyl methacrylate in sequence Esters, 1Kg acrylic acid, and 0.1Kg benzoyl peroxide, heated up to 78°C for 3-4 hours, cooled the reaction product to room temperature, filtered, washed with water, and dried to obtain intestinal-targeted sustained-release sarafloxacin hydrochloride Microcapsule finished product.

[0027] Take two portions of sarafloxacin hydrochloride microcapsule powder prepared above, each 0.100g, and put them into 100mL HCl solution simulated gastric juice (pH=1.20) and phosphate buffer solution simulated intestinal juice (pH=7.45) respectively, at (37±1 ) °C, stirred and released at a speed of 100 rpm for 3 hours, during which time 1mL solution was drawn from it at regular intervals, and the volume was fixed to 100mL with 0.1mol / L NaOH solution, and...

Embodiment 2

[0030] Add 50Kg of sarafloxacin hydrochloride to a 500L reaction kettle, then add 250Kg of purified water, 0.25Kg of Span-80, and stir vigorously for 1 to 2 hours; keep stirring, add 6Kg of methyl methacrylate, 1.3Kg of methacrylic acid in sequence Allyl ester, 1.5Kg acrylic acid, and 0.05Kg benzoyl peroxide, heated up to 78°C for 3-4 hours, cooled the reaction product to room temperature, filtered, washed with water, and dried to obtain intestinal-targeted slow-release hydrochloric acid The finished product of sarafloxacin microcapsules.

Embodiment 3

[0032] Add 30Kg sarafloxacin hydrochloride to a 500L reactor, then add 300Kg purified water, 10Kg Span-80, and stir vigorously for 1 to 2 hours; keep stirring, add 9Kg methyl methacrylate, 3Kg allyl methacrylate in turn Esters, 3Kg acrylic acid, and 0.3Kg benzoyl peroxide, heated up to 78°C for 3-4 hours, cooled the reaction product to room temperature, filtered, washed with water, and dried to obtain intestinal-targeted sustained-release sarafloxacin hydrochloride Microcapsule finished product.

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Abstract

The invention discloses a slow-release type sarafloxacin hydrochloride microcapsule. The slow-release type sarafloxacin hydrochloride microcapsule consists of a microcapsule core and a microcapsule wall wrapped at the outer part of the microcapsule core, wherein the component of the microcapsule core is sarafloxacin hydrochloride accounting for 50-90% of the total mass of the microcapsule, the microcapsule wall accounts for 10-50% of the total mass of the microcapsule, and is a copolymer polymerized by the following materials in percent by mass under the existence of an initiator: 60-95% of alkyl methacrylate / aryl ester, 0-20% of allyl ester crosslinking agent and 5-20% of acrylic acid / methacrylic acid. The slow-release type sarafloxacin hydrochloride microcapsule disclosed by the invention is good in fluidity, is beneficially mixed with feed, can cover abnormal taste of medicines, has better palatability, and can increase the feed intake of livestock and poultry; the capsulated sarafloxacin hydrochloride is good in stability, the release speed in the stomach and the intestine can be reduced after oral administration, the long-lasting action of the medicine effect can be maintained and the stability and the bioavailability of the medicines are effectively improved.

Description

technical field [0001] The invention belongs to the technical field of veterinary pharmaceutical preparations, and relates to an antibacterial drug sarafloxacin hydrochloride for livestock and poultry, in particular to a sustained-release sarafloxacin hydrochloride preparation targeting the intestinal tract, and a preparation method of the preparation. technical background [0002] Sarafloxacin hydrochloride is a quinolone antibacterial drug, which has a broad antibacterial spectrum, strong antibacterial effect, and has a long post-antibacterial effect, and has a strong killing effect on bacteria in the stationary phase and growth phase. Sarafloxacin is sensitive to Escherichia coli, Salmonella, Klebsiella, Haemophilus, etc., and its in vitro antibacterial activity against most aerobic Gram-negative bacteria, including a variety of Enterobacteriaceae and Pseudomonas aeruginosa Star 2 times, the activity of gram-positive bacteria such as streptococcus and staphylococcus is 2 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/496A61K47/32A61P31/04
Inventor 杨宏伟粱占学张松王勇
Owner 山西沃德华兽生物技术有限公司
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