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Sitafloxacin tablet and preparation method thereof

A sitafloxacin and tablet technology, applied in the pharmaceutical field, can solve the problems of cumbersome preparation process, low dissolution rate of active ingredients in tablets, and it takes more than 2 hours to achieve good without interference, and achieves good dissolution rate. , The effect of reducing the time of crystallization and purification

Active Publication Date: 2021-07-30
CHINA MEHECO SANYANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its purpose is to provide a sitafloxacin tablet that does not need to add an opacifying agent but is stable to light and has a relatively ideal release rate and its preparation process. Although the present invention solves the problem, the preparation process is cumbersome
[0005] In the prior art, in order to improve the quality of the drug, the crude sitafloxacin is usually pretreated, that is, crystallized and purified. The steps are to add alkali solution to form a salt, activate carbon to decolorize and filter, and add an organic solvent to remove the organic compound. Phase, add acid to crystallize, but if you do not interfere with the crystallization after adding acid, it will take more than 2 hours to achieve a good yield
[0006] In addition, due to the insoluble characteristics of sitafloxacin in water, if it is not treated, it will cause the problem of low dissolution rate of the active ingredients of the tablet. One of the ways to deal with this problem is to combine sitafloxacin powder with hydrophilic Joint research of excipients, but the amount of hydrophilic excipients used in joint research in the prior art is generally at least ten times that of sitafloxacin powder

Method used

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  • Sitafloxacin tablet and preparation method thereof

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preparation example Construction

[0025] The present invention provides a kind of preparation method of sitafloxacin tablet, it is characterized in that, comprises the steps:

[0026] S1 Add 30-40g of sitafloxacin crude product into 500ml of water, add it into 0.1mol / L sodium hydroxide solution at a constant speed and stir until the precipitate is completely dissolved;

[0027] S2 decolorizes and filters the solution with activated carbon to remove physical impurities, and collects the filtrate;

[0028] S3 Add a mixture of 100ml ethanol and 100-400ml acetone to the filtrate and stir to remove the organic phase, then add 0.1mol / L hydrochloric acid solution to adjust the pH to 6.5-7, stir and crystallize for 45 minutes, add 0.5- 1g of iron oxide powder; the method of adding iron oxide powder is to add in three equal amounts, and the adding time points are 0, 15, and 30 minutes respectively.

[0029] S4 collects the precipitate by filtration and rinses the precipitate with ethanol, and obtains powder A after dr...

Embodiment 1

[0034] Preparation:

[0035] S1 Add 30g of sitafloxacin crude product into 500ml of water, add it into 0.1mol / L sodium hydroxide solution at a constant speed and stir until the precipitate is completely dissolved;

[0036] S2 decolorizes and filters the solution with activated carbon to remove physical impurities, and collects the filtrate;

[0037] S3 adds the mixed solution that 100ml ethanol and 350ml acetone forms in the filtrate and removes the organic phase after stirring, then adds 0.1mol / L hydrochloric acid solution to adjust pH7, stirs and crystallizes for 45 minutes, adds 0.8g iron oxide powder in the stirring process; Iron oxide The method of adding the powder is to add in three equal amounts, and the adding time points are respectively 0, 15, and 30 minutes.

[0038] S4 collects the precipitate by filtration and rinses the precipitate with ethanol, and obtains powder A after drying;

[0039] S5 Add mannitol into the grinder and add powder A step by step in equal ...

Embodiment 2

[0042] Preparation:

[0043] S1 Add 40 g of sitafloxacin crude product into 500 ml of water, add it into 0.1 mol / L sodium hydroxide solution at a constant speed and stir until the precipitate is completely dissolved;

[0044] S2 decolorizes and filters the solution with activated carbon to remove physical impurities, and collects the filtrate;

[0045] S3 Add a mixed solution of 100ml ethanol and 100ml acetone to the filtrate and stir to remove the organic phase, then add 0.1mol / L hydrochloric acid solution to adjust pH6.5, stir and crystallize for 45 minutes, add 1g iron oxide powder during stirring; The method of adding the iron powder is to add in three equal amounts, and the adding time points are 0, 15, and 30 minutes respectively.

[0046] S4 collects the precipitate by filtration and rinses the precipitate with ethanol, and obtains powder A after drying;

[0047] S5 Add mannitol into the grinder and add powder A step by step in equal amounts for co-grinding until the ...

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Abstract

The invention relates to a sitafloxacin tablet and a preparation method thereof. Common opacifying agent ferric oxide is added in the crystallization and purification process of a crude product of the sitafloxacin tablet, so the purification time of the sitafloxacin tablet can be effectively shortened, and the effect of the ferric oxide serving as the opacifying agent is not influenced; moreover, the refined sitafloxacin powder is added step by step and is ground together with one to two times of mannitol, so the finally formed tablet has good dissolution rate under the condition of using a small amount of mannitol, and meanwhile, the taste of the tablet can be adjusted through the mannitol, so that the compliance of a patient is improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a sitafloxacin tablet and a preparation method thereof. Background technique [0002] Sitafloxacin hydrate is a broad-spectrum quinolone antibacterial drug developed by Daiichi Sankyo, and its monohydrate is clinically used for the treatment of severe and refractory infectious diseases. [0003] Sitafloxacin tastes bitter and is insoluble in water. Therefore, direct wet or dry granulation will lead to very unsatisfactory dissolution rate of active ingredients in solid preparations, and the extremely bitterness will lead to poor patient compliance. [0004] Application number 201310013310.2 discloses a sitafloxacin tablet and its preparation method, that is, sitafloxacin or its pharmaceutically acceptable salt and pellet excipients are made of soft material with ethanol aqueous solution and then extruded and spheronized to prepare drug-containing pellets , and then add the prepa...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4709A61K47/02A61K47/26A61P31/04
CPCA61K9/2018A61K9/2009A61K31/4709A61P31/04
Inventor 李宏仁朱峰刘超陈晞符惠金李隆财吴英璨简梧桐
Owner CHINA MEHECO SANYANG PHARMA CO LTD
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