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Sitafloxacin microcapsule preparation and preparation method thereof

A sitafloxacin and preparation technology, applied in the field of sitafloxacin microcapsule preparation and its preparation, can solve the problems of uneven particles, unstable dissolution, poor bitterness masking effect, etc., achieve stable disintegration and dissolution, and improve drug Compliance, the effect of improving drug safety

Inactive Publication Date: 2019-08-27
成都药云科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the above-mentioned defects of the prior art, the technical problem to be solved by the present invention is that the sitafloxacin preparations in the prior art have poor bitterness masking effect, uneven particles and unstable dissolution

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1, the preparation of sitafloxacin microcapsule tablet

[0043] The preparation raw materials include: 35g of sitafloxacin, 20g of gelatin, 25g of hydroxyethyl cellulose, 10g of croscarmellose sodium, 10g of microcrystalline cellulose, 10g of lactose, and 90g of 70% ethanol aqueous solution;

[0044] The process preparation method specifically includes:

[0045] Step 1, add the sitafloxacin of 35g in the fluidized bed, pass into air and make it suspend;

[0046] Step 2, mix 20g of gelatin, 25g of hydroxyethyl cellulose and 90g of 70% ethanol aqueous solution to obtain a capsule material solution, the capsule material solution is atomized and passed into a fluidized bed suspended with sitafloxacin, and the capsule material solution is passed into The conveying speed of fluidized bed is 50r / min, drying, crosses 800 mesh sieves and obtains sitafloxacin microcapsule core;

[0047] Step 3. Mix the sitafloxacin microcapsule core obtained in step 2 with 10 g of cr...

Embodiment 2

[0048] Embodiment 2, the preparation of sitafloxacin microcapsule capsule

[0049] The preparation raw materials include: 45g of sitafloxacin, 25g of polyvinyl alcohol, 30g of carboxymethylcellulose, 15g of low-substituted hydroxypropyl cellulose, 10g of starch, 5g of sucrose, and 100g of 70% ethanol aqueous solution;

[0050] The process preparation method specifically includes:

[0051] Step 1, add the sitafloxacin of 45g in the fluidized bed, pass into air and make it suspend;

[0052] Step 2, mix 25g of polyvinyl alcohol, 30g of carboxymethyl cellulose and 100g of 70% ethanol aqueous solution to obtain a capsule material solution, the capsule material solution is sprayed into a fluidized bed suspended with sitafloxacin, and the capsule material solution The conveying speed of passing into fluidized bed is 50r / min, dry, cross 800 mesh sieves and obtain sitafloxacin microcapsule core;

[0053] Step 3. Mix the sitafloxacin microcapsule core obtained in step 2 with 15 g of l...

Embodiment 3

[0054]Embodiment 3, preparation of sitafloxacin microcapsule granules

[0055] The preparation raw materials include: 40g of sitafloxacin, 50g of polyvinylpyrrolidone, 5g of copovidone, 10g of microcrystalline cellulose, and 100g of 70% ethanol aqueous solution;

[0056] The process preparation method specifically includes:

[0057] Step 1, add the sitafloxacin of 40g in the fluidized bed, pass into air and make it suspend;

[0058] Step 2. Mix 50 g of polyvinylpyrrolidone and 100 g of 70% ethanol aqueous solution to obtain a capsule material solution. The capsule material solution is atomized and passed into a fluidized bed suspended with sitafloxacin, and the capsule material solution is passed into the fluidized bed for transportation Speed ​​is 50r / min, dry, pass through 800 mesh sieves to obtain sitafloxacin microcapsule core;

[0059] Step 3. Mix the sitafloxacin microcapsule core obtained in step 2 with 5 g of copovidone and 10 g of microcrystalline cellulose, granula...

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PUM

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Abstract

The invention discloses a sitafloxacin microcapsule preparation. The Sitafloxacin microcapsule preparation comprises a microcapsule core and other auxiliary materials, wherein the microcapsule core isprepared from a main drug sitafloxacin and capsule wall materials. The invention further provides a technological preparation method and application of antisepsis and anti-inflammation of the sitafloxacin microcapsule preparation. According to the sitafloxacin microcapsule preparation disclosed by the invention, a better effect of covering bitter taste is realized, stable disintegration and dissolution of the main drug are facilitated, sitafloxacin medicine compliance is improved, and medication safety is improved; the technological method of the sitafloxacin microcapsule preparation disclosed by the invention is simple and convenient, easy to operate, and safe and environmentally friendly; the realization of industrialized application expanding is facilitated.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a sitafloxacin microcapsule preparation and a preparation method thereof. Background technique [0002] The chemical name of sitafloxacin (sitafloxacin hydrate) is 7-[(7S)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R , 2S)-cis-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid is a broad-spectrum quinolone developed by Daiichi Sankyo Co., Ltd. Antibacterial drugs for the treatment of severe and refractory infectious diseases. [0003] Currently, the dosage forms of sitafloxacin on the market include tablets, granules, and injections. The taste of sitafloxacin is extremely bitter, insoluble in alcohol, and insoluble in water. In the prior art, solid preparations use granules to prepare inclusion complexes of sitafloxacin to cover up its bitter taste, and increase the concentration of sitafloxacin by adding auxiliary materials. Di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4709A61K47/42A61K47/38A61K47/32A61P31/04A61P29/00
CPCA61K9/5026A61K9/5047A61K9/5057A61K31/4709A61P29/00A61P31/04
Inventor 穆云万家强
Owner 成都药云科技有限公司