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Sitafloxacin hydrate granules and preparation method of sitafloxacin hydrate granules

A technology of sitafloxacin and granules, which is applied in the field of medicine, can solve the problems of low dissolution rate and low uniformity of drug granules, and achieve the effects of high dissolution rate, rapid dissolution and simple preparation process

Active Publication Date: 2016-06-15
JUMPCAN PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, although the inclusion compound can cover the bitter taste of sitafloxacin, it is prone to the problems of low uniformity of drug particles and low dissolution rate

Method used

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  • Sitafloxacin hydrate granules and preparation method of sitafloxacin hydrate granules
  • Sitafloxacin hydrate granules and preparation method of sitafloxacin hydrate granules
  • Sitafloxacin hydrate granules and preparation method of sitafloxacin hydrate granules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-4

[0023] The prescription of table 1 embodiment 1-4 (unit: g)

[0024]

[0025] Preparation Process:

[0026] According to the prescription amount, sitafloxacin was crushed through a 140 mesh sieve; mannitol was added to silicon dioxide and crushed through a 200 mesh sieve; aspartame was crushed through a 200 mesh sieve; the remaining pharmaceutical excipients were passed through a 140 mesh sieve; Promellose, vanillin essence and other pharmaceutical excipients are mixed evenly, then add sitafloxacin, mannitol, silicon dioxide mixture and mix evenly; spray 30% ethanol solution of hypromellose, granulate, Then add coating solution for coating, then spray 20% aqueous solution of vanillin essence, dry, granulate, sieve out the granules between 40-140 mesh, and pack.

[0027] The preparation method of the coating solution: take Eudragit L30D55 ​​in the formula amount, add 6ml of purified water, triethyl citrate, lactose, talcum powder, stir, and make the mixture evenly.

[0028...

Embodiment 5

[0037] The preparation of sitafloxacin granule composition: it comprises the following steps: (1) preparation concentration is the carrageenan solution of 5%: get carrageenan 10g, add 200m1 hot water and make dissolving, cool to room temperature, use 0.1mol / L Sodium hydroxide solution to adjust the pH to 5.5, for later use; weigh 105g of sitafloxacin, add carrageenan solution to make it wet and repeat the granulation in a swinging granulator, dry for 4 hours, and pulverize to make sitafloxacin Carrageenan granule; (2) preparation concentration is 5% sodium chloride solution 25ml, adjusts pH to be 8.5 with 0.1mol / L sodium hydroxide solution, for subsequent use; The sitafloxacin carrageenan granule in step (1) Add sodium chloride solution to make it wet and solidify, dry at 65°C for 4 hours, and prepare sitafloxacin inclusion complex; (3) Weigh 2kg sucrose, 200g starch, and 15g sodium carboxymethylcellulose, and mix them in a wet mixing method. Dry mix in the granulator for 500-...

Embodiment 6

[0039] The prescription of sitafloxacin granules is as follows:

[0040]

[0041] The coating prescription is as follows:

[0042]

[0043] Preparation Process:

[0044] According to the prescription quantity, each material is pulverized and passed through a mesh sieve, mixed uniformly, granulated, then added with a coating solution for coating, granulated, and packaged to obtain the product. The preparation method of the coating solution: take Eudragit L30D55 ​​in the formula amount, add purified water, plasticizer, porogen, and anti-sticking agent, stir, and mix evenly.

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Abstract

The invention relates to sitafloxacin hydrate granules. The formula comprises 10 parts of sitafloxacin hydrate, 50 to 100 parts of mannitol, 0.5 to 1 part of silicon dioxide, other pharmaceutically acceptable auxiliary materials and 15 to 30 parts of coating liquid. Compared with the prior art, the sitafloxacin hydrate granules produced by the invention effectively cover the bitter taste of the sitafloxacin hydrate, and have uniform granules and high dissolution rate. A mixing method of the materials in a preparation process of the sitafloxacin hydrate granules, provided by the invention, effectively prevents dust dispersion and static bonding, and the problem that screening is difficult is overcome; the flowability of the materials is improved and the mixing uniformity is improved; the preparation process is simple and is applicable to industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a sitafloxacin granule and a preparation method thereof. Background technique [0002] The chemical name of sitafloxacin (sitafloxacinhydrate) 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 antibacterial developed by Daiichi Sankyo Co., Ltd. It is a medicine with bactericidal effect and is used to treat severe and refractory infectious diseases. Sitafloxacin can inhibit bacterial DNA gyrase and topoisomerase IV, and its inhibitory effect on these two enzymes is stronger than that of other quinolones. In addition, sitafloxacin also showed a strong inhibitory effect on enzymes of quinolone-resistant bacteria. Because the structure contains a cis-fluorocyclopropylamine group, it has good pharmacokinetic properties and can reduce adverse reac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/26A61K47/02A61K31/4709A61P31/04
CPCA61K9/1611A61K9/1623A61K31/4709
Inventor 曹龙祥董自波牛犇邵建国李萍杭夏清
Owner JUMPCAN PHARMA GRP
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