Sitafloxacin fine granule and preparation process thereof

A technology of sitafloxacin and sitafloxacin hydrate, which is applied in the field of medicine, can solve the problems of poor dispersion of sitafloxacin particles, large particle size distribution and poor uniformity of sitafloxacin fine particles, and achieve Good dissolution effect, low cost and short production cycle

Pending Publication Date: 2021-06-08
JUMPCAN PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Control the particle size of raw materials, intermediates and finished products in the process of pretreatment, granulation and coating of sitafloxacin fine granule raw materials, effectively solving the problem of large and uniform particle size distribution of sitafloxacin fine granule Improve the coating effect, improve the permeability of the preparation, improve the bioavailability, and improve the absorption capacity of the drug in the body;
[0010] Through the control of parameters such as isolation weight gain, coating weight gain, hydroxypropyl cellulose and corn starch dosage, the quality of intermediates and finished granules was significantly improved, and the problem of excessive disintegration and sticking of sitafloxacin granules was effectively solved. Problems such as agglomeration and poor dispersibility, improve the dissolution effect of the drug, and improve the stability of the drug

Method used

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  • Sitafloxacin fine granule and preparation process thereof
  • Sitafloxacin fine granule and preparation process thereof
  • Sitafloxacin fine granule and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1 preparation method is:

[0055] (1) Pre-treatment of raw and auxiliary materials: manually pass sitafloxacin hydrate through a 200-mesh sieve, mannitol through a 80-mesh sieve, and microcrystalline cellulose through a 80-mesh sieve after crushing.

[0056] (2) Mixing: Weigh and sieve sitafloxacin hydrate, microcrystalline cellulose, mannitol, and cornstarch according to the prescription amount, pass through a No. 2 pharmacopoeia sieve and mix.

[0057] (3) Preparation of binder solution: Take the calculated hydroxypropyl cellulose HPC-L and add it into a beaker and add purified water to dissolve it.

[0058] (4) Granulation: Put the mixture of raw and auxiliary materials in the top spraying device of the fluidized bed, premix and preheat, and then spray the binder solution. After the granulation is finished, dry, start to detect the moisture after 3 minutes of drying, and then take samples every 5 minutes to measure the moisture content of the granules. Wh...

Embodiment 2-9

[0071] In order to improve the problems existing in the preparation of granules in Example 1, the experiment at this stage changed the formulation of the coating solution, reduced the amount of hydroxypropyl cellulose in the prescription, and investigated the differences in the properties of the finished product under different isolation and coating weight gain conditions.

[0072] The fluidity of the particle inner core becomes better after isolation, the particle size decreases slightly at 2.5% of the isolation weight gain, the particle size distribution tends to be concentrated, and the fluidity increases significantly; the particle size of the 5% isolation weight gain increases significantly, and the degree of particle size concentration is almost unchanged. Liquidity is significantly improved. At 2.5% isolation weight gain, the particle size after coating did not change much, the particle size distribution tended to be dispersed, and the fluidity increased slightly; at 5% ...

Embodiment 10-11

[0089] In Examples 10 and 11, the purpose of inhibiting the disintegration speed of self-made granules was achieved by increasing the amount of hydroxypropyl cellulose and reducing the amount of corn starch. Dissolution test results ( Figure 4) shows that the amount of corn starch formulation has a certain impact on the dissolution curve. After reducing the amount of corn starch formulation, the dissolution rate of the granules of Example 11 in the pH5.0 medium is significantly lower than that of the granules of Example 10, and the dissolution rate at the end point is also significantly reduced. The expected result is consistent with the formulation of the action plan in the pH5.0 medium, that is, the slower disintegration is not conducive to the dissolution of sitafloxacin API in high solubility medium.

[0090] A kind of formula of sitafloxacin fine granule embodiment 10-11 of table 6

[0091]

[0092]

[0093] 2. Detection test and effect

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Abstract

The invention discloses a sitafloxacin fine granule and a preparation process thereof. By adjusting the dosage and component proportion of an isolation layer and a coating in the granulation process, the problems of too fast disintegration, caking and poor dispersibility easily caused by a large variety of auxiliary materials and large prescription dosage in the preparation process of the sitafloxacin fine granule can be effectively solved, and the obtained finished product is narrow in particle size distribution, uniform in mixing and good in dissolution effect. The auxiliary materials are cheap and easy to obtain, the preparation is easy, no special equipment is needed, the production cycle is short, the cost is low, and the fine granule is very suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and mainly relates to a preparation method of sitafloxacin fine granule. Background technique [0002] Sitafloxacin (DU-6859a) is a broad-spectrum quinolone antibacterial drug developed by Daiichi Sankyo, Japan, with a chemical name of 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. [0003] Studies have shown that sitafloxacin has broad-spectrum antibacterial activity against many clinical isolates of Gram-positive bacteria, Gram-negative bacteria and anaerobic bacteria, including fluoroquinolone-resistant strains, and also has antibacterial activity against many common clinical fluoroquinolone-resistant strains. Good bactericidal effect. And sitafloxacin was less likely to develop resistance mutations during treatment than other fluoroquinolones. [0004] Patent Nos. CN102988298A and CN10566305...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/38A61K47/32A61K47/36A61K47/26A61K47/20A61K31/4709A61P31/04
CPCA61K9/5047A61K9/5026A61K9/5015A61K9/5073A61K47/36A61K31/4709A61P31/04
Inventor 曹龙祥韦明元许斌万华斌蔡虎
Owner JUMPCAN PHARMA GRP
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