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Norfloxacin D crystal form, and preparation method, preparation and application thereof

A technology of norfloxacin and crystal form, applied in the field of norfloxacin D crystal form and preparation thereof, and can solve problems such as unfavorable preparations

Inactive Publication Date: 2017-01-04
HANGZHOU XINBOSI BIOMEDICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the crystal form A is metastable and has strong hygroscopicity, which is not conducive to the next step of making corresponding preparations.

Method used

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  • Norfloxacin D crystal form, and preparation method, preparation and application thereof
  • Norfloxacin D crystal form, and preparation method, preparation and application thereof
  • Norfloxacin D crystal form, and preparation method, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: the preparation of norfloxacin D crystal form

[0025] Add 2 kg of ethanol, 5 kg of water, 150 g of glacial acetic acid, 1 g of disodium edetate, and 1 kg of norfloxacin into a 10 L three-neck flask. Heat to 70°C and stir for 0.5 hours. Filtrate while hot, adjust the filtrate to neutrality with ammonia water at 70°C, and continue stirring for 0.5h. The temperature was lowered to 10°C, a large amount of solids were precipitated, filtered, the filter cake was washed with water and dried at 105°C to obtain 0.91Kg of light yellow solid (yield: 91%), which was norfloxacin D crystal form. The X-ray powder diffraction pattern of norfloxacin D crystal form is as follows figure 1 As shown, the specific characterization is as follows:

[0026]

[0027] The chemical purity of obtained norfloxacin D crystal form detected by high performance liquid chromatography is measured to be 99.88% (see image 3 ), particle size distribution see Figure 4 . See Table 1 f...

Embodiment 2

[0034] Embodiment 2: Norfloxacin D crystal form prepares solid oral preparation

[0035] Take by weighing 200g of norfloxacin D crystal form, 52g microcrystalline cellulose, 2g hydroxypropyl cellulose, 12g croscarmellose sodium, 2g silicon dioxide, put in a multi-directional motion mixer and mix for 5min, then Add 2g of magnesium stearate and mix for 2 minutes; test the granule properties, start to compress the tablet after moisture determination, according to the theoretical tablet weight of 270mg, the hardness is 5-10kg, the difference of tablet weight is within ±5%, the total weight is 270g / 1000 tablets, the dissolution curve (compared with norfloxacin A crystal tablet prepared by the same method) see Figure 6 .

[0036] The crystal form D of norfloxacin provided by the invention has good stability and dissolution, and can be applied to the preparation of antibacterial drugs.

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Abstract

The invention discloses a new norfloxacin compound crystal form, and a preparation method, a preparation and application thereof. The new crystal form is named as a D crystal form; a diffraction angle 2 theta of an X-ray powder diffraction pattern of the norfloxacin D crystal form displays characteristic diffraction peaks at positions of 8.8+ / -0.2, 9.8+ / -0.2, 15.7+ / -0.2, 16.1+ / -0.2, 16.5+ / -0.2, 17.8+ / -0.2, 18.9+ / -0.2, 19.4+ / -0.2, 20.7+ / -0.2, and 21.0+ / -0.2. The norfloxacin D form provided by the invention has favorable dissolution rate and stability. The preparation method provided by the invention has the advantages of high operability, safety and environmental protection, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a D crystal form of norfloxacin and a preparation method, preparation and application thereof. Background technique [0002] Norfloxacin (Norfloxacin), chemical name 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid, alias Norfloxacin, its chemical structural formula is: [0003] [0004] Norfloxacin was developed by Kyorin Seiyaku Kabushiki Kaisha in 1978 and is currently on the market in about 60 countries. It is the third generation of quinolone antibiotics and is effective against Gram-positive and Gram-negative bacteria. Both have obvious inhibitory effects, and are mainly used to treat bacterial infections of the urinary system and gastrointestinal tract. Norfloxacin is widely used clinically because of its broad antibacterial spectrum, strong effect, low price and convenient administration. [0005] Norfloxacin has polymorph...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/56A61K31/496A61P31/04
CPCC07D215/56C07B2200/13
Inventor 陈德宝张佳红蔡盛丁建圣刘艳华朱伟英
Owner HANGZHOU XINBOSI BIOMEDICAL CO LTD
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