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Sparfloxacin hemisulphate, its preparation method and application

A technology of hemisulfate and sparfloxacin, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, antibacterial drugs, etc., can solve the problems of changing drug bioavailability and curative effect, affecting drug absorption, etc., and achieve significant Economic and social benefits, simple preparation process, and easy handling

Inactive Publication Date: 2012-03-07
FUJIAN AGRI & FORESTRY UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing literature shows that the amorphous state and crystalline state of the drug can affect the absorption of the drug, and may also change the bioavailability and efficacy of the drug

Method used

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  • Sparfloxacin hemisulphate, its preparation method and application
  • Sparfloxacin hemisulphate, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Add 1 g of sparfloxacin lactate and 0.18 g of vanadyl sulfate to 50 ml of distilled water, and heat it to reflux. After refluxing for 6 hours, filter, and add 20 ml of methanol to the filtrate to volatilize to obtain a sparfloxacin sample. With the following powder X-ray diffraction pattern table (see figure 1 ) characterization, X-ray diffraction Bragg angle 2θ is about: 5.6±0.2, 9.0±0.2, 11.4±0.2, 16.9±0.2, 19.7±0.2, 21.3±0.2, 22.0±0.2, 22.9±0.2, 23.7±0.2, 24.8± 0.2, 25.8±0.2, 27.5±0.2, 28.6±0.2, 29.1±0.2, 30.3±0.2, 40.5±0.2, 42.6±0.2, 43.7±0.2, 46.0±0.2.

Embodiment 2

[0024] 0.2 g of sparfloxacin lactate and 0.036 g of vanadyl sulfate were added to 15 ml of distilled water, which was heated to reflux. After reflux for 4 hours, filter, and add 5 ml of methanol to the filtrate to volatilize to obtain a sparfloxacin sample.

Embodiment 3

[0026] 0.1 g of sparfloxacin lactate and 0.016 g of vanadyl sulfate were added to 15 ml of distilled water, which was heated to reflux. After refluxing for 8 hours, filter, and add 5 ml of ethanol to the filtrate to volatilize to obtain a sparfloxacin sample.

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Abstract

The invention discloses Sparfloxacin hemisulphate, its preparation method and application. Characterized by clear crystal form, good stability, easy treatment during medicament processing and simple preparation technology, the Sparfloxacin hemisulphate provided in the invention has substantial economic and social benefits.

Description

technical field [0001] The invention belongs to the field of crystallization technology, in particular to a sparfloxacin hemisulfate and its preparation method and application. Background technique [0002] Sparfloxacin is a kind of quinolone antibacterial drugs, and its mechanism of action is to inhibit the DNA gyrase in the process of bacterial DNA synthesis to play a bactericidal effect. It not only has good antibacterial effect on Gram-positive bacteria and Gram-negative bacteria, but also has good antibacterial effect on Mycoplasma, Chlamydia, Legionella, anaerobic bacteria including Bacteroides fragilis and Mycobacterium. Due to its good antibacterial effect, its tablets and capsules have been widely used at home and abroad. However, since sparfloxacin itself is insoluble in water, it is difficult to formulate water-soluble preparations, so one of the methods to improve its efficacy is to make it into an aqueous solution of sparfloxacin salt. As described in EP 322,8...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/496A61P31/04
Inventor 李涛
Owner FUJIAN AGRI & FORESTRY UNIV
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