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Norfloxacin and vanillin eutectic and preparation method thereof

A technology of norfloxacin and vanillin, which is applied in the field of new norfloxacin co-crystal and its preparation, and can solve problems such as limited application

Inactive Publication Date: 2017-08-25
ZHEJIANG UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The formation of co-crystals with isonicotinamide uses chloroform as a solvent, and there is a molecule of chloroform in the co-crystal species, which limits its application in medicine

Method used

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  • Norfloxacin and vanillin eutectic and preparation method thereof
  • Norfloxacin and vanillin eutectic and preparation method thereof
  • Norfloxacin and vanillin eutectic and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment 1

[0024] Add 104g of deionized water into a 250ml three-neck flask, slowly add 348mg of norfloxacin and 166mg of vanillin, raise the temperature to 100°C, dissolve the norfloxacin and vanillin, filter the reaction solution quickly after dissolution, and place the filtrate in a 250ml beaker , naturally cooled, placed for 24 hours, crystals were precipitated, filtered, and dried to obtain 502 mg of needle-shaped white crystals, that is, norfloxacin and vanillin eutectic. Record the solubility of norfloxacin, norfloxacin and vanillin eutectic at 25 ℃ of pure water species as shown in table 1, as can be seen from the table, eutectic of the present invention compares with norfloxacin, greatly improves The solubility in water is improved, and the bioavailability is greatly improved; and it is also beneficial to the processing operation of the subsequent pharmaceutical process.

[0025] Table 1 Solubility of norfloxacin, norfloxacin and vanillin eutectic in pure water at 25°C

[0026]...

specific Embodiment 2

[0028] Add 174g of deionized water to a 250ml three-necked flask, slowly add 348mg of norfloxacin and 166mg of vanillin, raise the temperature to 90°C, dissolve the norfloxacin and vanillin, filter the reaction solution quickly after dissolution, and place the filtrate in a 250ml beaker , naturally cooled, placed for 24 hours, crystals were precipitated, filtered, and dried to obtain 502 mg of needle-shaped white crystals, that is, norfloxacin and vanillin eutectic. The measured solubility in eutectic water is shown in Table 2.

[0029] Table 2 Solubility of norfloxacin, norfloxacin and vanillin eutectic in pure water at 25°C

[0030] compound Solubility (mg / mL) Norfloxacin 0.28 Co-crystal of norfloxacin and vanillin 27.9

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Abstract

The invention belongs to the technical field of organic drug eutectic and specifically relates to a norfloxacin and vanillin eutectic and a preparation method thereof. In the norfloxacin and vanillin eutectic provided by the invention, norfloxacin active ingredient is used as a drug active ingredient API, vanillin is used as an eutectic forming material and a series of characteristic peaks exist in a XRD graph 2 theta within the scope of 6.780, 7.760, 9.440, 10.380, 11.757, 13.899, 15.280, 17.100, 18.559, 20.620, 22.381, 23.018, 24.420, 25.080, 27.657 and 30.320. The preparation method for the eutectic comprises the following steps: dissolving norfloxacin and vanillin in water at 90-100 DEG C, wherein the mole ratio of norfloxacin to vanillin is 1:1 and the mass ratio of norfloxacin to water is 1:(300-500); filtering the reaction solution and cooling the filtrate after dissolving; separating out the crystal; filtering and drying, thereby acquiring the crystal, namely, the norfloxacin and vanillin eutectic. The invention provides the possibility of further widening the solid form of norfloxacin, modifying the physical and chemical properties of the drug, increasing the solubility in water and promoting the pesticide effect and the bioavailability.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a novel norfloxacin co-crystal and a preparation method thereof. Background technique [0002] "Drug co-crystal" is a pharmaceutical active ingredient (API) and a physiologically acceptable ligand (CCF) through molecular recognition, without destroying the API's own chemical bonds, through intermolecular forces (hydrogen bonds, halogen bonds, π stacking and van der Waals forces) to form specific crystal structures. The drug co-crystal based on crystal engineering is essentially a supramolecular self-assembly system, which is the result of the balance of thermodynamics, kinetics, and molecular recognition. For pharmaceutical active ingredients, its crystalline form can affect many of its physical and chemical properties, such as melting point, solubility, stability, bioavailability, etc. Since the formation of pharmaceutical co-crystals will not destroy the ...

Claims

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Application Information

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IPC IPC(8): C07D215/56C07C45/81C07C47/58
CPCC07B2200/13C07C45/81C07C47/58C07D215/56
Inventor 蒋成君傅方杰
Owner ZHEJIANG UNIVERSITY OF SCIENCE AND TECHNOLOGY
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