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Enoxacin-phthalic acid drug salt monocrystal and preparation method thereof

A technology of phthalic acid and enoxacin, which is applied in the field of enoxacin pharmaceutical salt single crystal, can solve the problems of affecting the exertion of drug efficacy and clinical application, unsatisfactory uniformity and stability, low bioavailability and the like, Achieve significant clinical application value, avoid deterioration or mildew, and improve solubility

Inactive Publication Date: 2019-01-15
JIAMUSI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of enoxacin itself, when it enters the human body, the dissolution rate is slow, resulting in low bioavailability in the body, which affects its drug efficacy and clinical application.
At present, the water solubility of enoxacin is mainly improved by inclusion, microemulsion, solid dispersion, liposome preparation or making nanoparticles, but the uniformity and stability are not ideal

Method used

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  • Enoxacin-phthalic acid drug salt monocrystal and preparation method thereof
  • Enoxacin-phthalic acid drug salt monocrystal and preparation method thereof
  • Enoxacin-phthalic acid drug salt monocrystal and preparation method thereof

Examples

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Effect test

Embodiment 1

[0026] A preparation method of the enoxacin-phthalic acid drug salt single crystal, enoxacin 0.05mmol and phthalic acid 0.15mmol are placed together in a glass container at a molar ratio of 1:3, and then jointly Dissolve in a mixed solution of water (5mL) and methanol (5mL), place the glass container containing the mixed solution on a heating stirrer, and stir in a constant temperature water bath at 45°C for 3 hours. After fully reacting, dry Slowly volatilize under the environment, and after 1-30 days, a colorless block crystal is formed, which is the single crystal of enoxacin-phthalic acid drug salt.

Embodiment 2

[0028] A preparation method of the enoxacin-phthalic acid pharmaceutical salt single crystal, enoxacin 0.1mmol and phthalic acid 0.3mmol are placed together in a glass container at a molar ratio of 1:3, and then jointly Dissolve in a mixed solution of ethanol (7mL) and water (3mL), place the glass container containing the mixed solution on a heating stirrer, and stir in a constant temperature water bath at 40°C for 3.5 hours. After fully reacting, dry Slowly volatilize under the environment, and after 1-30 days, a colorless block crystal is formed, which is the single crystal of enoxacin-phthalic acid drug salt.

Embodiment 3

[0030] A preparation method of the enoxacin-phthalic acid drug salt single crystal, enoxacin 0.05mmol and phthalic acid 0.15mmol are placed together in a glass container at a molar ratio of 1:3, and then jointly Dissolve in a mixed solution of ethanol (9mL) and water (1mL), place the glass container containing the mixed solution on a heating stirrer, and stir in a constant temperature water bath at 45°C for 3 hours. After fully reacting, dry Slowly volatilize under the environment, and after 1-30 days, a colorless block crystal is formed, which is the single crystal of enoxacin-phthalic acid drug salt.

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Abstract

The invention provides a preparation method for an enoxacin drug salt monocrystal and specifically relates to an enoxacin-phthalic acid drug salt monocrystal and a preparation method thereof. The prepared enoxacin-phthalic acid drug salt monocrystal has a chemical formula of C15H18FN4O3.C8H5O4; the monocrystal belongs to a triclinic system; the space group of the monocrystal is P1; a is equal to 7.7908(6) angstroms; b is equal to 9.1689(8) angstroms; c is equal to 17.0756(11) angstroms; alpha is equal to 105.136(7) degrees; beta is equal to 90.283(6) degrees; gamma is equal to 108.962(7) degrees; V is equal to 1108.15(16) angstroms<3>; and Z is equal to 2. The enoxacin-phthalic acid drug salt monocrystal prepared in the invention can effectively improve the solubility and hygroscopic stability of enoxacin and enhance the capability of enoxacin in inhibiting Staphylococcus aureus, Staphylococcus albus and Escherichia coli while maintaining the original medicinal activity of enoxacin unchanged, and has significant academic research significance and clinical application value.

Description

technical field [0001] The invention provides an enoxacin drug salt single crystal, in particular to an enoxacin-phthalic acid drug salt single crystal and a preparation method thereof. Background technique [0002] Enoxacin (Enoxacin, EX), C 15 h 17 FN 4 o 3 , its chemical structure is as follows: [0003] [0004] Enoxacin (Ex), also known as fluoxacin, is a commonly used third-generation fluoroquinolone antibiotic with broad-spectrum antibacterial effects and no cross-resistance with other antibacterial drugs. It is mainly used clinically to treat Infections caused by Gram-negative bacteria and positive bacteria, such as the treatment of infectious diseases such as urinary tract, intestinal tract, respiratory tract and ENT. However, due to the poor water solubility of enoxacin itself, when it enters the human body, its dissolution rate is slow, resulting in low bioavailability in vivo, which affects its drug efficacy and clinical application. At present, the wate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04C07C63/20C07C51/41
CPCC07B2200/13C07C51/412C07C63/20C07D471/04
Inventor 刘立新邹冬玉张羽男
Owner JIAMUSI UNIVERSITY
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