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Fenbufen pharmaceutical co-crystal and preparation method thereof

A technology of drug and drug activity, which is applied in the field of fenbufen drug co-crystal and its preparation, can solve the problems of decreased solubility and achieve the effects of low cost, improved solubility and bioavailability, and improved oral absorption rate

Pending Publication Date: 2022-05-06
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although drug co-crystals have obvious advantages in improving the solubility of drugs, it is not that the solubility of drugs will be improved after forming co-crystals, and the solubility of some drugs will decrease after forming co-crystals.

Method used

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  • Fenbufen pharmaceutical co-crystal and preparation method thereof
  • Fenbufen pharmaceutical co-crystal and preparation method thereof
  • Fenbufen pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh 254.2 mg of fenbufen and 122.2 mg of isonicotinamide, dissolve them in 10 ml of a mixed solvent of acetone and cyclohexane with a volume ratio of 1:1, ultrasonicate for 50 min, cool slowly, and filter the resulting suspension to obtain The clarified solution was placed in a constant temperature incubator at 35° C. for constant temperature cultivation. After 7 days, the fenbufen-isonicotinamide co-crystal was obtained. Using SXRD to characterize and analyze the crystal, the obtained fenbufen-isonicotinamide crystal structure is as follows: figure 1 As shown, its crystal structure belongs to the triclinic crystal system, and the space group is Shaft length: Angle: α / °=84.335(4), β / °=86.495(4), γ / °=80.888(4), Z=2.

Embodiment 2

[0036] Weigh 127.1mg of fenbufen and 122.2mg of isonicotinamide, dissolve in 12ml of acetonitrile and chloroform mixed solvent with a volume ratio of 2:1, sonicate for 80min, cool slowly, and filter the resulting suspension to obtain a clear solution Placed in a constant temperature incubator at 30°C for constant temperature cultivation, after 10 days, the fenbufen-isonicotinamide co-crystal was obtained. The crystals were characterized by differential scanning calorimetry, and the fenbufen-isonicotinamide cocrystal had an absorption peak at 143.31°C, and the DSC figure was as follows figure 2 shown.

Embodiment 3

[0038] Weigh 254.2mg of fenbufen and 61.1mg of isonicotinamide, dissolve in 15ml of a mixed solvent of ethanol and acetone with a volume ratio of 4:1, sonicate for 120min, cool slowly, and filter the resulting suspension to obtain a clear solution Placed in a constant temperature incubator at 25°C for constant temperature cultivation, after 15 days, the fenbufen-isonicotinamide co-crystal was obtained. Using PXRD to characterize the obtained crystals, the fenbufen-isonicotinamide cocrystals are at 2θ=5.8°, 8.9°, 12.0°, 17.9°, 19.6°, 20.9°, 21.6°, 23.9°, 25.8°, 27.1° , there are characteristic peaks at 30.1°, 36.3°, and 46.0°, and the characteristic curves are as follows image 3 shown.

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Abstract

The invention discloses two fenbufen pharmaceutical co-crystals and a preparation method thereof, and the two co-crystals both take fenbufen as pharmaceutical active ingredients and take isonicotinamide or nicotinamide as co-crystal formations respectively. The two eutectic crystals are prepared by adopting a solvent evaporation method. The obtained eutectic crystal is characterized by differential scanning calorimetry, powder X-ray diffraction and single crystal X-ray diffraction, and formation of a new crystal form is proved. The solubility of the fenbufen medicine and the two eutectic crystals of the fenbufen medicine in water and a simulated duodenum solution is investigated, the two pharmaceutical eutectic crystals obviously improve the solubility of the fenbufen medicine, and the bioavailability of the fenbufen medicine is improved.

Description

technical field [0001] The invention belongs to the field of organic drug co-crystals, in particular to fenbufen drug co-crystals and a preparation method thereof. Background technique [0002] The solid forms of drugs generally include salts, polymorphs, hydrates, solvates, amorphous forms, and co-crystals, and crystalline drugs are often selected because of their advantages in stability and operability. The study of drug crystal forms has great and far-reaching significance. At the same time, drug co-crystal research is an important part of drug crystal form research. [0003] Drug co-crystal is a novel solid form formed by the active ingredient of the drug and the co-crystal reagent through intermolecular force (such as hydrogen bond). Drug co-crystals can have a significant impact on the physical and chemical properties of drug active ingredients without changing the covalent structure of drugs, thereby improving the bioavailability of drugs, enhancing drug efficacy, a...

Claims

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Application Information

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IPC IPC(8): C07C59/84C07D213/81C07D213/82C07C51/43
CPCC07C59/84C07D213/81C07D213/82C07C51/43C07B2200/13
Inventor 王明亮邢可从扬
Owner SOUTHEAST UNIV
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