Baicalein-nicotinamide eutectic crystal

A technology of baicalein nicotinamide and baicalein, which is applied in the field of medicine, can solve the problems of organic solvent environmental pollution, cumbersome process, and too long eutectic time, and achieve the effects of increasing yield, avoiding technological process, and reducing experiment cycle

Inactive Publication Date: 2014-06-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method also has many deficiencies: including the preparation of eutectic time is too long, the process is cumbersome, organic solvents cause environmental pollution, etc.

Method used

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  • Baicalein-nicotinamide eutectic crystal
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  • Baicalein-nicotinamide eutectic crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1: Preparation of baicalein nicotinamide cocrystal

[0067] Precisely weigh 1.1 g of baicalein and 497.7 mg of nicotinamide, mix them evenly, add them to a ball mill jar, add grinding balls, install them on a planetary ball mill, and grind for 3 hours at a speed of 500 r / min to obtain 1.5 g of yellow crystals.

Embodiment 2

[0068] Embodiment 2: Preparation of baicalein nicotinamide cocrystal

[0069] Precisely weigh 1.1g of baicalein and 497.7mg of nicotinamide, mix them evenly, add them to a ball mill jar, add grinding balls, install them on a planetary ball mill, and grind for 1 hour at a speed of 700r / min to obtain 1.3g of yellow crystals.

Embodiment 3

[0070] Embodiment 3: Preparation of baicalein nicotinamide cocrystal

[0071] Precisely weigh 1.1 g of baicalein and 497.7 mg of nicotinamide, mix them evenly, add them to a ball mill jar, add grinding balls, install them on a planetary ball mill, and grind for 5 hours at a speed of 200 r / min to obtain 1.2 g of yellow crystals.

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Abstract

The invention relates to a eutectic crystal formed from baicalein and nicotinamide. An XRPD (X Ray Powder Diffraction) pattern of the baicalein-nicotinamide eutectic crystal disclosed by the invention has characteristic peaks at 5.83 degrees, 7.71 degrees, 11.70 degrees, 14.44 degrees, 15.70 degrees, 19.81 degrees, 20.19 degrees, 26.05 degrees and 26.56 degrees, a DSC (Differential Scanning Calorimetry) diagram of the baicalein-nicotinamide eutectic crystal has a strong endothermic peak at 165.65 DEG C, and an infrared spectroscopy of the baicalein-nicotinamide eutectic crystal has characteristic wave numbers at 3444.98cm<-1>, 3338.89cm<-1>, 3180.72cm<-1>, 1641.48cm<-1> and 1386.86cm<-1>; the measurement results of the XRPD pattern, the DSC diagram and the infrared spectroscopy of the baicalein-nicotinamide eutectic crystal are all different from the related measurement results of baicalein and physical mixtures of baicalein and nicotinamide, which indicates that the crystal is a novel crystal form completely different from that of baicalein and physical mixtures of baicalein and nicotinamide.The baicalein-nicotinamide eutectic crystal is prepared by a grinding method which is simple and convenient in flow, free of pollution, low in cost and high in yield.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a co-crystal of baicalein nicotinamide and a preparation method thereof. Background technique [0002] For pharmaceutical active ingredients, its crystalline form can affect its many properties, such as melting point, solubility, stability, bioavailability, etc. Studies have shown that drug co-crystals can use hydrogen bonds or other non-covalent bonds to generate supramolecular compounds through intermolecular recognition, thereby effectively improving the crystallization properties, physical and chemical properties and efficacy of drugs themselves. choose. Since the formation of pharmaceutical co-crystals does not destroy the covalent bonds of active ingredients of pharmaceuticals, it is a good means to improve the properties of pharmaceuticals. Therefore, for a specific drug, hundreds of drug co-crystals may be generated, which can not only improve the physical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30C07D213/82
CPCC07D311/30C07D213/82
Inventor 高缘张博文黄燕婷张建军
Owner CHINA PHARM UNIV
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