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A crystal form and b crystal form of triptolide, and preparation method and use thereof

A technology of tripteryglide and its crystal form, which is applied in the field of medicinal chemistry, can solve the problems of low bioavailability, poor water solubility of tripteryne, hindering the development of finished medicine, etc., and achieve simple preparation methods, high solubility, and improved physical and chemical properties. Effect

Active Publication Date: 2019-06-28
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Because tripterine has poor water solubility, low bioavailability, especially its strong toxicity hinders the development of its finished medicine

Method used

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  • A crystal form and b crystal form of triptolide, and preparation method and use thereof
  • A crystal form and b crystal form of triptolide, and preparation method and use thereof
  • A crystal form and b crystal form of triptolide, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Take 20mg of tripterine raw material, add 1mL of acetonitrile solvent, suspend at room temperature for 2 days, centrifuge and take powdery solid, after vacuum drying, put it in an oven at 150°C and heat to obtain the A crystal form of tripterine. For the red powder.

[0084] Carry out X-ray powder diffraction analysis to the A crystal form solid sample of tripterine obtained in Example 1, the analysis results are shown in figure 1 . Adopt TG209F3 type thermal gravimetric analyzer of German Netzsch Scientific Instrument Co., Ltd. to carry out thermogravimetric analysis to the A crystal form of tripteryglide produced in Example 1, the analysis results are shown in figure 2 . From figure 2 As can be seen in the figure, this crystal form A is non-hydrate or non-solvate.

[0085] The DSC Q2000 differential scanning calorimeter of U.S. TA instrument company is used to detect that the A crystal form of tripterine produced in Example 1 is subjected to differential scannin...

Embodiment 2

[0088] Take 10 mg of tripterine as a raw material, add 5 mL of acetonitrile solvent, dissolve it by ultrasonic waves, volatilize and dry at room temperature, heat the obtained powdery solid in an oven at 150°C, and obtain tripterine A crystal form, which is red powder.

Embodiment 3

[0090] Take 50mg of tripterine raw material, add 2mL of nitromethane solvent, suspend at 25°C for 2 days, centrifuge and take powdery solid, after vacuum drying, put it into an oven at 130°C and heat it to get tripterine Form A is a red powder.

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Abstract

The invention relates to crystal forms A and B of celastrol as well as a preparation method and application thereof. According to comprehensive representation of the crystal forms A and B of celastrol by use of the means such as X-ray diffraction, infrared spectrum, Raman spectrum, differential scanning calorimetry, thermogravimetric analysis and hygroscopicity analysis, better physicochemical properties and patent medicine property of the crystal forms A and B are discovered. The preparation method of the crystal forms A and B of celastrol has the advantages of simple operation, easy control, high reproducibility, high solubility and high stability.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and specifically relates to A crystal form and B crystal form of tripterine, a preparation method and application thereof. Background technique [0002] Polymorphism refers to the phenomenon that solid substances form solid states with different physical and chemical properties in two or more different spatial arrangements. In the field of pharmaceutical research, polymorphism includes multi-component crystal forms such as organic solvates and hydrates. Drug polymorphism widely exists in the drug development process and is an inherent characteristic of small organic molecules. Polymorphism is not only controlled by internal factors such as the spatial structure and functional group properties of the molecule itself, intramolecular and intermolecular interactions, but also by drug synthesis process design, crystallization and purification conditions, preparation excipients selection, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P3/04A61P29/00A61P35/00A61P31/12
CPCC07B2200/13C07J63/008
Inventor 梅雪锋查珺张奇王建荣
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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