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A crystal form of icariin form α, its preparation method, its pharmaceutical composition and application

A technology of icariin and crystal form, applied in the field of medicinal chemistry, can solve the problems of poor oral absorption, poor water solubility of icariin, limited clinical application, etc., and achieves favorable absorption and utilization, good reproducibility, and oral absorption. high rate effect

Active Publication Date: 2017-12-19
ZHUCHENG HAOTIAN PHARMA
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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 icariin and poor oral absorption, its clinical application is greatly limited.
At present, there is no report on the polymorphic form of icariin

Method used

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  • A crystal form of icariin form α, its preparation method, its pharmaceutical composition and application
  • A crystal form of icariin form α, its preparation method, its pharmaceutical composition and application
  • A crystal form of icariin form α, its preparation method, its pharmaceutical composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Take 10 mg of icariin and heat it to 180°C for 5 minutes to obtain the Formα crystal form of icariin.

Embodiment 2

[0037] Take 30 mg of icariin and heat it to 180°C for 10 minutes to obtain the Formα crystal form of icariin.

Embodiment 3

[0039] Take 50 mg of icariin and heat it to 180°C for 15 minutes to obtain the Formα crystal form of icariin.

[0040] A kind of icariin Formα crystal form provided by the present invention, through X-ray powder diffraction (XRPD), thermogravimetric analysis (TG), differential scanning calorimetry (DSC), dynamic water adsorption (DVS), infrared ( IR) and Raman (Raman) and other solid-state methods for characterization.

[0041] Carry out X-ray powder diffraction analysis to the icariin Form α crystal form solid sample that embodiment 1 makes, it adopts the diffractometer of Bruker D8advance type of German Bruker Instrument Co., Ltd., adopts Cu-K α ray The voltage is 40 kV, the current is 40 mA, the scanning speed is 12 degrees per minute, the step size is 0.02 degrees, and each step takes 0.1 seconds. The results of the analysis can be found in figure 1 .

[0042] The icariin Formα crystal solid sample prepared in Example 1 was subjected to thermogravimetric analysis using...

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Abstract

The invention belongs to the technical field of medicinal chemistry and particularly relates to an icariin form-alpha crystal, a preparation method thereof and a medicinal combination and application thereof. The crystal is represented through an X-ray powder diffraction diagram; the preparation method thereof comprises the step of heating icariin to 180 DEG C; the medicinal combination comprises the icariin form-alpha crystal and pharmaceutically acceptable carriers; the icariin form-alpha crystal is applied to the medicines for preventing and treating immune system diseases, tumor tissue diseases, genital system diseases, endocrine system diseases, bone tissue diseases, cardiovascular system diseases and nervous system diseases. The icariin form-alpha crystal provided by the invention has the advantages that the preparation method thereof is simple to operate, the crystallization process is easy to control, the crystallization degree is high, the reproducibility of the crystal is good and the stability is good.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a Formα crystal form of icariin, a preparation method thereof, a pharmaceutical composition 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. [0003] Drug polymorphism widely exists in the drug development process and is an inherent characteristic of small organic molecules. Theoretically, small-molecule drugs can have an infinite number of crystal packing methods - polymorphic forms. Studies have shown that the number of drug polymorphic forms discovered is proportional to the time and resources invested in research. For example, Lipitor, the drug ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/07C07H1/06A61K31/7048A61P37/02A61P35/00A61P15/00A61P5/00A61P19/00A61P9/00A61P25/00
CPCC07B2200/13C07H1/06C07H17/07
Inventor 朱理平梅雪锋贾丽娜王建荣张奇
Owner ZHUCHENG HAOTIAN PHARMA
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