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Icariin H1 crystal form, as well as production method, pharmaceutical composition and application thereof

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

Active Publication Date: 2015-08-12
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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  • Icariin H1 crystal form, as well as production method, pharmaceutical composition and application thereof
  • Icariin H1 crystal form, as well as production method, pharmaceutical composition and application thereof
  • Icariin H1 crystal form, as well as production method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Take 30 mg of icariin in a bottle, add 3 mL of methanol, sonicate to dissolve and become supersaturated, suspend at room temperature for 3 days, centrifuge the suspension, discard the supernatant, and centrifuge The solid was vacuum-dried at 50°C to obtain icariin H1 crystal form.

Embodiment 2

[0039] Take 30mg of icariin in a bottle, add 3mL of absolute ethanol, ultrasonicate to dissolve and become supersaturated, suspend at room temperature for 3 days, centrifuge the suspension, discard the supernatant, and centrifuge The resulting solid was vacuum-dried at 50° C. to obtain icariin H1 crystal form.

Embodiment 3

[0041]Take 30 mg of icariin in a bottle, add 3 mL of n-propanol with a mass concentration of 70%, ultrasonically dissolve it and make it supersaturated, suspend at room temperature for 3 days, centrifuge the suspension, and discard For the supernatant, the centrifuged solid was evaporated to dryness at 100°C to obtain icariin H1 crystal form.

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PUM

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Abstract

The invention belongs to the technical field of medicinal chemistry and particularly relates to an icariin H1 crystal form, as well as a production method, a pharmaceutical composition and an application thereof. The crystal form is represented through an X-ray powder diffraction pattern. The preparation method comprises the following steps: dissolving the icariin by a single solvent or a mixed solvent, suspending under room temperature, performing vacuum drying on the centrifuged solid or drying at the temperature of higher than 100 DEG C. The pharmaceutical composition comprises the icariin H1 crystal form and a pharmaceutically acceptable carrier. The icariin H1 crystal form is applied to prepare a medicine for preventing the immune system disease, the tumor tissue disease, the genital system disease, the endocrine system disease, the bone tissue disease, the disease of cardiovascular system and the disease of central nervous system. The icariin H1 crystal form provided by the invention is simple in preparation method operation, easy to control in the crystallizing process, high in degree of crystallinity, good in crystal form reproducibility and good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a crystal form of icariin H1, 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 wit...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/00A61K31/7048A61P37/00A61P35/00A61P15/00A61P5/00A61P19/08A61P9/00A61P25/00
CPCA61K9/2059C07H1/06C07H17/07
Inventor 朱理平梅雪锋贾丽娜王建荣张奇
Owner ZHUCHENG HAOTIAN PHARMA
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