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Two anhydroicaritin crystal forms and preparation method thereof

A technology of dehydrated icariin and crystal form, applied in the direction of organic chemistry, etc., can solve the problem of not paying attention to the screening of the crystal form of dehydrated icariin, and achieve the effects of improving the solubility curve, stabilizing the dissolution rate and improving the stability.

Inactive Publication Date: 2015-08-26
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Domestic patent (CN201210071686.4) studies the application of dehydrated icariin as an active ingredient in the preparation of anti-osteoporosis and bone repair drugs; no attention has been paid to the crystal form screening of dehydrated icariin

Method used

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  • Two anhydroicaritin crystal forms and preparation method thereof
  • Two anhydroicaritin crystal forms and preparation method thereof
  • Two anhydroicaritin crystal forms and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation method 1 of crystal form A of dehydrated icariin

[0044] Dissolve the dehydrated icariin completely with chloroform, let it stand in a small beaker, then put the small beaker into a closed large beaker filled with methanol, use the method of gas-liquid diffusion, and place it at a temperature range of 4 ° C, relatively Under environmental conditions with a humidity range within 90%, after 20 days of crystal growth, a solid sample of Form A was prepared.

[0045] The preparation method of the A crystal form of dehydrated icariin 2

[0046]Dissolve the dehydrated icariin completely with chloroform, let it stand in a small beaker, then put the small beaker into a closed large beaker filled with methanol, use the method of gas-liquid diffusion, place it in a temperature range of 20 ° C, relatively Under environmental conditions with a humidity range within 90%, after 15 days of crystal growth, a solid sample of Form A was prepared.

[0047] The preparation me...

Embodiment 2

[0050] Preparation method 1 of crystal form A of dehydrated icariin

[0051] Dissolve the dehydrated icariin completely with dichloromethane, put it in an appropriate container, use the method of volatilization and crystallization, place it at a temperature of 4°C, and the relative humidity range is within 90% of the environmental conditions, after 20 days of crystallization growth time , to prepare a solid sample of Form A.

[0052] The preparation method of the A crystal form of dehydrated icariin 2

[0053] Firstly dissolve the dehydrated icariin completely with dichloromethane, put it in an appropriate container, use the method of volatilization and crystallization, place it under the environmental conditions of temperature 30°C and relative humidity within 90%, after crystallization growth time 8 On the first day, a solid sample of Form A was prepared.

[0054] The preparation method of the A crystal form of dehydrated icariin 3

[0055] First dissolve the dehydrated i...

Embodiment 3

[0057] The preparation method 1 of the B crystal form of dehydrated icariin

[0058] Dissolve dehydrated icariin completely with ethyl acetate, put it in a test tube, use the method of volatilization and crystallization, place it under the environmental conditions with a temperature range of 4°C and a relative humidity range of 90%, after crystallization growth time 20 On the next day, a solid sample of Form B was prepared.

[0059] The preparation method of the B crystal form of dehydrated icariin 2

[0060] Dissolve dehydrated icariin completely with ethyl acetate, put it in a test tube, use the method of volatilization and crystallization, place it under the environmental conditions with a temperature range of 30°C and a relative humidity range of 90%, after crystallization growth time 15 On the next day, a solid sample of Form B was prepared.

[0061] The preparation method of the B crystal form of dehydrated icariin 3

[0062] Dissolve dehydrated icariin completely wit...

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Abstract

The invention discloses an anhydroicaritin crystal form A and an anhydroicaritin crystal form B and a preparation method thereof and belongs to the technical field of pharmaceutical chemistry. The preparation method of the anhydroicaritin crystal form A and the anhydroicaritin crystal form B is simple in process and high in conversion rate. The prepared crystal form A and crystal form B are single in crystal form and high in purity and has a significantly improved solubility curve when compared with amorphous powder, so that the stability of bioavailability is improved, and the druggability of the anhydroicaritin is facilitated. The structural formula of the anhydroicaritin is shown in the description.

Description

technical field [0001] The invention discloses two crystal forms of dehydrated icariin and a preparation method thereof, belonging to the field of medicinal chemistry. Background technique [0002] Dehydrated icariin is the main active compound isolated and identified from Epimedium medicinal material, and its molecular structure is as follows: [0003] [0004] Dehydrated Icaritin [0005] The domestic patent (CN200810094122.6) mixes β-anhydroicariin with pharmaceutically acceptable excipients in a certain proportion to make a combined drug for preventing and treating cardiovascular diseases. However, this invention ignores the polymorphic solid state of dehydrated icariin. Dehydrated icariin will form different crystals under the influence of various factors, and different crystals will show different solubility and dissolution stability. Then make its efficacy and even drug properties change. As a drug, if there is no in-depth research on crystal form screening, the...

Claims

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Application Information

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IPC IPC(8): C07D493/04
CPCC07D493/04
Inventor 李海舟周义梅晶李蓉涛
Owner KUNMING UNIV OF SCI & TECH
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