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Hairy sepal ponicidin crystallization, preparation method and medicament composition containing the same

A technology of eelin and composition, applied in the field of diterpene compounds, which can solve the problems of poor storage stability, easy moisture absorption, unfavorable industrial production, etc.

Active Publication Date: 2008-12-10
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the calyxin disclosed in the prior art is an amorphous powder, and it is easy to absorb moisture, has poor storage stability, is difficult to dry, and is unfavorable for large-scale industrial production.

Method used

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  • Hairy sepal ponicidin crystallization, preparation method and medicament composition containing the same
  • Hairy sepal ponicidin crystallization, preparation method and medicament composition containing the same
  • Hairy sepal ponicidin crystallization, preparation method and medicament composition containing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Method 1 for the preparation of echinocetin crystal type I sample:

[0057] Take 100mg of echinacein B sample, heat it at 40°C and dissolve it completely in 50mL of methanol solution, place it at room temperature and pressure for 96 hours for recrystallization, filter and wash the obtained crystal, and dry it under vacuum for 2 hours to prepare the obtained crystal I-type calyxin B solid matter 82mg.

[0058] Method 2 for the preparation of echinocetin crystal type I samples:

[0059] Take 100 mg of eelin B, heat it at 45°C and dissolve it completely in 50 mL of ethanol: acetone = 1: 1 solution, place it under normal temperature and pressure for 72 hours for recrystallization, filter and wash the obtained crystals, and dry under vacuum After 2 hours, 84 mg of crystalline form I eclexin was prepared as a solid substance.

[0060] Problems that need to be explained: Since there are 12 single organic solvents that can be used to prepare samples of crystalline form B, and...

Embodiment 2

[0062] Method 1 for the preparation of echinacein crystal type II samples:

[0063] Take 200 mg of calyxin, and use crystal type I solid sample as the preparation raw material at a temperature of 10-30°C, and use the method of physical and mechanical lattice destruction and molecular rearrangement to crystallize to obtain the solid material of calyxin crystal form 185 mg, or 188 mg of echinacein crystal II solid substance prepared by changing physical pressure conditions and temperature conditions.

[0064] Method 2 for the preparation of echinocetin crystal type II samples:

[0065] Take 200mg of eriocalyxin sample, first use acetone solvent to completely dissolve the eriocalyxin sample at room temperature of 15-25°C, and then quickly prepare 193mg of crystalline type II eriocalyxin as a solid substance by cold spray method.

[0066] Problems that need to be explained: Since there are 12 single organic solvents that can be used to prepare samples of crystalline form B, and t...

Embodiment 3

[0068] The preparation method of echinocetin crystal type III sample:

[0069] Take 100mg of eriocalyxin, heat it at 40°C and dissolve it completely in 50mL of methanol, and then use a rotary evaporator to quickly evaporate the solvent under a vacuum condition at a temperature of 45°C to prepare a solid substance of crystalline type I eriocalyxin 97mg, and then the obtained sample was placed in a 225°C incubator and heated for 30 minutes to transform the crystal to obtain 95mg of the crystalline type III solid sample of calyxin.

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Abstract

The invention provides a new crystal form of an eriocalyxin B compound with the following structural formula. The invention also provides a method for preparing the new eriocalyxin B crystal form and a drug composition containing the new eriocalyxin B crystal form as an active ingredient; and the new eriocalyxin B crystal form and the drug composition containing the new crystal form have good biological utilization degree and can better play a clinical role in preventing or treating cancer.

Description

technical field [0001] The invention relates to diterpene compound eriocalyxin B (English name eriocalyxinB) crystal with antitumor activity, its preparation method, pharmaceutical composition containing it and its application in the preparation of antitumor drugs. Background technique [0002] Most of the existing antineoplastic drugs are organically synthesized compounds, but they have the disadvantages of limited efficacy and severe side effects. As we all know, although the natural source of anti-tumor drugs represented by paclitaxel has achieved great clinical success, it can only be extracted and isolated from the bark of the natural plant Taxus chinensis. Not only the cost is extremely high, but also due to the use of bark, The damage caused to plant resources is difficult to recover in a short period of time. Therefore, it is necessary to find anti-tumor drugs with definite efficacy and little damage to resources from natural raw materials. [0003] The inventor ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08A61K31/35A61P35/00
Inventor 孙汉董朱兆云吕扬普建新杜冠华肖伟烈常颖强桂芬王京昆
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI