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Scutellarin

A technology of scutellarin and breviscapine, applied in the field of scutellarin, can solve the problems of low scutellarin content, low bioavailability, unsatisfactory clinical efficacy and the like

Inactive Publication Date: 2009-11-25
周玲
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Scutellarein, also known as scutellarin saponin aglycon, its chemical structure is 5,6,7,4-tetrahydroxyflavone, the difference from scutellarin is the 7 free hydroxyl group, scutellarin is the The main component of breviscapine injection has the effect of treating cardiovascular and cerebrovascular diseases, and has a good therapeutic effect in clinical practice. However, because of the low bioavailability of breviscapine oral preparations, the clinical efficacy is not very ideal. A large number of literature reports , the metabolite of scutellarin in the body is scutellarein, and the bioavailability of scutellarein is several times higher than that of scutellarin ("Comparison of pharmacokinetics of different doses of scutellarin in rats", Che Qingming, etc., Chinese Journal of New Drugs, Volume 15, No. 18, 2006), therefore, medical researchers believe that scutellarein can be developed into a new drug, but the content of scutellarein in breviscapine is very low, so scientific research work is needed Solve the problem of wild scutellarein raw material

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Add water to dissolve scutellarin completely, adjust the pH value to 2, heat to 50°C, concentrate at a constant temperature of 50°C for 3-hours, put the concentrated solution on a polyamide column, wash it with water first, then wash it with 20%% ethanol, keep the ethanol eluent, Concentrate and dry to obtain scutellarein.

Embodiment 2

[0048] Add water to dissolve scutellarin completely, adjust the pH value to 6, heat to 80°C, keep the temperature at 80°C for 24 hours, concentrate, put the concentrate on a polyamide column, wash with water first, then wash with 90% ethanol, keep the ethanol eluent, concentrate , dried to obtain scutellarein.

Embodiment 3

[0050] Add water to dissolve scutellarin completely, adjust the pH value to 4, heat to 65°C, keep the temperature at 65°C for 15 hours, concentrate, put the concentrate on a polyamide column, wash with water first, then wash with 55% ethanol, keep the ethanol eluent, concentrate , dried to obtain scutellarein.

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PUM

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Abstract

The invention discloses a scutellarin, characterized in that the scutellarin is prepared by the following steps: dissolving breviscapine in water completely, heating to 35 to 45 DEG C, keeping at the constant temperature between 35 DEG C and 45DEG C, adjusting the pH value to 2 to 6, adding digestive enzyme, keeping at the constant temperature between 35 DEG C and 45DEG C for 2 to 12 hours, concentrating, adding the concentrated solution into a polyamide column, eluting with water, eluting with 20 % to 90% ethanol, concentrating the ethanol eluent, drying. The process of the invention has high extraction yield, the scutellarin purity is high as the active ingredient of the medicinal preparation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a scutellarein Background technique [0002] Scutellarein, also known as scutellarin saponin aglycone, its chemical structure is 5,6,7,4-tetrahydroxyflavone, the difference from scutellarin is the 7 free hydroxyl group, scutellarin is scutellaria The main component of breviscapine injection has the effect of treating cardiovascular and cerebrovascular diseases, and has a good therapeutic effect in clinical practice. However, because of the low bioavailability of breviscapine oral preparations, the clinical efficacy is not very ideal. A large number of literature reports , the metabolite of scutellarin in the body is scutellarein, and the bioavailability of scutellarein is several times higher than that of scutellarin ("Comparison of pharmacokinetics of different doses of scutellarin in rats", Che Qingming, etc., Chinese Journal of New Drugs, Volume 15, No. 18, 2006), therefore,...

Claims

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Application Information

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IPC IPC(8): C07D311/30C07D311/40A61K31/352A61P9/00
Inventor 周小亮周美吟安晓雪
Owner 周玲
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