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Scutellarein

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

Inactive Publication Date: 2009-12-02
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

[0047] Breviscapine was completely dissolved in water, adjusted to pH 8, heated to 50 ° C, constant temperature of 50 ° C for 3-hours, adjusted to pH value of 2, concentrated, the concentrated solution was placed on a polyamide column, washed with water first, then washed with 20% ethanol, The ethanol eluent was retained, concentrated and dried to obtain scutellarin.

Embodiment 2

[0049] Breviscapine was completely dissolved in water, adjusted to pH 12, heated to 80°C, constant temperature of 80°C for 24 hours, adjusted to pH value of 6.5, concentrated, and the concentrate was applied to a polyamide column, washed with water first, then washed with 90% ethanol, and retained the ethanol The eluate was concentrated and dried to obtain scutellarin.

Embodiment 3

[0051] Breviscapine was completely dissolved in water, adjusted to pH 10, heated to 65°C, constant temperature of 65°C for 15 hours, adjusted to pH value of 4.5, concentrated, the concentrate was placed on a polyamide column, washed with water first, then washed with 55% ethanol, and the ethanol was retained. The eluate was concentrated and dried to obtain scutellarin.

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Abstract

The invention discloses scutellarein, which is characterized in that the scutellarein is prepared by the following steps: adding water into breviscapinun and fully dissolving the breviscapinun, heating the water solution to between 35 and 45 DEG C, keeping the water solution at the constant temperature of between 35 and 45 DEG C, adjusting the pH value to between 8.0 and 12.0, adding digestive enzyme into the water solution, keeping the water solution at the constant temperature of between 35 and 45 DEG C, placing the water solution for 2 to 12 hours, adjusting the pH value to between 2.0 and 6.5, concentrating the water solution, loading concentrate on a polyamide column, washing the polyamide column by water, then washing the polyamide column by 20 to 90 percent ethanol, keeping ethanol eluent, concentrating the eluent, and drying the concentrate to obtain the scutellarein. The extraction rate of the process method is high, the purity of the scutellarein is high, and the scutellarein can be used as an active component of a medicinal preparation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a kind of scutellarin Background technique [0002] Scutellarin, also known as breviscapine saponin aglycone, its chemical structure is 5, 6, 7, 4-tetrahydroxyflavone, the difference from breviscapine is the free hydroxyl group at the 7th position, breviscapine is breviscapine The main component of scutellarin injection has the effect of treating cardiovascular and cerebrovascular diseases, and has a good clinical therapeutic effect, while the oral preparation of breviscapine has low bioavailability, and its clinical efficacy is not very satisfactory. A large number of literature reports , the metabolite of scutellarin in the body is scutellarin, and the bioavailability of scutellarin is several times higher than that of scutellarin ("Comparison of the pharmacokinetics of scutellarin in rats with different doses of scutellarin", Che Qingming et al., China Journal of New Drugs, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
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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