Novel application of guanfu base A and guanfu base G

A technology of Guanfu A and Guanfuheptin, which is applied in the field of preparation of drugs for inhibiting the activity of drug-metabolizing enzymes, and can solve the problems of no literature reports on specific inhibitory effects

Active Publication Date: 2012-08-22
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the drug screening process, specific CYP2D6 inhibitors can be used in the prediction research of drug interactions, and the diterpenoid alkaloids of Guanbaifuzhong involved in the present invention are mainly composed of Guanfu A and its hydrochloric acid or sulfate, Guanfu There is no literature report on the specific inhibitory effect of fuheptin and its hydrochloric acid or sulfate on CYP2D6

Method used

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  • Novel application of guanfu base A and guanfu base G
  • Novel application of guanfu base A and guanfu base G
  • Novel application of guanfu base A and guanfu base G

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] Take Guanfu A hydrochloride, sucrose, cornstarch, and magnesium stearate in a ratio of 1:16:5:0.3 by weight and make a capsule according to a conventional method.

Embodiment 2

[0126] Get 10 g of heptanine sulfate, sucrose, cornstarch, and magnesium stearate in a ratio of 1:16:5:0.3 by weight, and make tablets according to a conventional method.

Embodiment 3

[0128] Take Guanfu A hydrochloride 1g, make intravenous injection according to the conventional process.

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PUM

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Abstract

The invention provides the application of norditerpenoid alkaloids which are guanfu base A and guanfu base G in Korean mondshood roots in the aspect of suppressing the activity of drug metabolizing enzymes. By the guanfu base A and the guanfu base G, the activity of CYP2D6 can be directly suppressed, the metabolism of drugs (substrates) is retarded, and the drug effect is reinforced; and moreover, the guanfu base A and the guanfu base G have no influence to the activity of other metabolizing enzymes.

Description

technical field [0001] The invention relates to a new application of diterpene alkaloids, in particular to the application of Guanfu A and Guanfuheptin in the preparation of drugs for inhibiting the activity of drug-metabolizing enzymes. Background technique [0002] Guanbaifu is the root tuber of Aconitum coreanum (Levl,) Rapaics, a traditional Chinese medicine. It is one of the common Chinese medicines. It is mainly used for heartache and blood stagnation. Its chemical composition is mainly related to Guanfu base G (GFG), Guanfu base A (GFA), etc., both of which are diterpenoid alkaloids. Among them, Guanfu A is a new type of safe and effective broad-spectrum antiarrhythmic drug discovered for the first time. [0003] Cytochrome P450 (CYP) is a superfamily enzyme system composed of isozymes encoded by the superfamily of genes related to structure and function, although the content of CYP2D6 accounts for only 2% of all CYP isozymes in the liver. 5%, but the drugs involved...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61P43/00
Inventor 孙建国王广基彭英董秀华吴慧尚丽丽刘静涵杨春华王国栋刘可俞广为胡天娇
Owner CHINA PHARM UNIV
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