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Dehydroandrographolide succinate crystal and use thereof

A compound, cu-k technology, applied in the field of medicine, can solve the problems of poor lactone stability, unstable production process, low purity of initial raw materials (andrographolide, etc.)

Active Publication Date: 2013-07-10
成都天台山制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reasons for the specific analysis of adverse reactions are (1) individual differences (allergic constitution); (2) andrographolide has poor stability and is prone to hydrolysis, ring opening, isomerization and oxidation of unsaturated bonds
(3) The purity of the initial raw material (andrographolide) is not high, and the main impurities are high-molecular plant protein, andrographolide hydrolysis, oxidation products, and pigments. It is reported in the literature that activated carbon is used for decolorization, and ultrafiltration membranes with a molecular cut-off of 5000 are used. After ultrafiltration, the LD50 of a single intravenous administration of mice can be increased from 757mg / kg to 910mg / kg; (4) Andrographolide is unstable in product quality due to unstable production process in the process of esterification and dehydration
To sum up, although the characteristics of traditional Chinese medicine injections determine that more or less adverse reactions of Chuanhuning or Yanhuning are inevitable, it is an indisputable fact that improving product quality and purity can greatly improve product clinical safety

Method used

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  • Dehydroandrographolide succinate crystal and use thereof
  • Dehydroandrographolide succinate crystal and use thereof
  • Dehydroandrographolide succinate crystal and use thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0079] Preparation of Chuanhuning:

[0080] The raw material used in the preparation of Yanhuning in the present invention is Chuanhuning, which can be prepared by prior art methods, for example:

preparation example 1

[0081] Chuanhuning preparation example 1: prepared by referring to the method in paragraphs [0048] to [0050] of the description of CN102617527A (Chinese patent application number 201210051312.6, Hubei Hope).

preparation example 2

[0082] Chuanhuning preparation example 2: It was prepared by referring to the method in paragraphs [0054] to [0056] of the description of CN102617527A (Chinese patent application number 201210051312.6, Hubei Hope).

[0083] In addition, commercially available Chuanhuning raw materials can also be used. For example, in the following examples of the present invention, the commercially available Chuanhuning used is produced by Chengdu Tiantaishan Pharmaceutical Co., Ltd. (National Drug Approval H51023411).

[0084] In the following example of preparing Yanhuning, the dosage of each batch is 20mol of Chuanhuning.

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Abstract

The invention relates to dehydroandrographolide succinate crystal and use thereof, and particularly relates to a compound in a formula shown in the specification, wherein Cu-Kalpha radiation is utilized; and diffraction peaks are formed at the parts which are about 10.60 degrees, about 12.76 degrees, about 14.58 degrees, and about 15.66 degrees in a powder X-ray diffraction pattern represented by a 2*theta angle. The compound disclosed by the invention has good pharmaceutical properties.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a crystal of Yanhuning, a preparation method of the crystal of Yanhuning and its medical application. Background technique [0002] Andrographis paniculata (Andrographis paniculata (Burm.F.) Nees) is the dry aerial part of the Acanthaceae plant. It is harvested when the stems and leaves are luxuriant in early autumn and dried in the sun. Andrographis paniculata, also known as spring lotus and autumn willow, is a joy at first sight, Lamicarpa, bitter gall grass, golden vanilla, golden ear hook, Indian grass, bitter grass and so on. It has the effects of clearing away heat and detoxification, reducing inflammation, reducing swelling and relieving pain. It is mainly used to treat bacillary dysentery, urinary tract infection, acute tonsillitis, enteritis, pharyngitis, pneumonia and influenza, etc. It can be used externally to treat sores, furuncles, swollen toxins, and traumatic infe...

Claims

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Application Information

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IPC IPC(8): C07D307/58A61K31/365A61P31/12A61P11/00
Inventor 赵东明方专王敬江威张莲莲董国明
Owner 成都天台山制药股份有限公司
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