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Two crystal form materials of salvianolic acid A, preparation method as well as medicine compound and application thereof

A technology of salvianolic acid and crystal form, applied in directions such as drug combination, preparation of carboxylate, preparation of organic compounds, etc., can solve problems such as no reports on the preparation method of solid crystal material.

Active Publication Date: 2010-05-26
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0027] After searching the literature, most of them are literatures about the research progress of the pharmacological action of salvianolic acid A, and there is no report on the preparation method of its solid crystalline substance

Method used

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  • Two crystal form materials of salvianolic acid A, preparation method as well as medicine compound and application thereof
  • Two crystal form materials of salvianolic acid A, preparation method as well as medicine compound and application thereof
  • Two crystal form materials of salvianolic acid A, preparation method as well as medicine compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Preparation method 1 of the α crystal form solid sample of salvianolic acid A:

[0087] The preparation method of the α crystal form solid sample of salvianolic acid A is characterized in that the salvianolic acid A sample is completely dissolved at 15-25°C at normal temperature using acetone or ethanol solvent, and the temperature is controlled at 45°C by vacuum filtration or spinning. Evaporation method The solvent in the sample is quickly suction filtered or evaporated to dryness, and the sample is then dried to finally prepare the α-crystal solid sample of salvianolic acid A.

[0088] Preparation method 2 of the α crystal form solid sample of salvianolic acid A:

[0089] The preparation method of the α-crystal form solid sample of salvianolic acid A is characterized in that the mixed solution is prepared by using n-propanol and water at a ratio of 2:1, and then the salvianolic acid A sample is completely dissolved and controlled under normal temperature of 15-25°C. ...

Embodiment 2

[0095] Preparation method 1 of the β crystal form solid sample of salvianolic acid A:

[0096] The preparation method of the β-crystal form solid sample of salvianolic acid A is characterized in that the α-crystal form solid sample of salvianolic acid A is placed in a thermostat at 105°C and heated for 60 minutes to obtain the β-crystal form of salvianolic acid A. type solid samples.

Embodiment 3

[0098] Pharmacodynamic characteristics of oral administration of crystalline components of salvianolic acid A:

[0099] Experimental animals: 120 SD male rats, weighing 180-200 g, purchased from Beijing Weitong Lihua Experimental Technology Co., Ltd., obtained type 2 diabetes model rats through modeling experiments, and detected TG, TC, LDL- Blood lipid levels such as C and NEFA and blood biochemical indicators such as SOD and MDA prove that the model of type 2 diabetic rats was successfully established.

[0100] Experimental method: For rats with type 2 diabetes, after fasting for 12 hours, each 3 mg / kg of salvianolic acid crystal form solid drug was administered by intragastric administration, once a day, for 6 consecutive weeks. Before administration and 3 days, 1 week, 2 weeks, and 6 weeks after administration, blood was taken from the eye sockets, and the body weight of rats was measured before administration and 3 days, 1 week, 2 weeks, and 3 weeks after administration. ...

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Abstract

The invention discloses two crystal form solid materials of compound salvianolic acid A, and also discloses a preparation method of the two crystal form solid material samples. The invention relates to a medicine compound which is prepared and developed by adopting crystal form materials as medicine active constituents, and applications thereof to the aspects in preventing and treating diseases of cardio-cerebral-vascular system, immunity system, hyperlipemia, diabetes mellitus and complicating diseases thereof, and the like. A molecular structure of the salvianolic acid A is shown in the formula.

Description

technical field [0001] The present invention relates to the discovery of two crystalline forms of salvianolic acid A in a solid state; and the invention of a preparation method for the α-crystal sample and the β-crystal sample of the salvianolic acid A solid material. [0002] The present invention relates to the use of the crystalline solid substance of crystalline salvianolic acid A as an active ingredient to prepare and develop a drug and its composition for clinical application in cardiovascular and cerebrovascular system, immune system, hyperlipidemia, diabetes and its complications and other diseases. application. In particular, the crystalline solid substance of salvianolic acid A affects the absorption rate of the active ingredients of the drug in the organism, enhances the blood drug concentration in the organism, and thus achieves the improvement of the clinical prevention and treatment effect of the drug. Background technique [0003] Salvianolic acid A, systemat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/732C07C67/52A61K31/216A61P9/00A61P37/00A61P3/06A61P3/10
Inventor 杜冠华吕扬常颖方莲花王珂杨秀颖
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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