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Scutellarin derivative and preparation method and application thereof

A technology of scutellarin and derivatives, which is applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problem of increased frequency and limitation of adverse reactions such as pH and heat instability, local irritation and allergies Problems such as the scope of application of scutellarin basic amino acid salt, to achieve the effect of good water solubility, stable and controllable quality, and stable structure

Inactive Publication Date: 2012-02-08
KPC PHARM INC
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, since scutellarin itself is unstable to pH and heat, it cannot be compatible with oxidizing substances, and basic amino acids such as arginine and lysine have salting-out characteristics. After injection, it is easy to produce flocculent precipitates when it is compatible with acidic high-salt infusion, and the basic amino acid salt can be dextrorotated in hydrochloric acid solution, which greatly limits the application range of scutellarin basic amino acid salt
On the other hand, after the preparation of scutellarin sodium salt or potassium salt injection, there is an increase in the frequency of adverse reactions such as local irritation and anaphylaxis in clinical application

Method used

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  • Scutellarin derivative and preparation method and application thereof
  • Scutellarin derivative and preparation method and application thereof
  • Scutellarin derivative and preparation method and application thereof

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preparation example Construction

[0035] The present invention also discloses a preparation method of scutellarin derivatives, the first preparation method specifically includes the following steps:

[0036] Step 1: Add meglumine to the scutellarin suspension and stir to form a clear solution;

[0037] Step 2: directly obtain the scutellarin derivative after freeze-drying.

[0038] Another preparation method of the scutellarin derivative of the present invention specifically comprises the following steps:

[0039] Step 1: Add meglumine to the scutellarin suspension and stir to form a clear solution;

[0040]Step 2: Concentrate the clarified solution in step (1) to 1 / 3-1 / 2 of the original volume, filter to obtain a precipitate, wash and filter the precipitate with an organic solvent, and dry to obtain the scutellarin derivative. Wherein, the organic solvent described in step 2 of the method is methanol, ethanol or acetone.

[0041] Wherein, the scutellarin suspension is prepared by dissolving scutellarin in ...

Embodiment 1

[0047] Example 1: The preparation method of the present invention prepares the scutellarin derivative

[0048] Take 46.2g (0.1 mol) of scutellarin, add 100ml of water and stir; take another 19.5g (0.1 mol) of meglumine, add 50ml of water to dissolve; slowly add the aqueous solution of meglumine dropwise to scutellarin In the plain suspension, stir for about 1 hour until the solution is clear. After lyophilization, 60 g of the product was obtained, and the product yield was 91.3% (product yield=product mass / sum of scutellarin and meglumine mass×100%).

Embodiment 2

[0049] Example 2: Determination of the structure of the scutellarin derivatives of the present invention

[0050] 1. Infrared spectral analysis

[0051] The product in Example 1 was analyzed by infrared spectroscopy, scutellarin reference substance, batch number: 8420-200102, provided by China National Institute for the Control of Pharmaceutical and Biological Products, see figure 1 .

[0052] Scutellarin Infrared Spectrum IRv max(KBr)cm -1 : 3513, 3370 (carboxyl OH), 1720 (carboxylate carbonyl C=O), 1660 (flavone carbonyl C=O), 1608 (C=C), 1574 (benzene ring).

[0053] Product infrared spectrum IR v max (KBr) cm described in embodiment 1 -1 : 3500-3000 (broad blunt peak), 1664 (flavone carbonyl C=O), 1608 (C=C), 1574 (benzene ring).

[0054] The infrared spectrum of the product described in Example 1 shows that the carboxyl OH disappears and a 3500-3000cm -1 The broad blunt peak, 1720cm -1 The carboxylic acid carbonyl C=O disappears, indicating that the carboxyl group h...

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Abstract

The invention relates to the field of medicinal chemistry, discloses a scutellarin derivative, and further discloses a preparation method and application of the scutellarin derivative. The scutellarin derivative is salified through carboxyl of scutellarin and methylamino of meglumine by using an ionic bond. The preparation method comprises the following steps of: adding meglumine into a scutellarin suspension for stirring to form a settled solution; and performing freeze drying to obtain the scutellarin derivative, or concentrating the settled solution to 1 / 3-1 / 2 of the original volume under reduced pressure, filtering to obtain a precipitate, and drying the precipitate to obtain the scutellarin derivative. In the method, the pH value is not required to be controlled, and the process is simple. The scutellarin derivative has high water solubility, and the water insolubility of scutellarin is changed. Meanwhile, as proved by a muscle irritation test on a rabbit and medicament stability research, the scutellarin derivative is safer and more stable than other scutellarin salts, and can be used for preparing a medicament for treating heart cerebrovascular diseases.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, and more specifically relates to a scutellarin derivative, and also relates to a preparation method and application of the scutellarin derivative of the present invention. Background technique [0002] Breviscapine is extracted and isolated from the dry whole herb of the breviscapine breviscapine of the Compositae plant - breviscapine. It has the effects of promoting blood circulation and removing blood stasis, dispelling cold and relieving the surface, relaxing tendons and activating collaterals, and expelling wind and dampness. It is often used clinically to treat cardiovascular and cerebrovascular diseases. The active ingredients of the scutellarin preparations currently used in clinical practice are generally the preparations mainly containing scutellarin extracted with ethanol and ethyl acetate. There have been many literature reports on the treatment of scutellarin in cardiovascu...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/00C07C215/10C07C213/08A61K31/7048A61P9/00
Inventor 张伟杨兆祥普俊学张国丽刘一丹
Owner KPC PHARM INC
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