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Ligustrazine salt

A technology of ligustrazine and methanesulfonic acid, applied in the salt field of ligustrazine, can solve problems such as unfavorable preservation and preparation preparation, easy sublimation of hygroscopicity and the like

Inactive Publication Date: 2009-09-30
沈阳华泰药物研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Ligustrazine itself is hygroscopic and easy to sublimate. In the pharmaceutical industry, drugs of this nature are unfavorable in terms of preservation and preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1. Preparation of ligustrazine mesylate

[0018] Preparation of ligustrazine: Dissolve 100 g of ligustrazine hydrochloride (commercially available) in 1500 mL of water, adjust the solution to pH 12 with 20% NaOH aqueous solution, a large amount of white solid precipitates out, extract with 1500 mL of dichloromethane, separate the organic layer, anhydrous It was dried over sodium sulfate, and the solvent was evaporated to obtain 57.5 g of free ligustrazine.

[0019] Preparation of ligustrazine mesylate: Dissolve 10 g of ligustrazine mesylate in 300 mL of ethyl acetate, add 4.8 ml of methanesulfonic acid dropwise while stirring, and continue stirring for 30 minutes after the addition. A solid precipitates out. Heat to reflux until the solid is completely dissolved. Cooling, crystallization, standing to obtain white needle-like crystals, filtering, washing with ethyl acetate, and vacuum drying at 60°C for 3 hours to obtain 13.4 g of white needle-like ligustrazine mesyl...

Embodiment 2

[0020] Example 2: Comparative experiment of sublimation of ligustrazine mesylate, ligustrazine phosphate and ligustrazine hydrochloride

[0021] Weigh 1g of ligustrazine phosphate (commercially available, Chinese Pharmacopoeia 2005 standard), ligustrazine hydrochloride (commercially available), and ligustrazine mesylate (prepared by the method in Example 1) respectively, and spread them on the same caliber dry to constant weight. In the weighing bottle, prepare 15 samples of each salt and dry them in an oven under normal pressure at 60℃. Weigh each salt at 0.5hr, 1.5hr, 2.5hr, 3.5hr, and 4.5hr time points. Measure the weight of three samples for each salt, record the weight loss of the sample, calculate the weight loss percentage, and use the average value to evaluate the weight loss of the salt at the time point as a percentage of the original weight. The experimental results are shown in the table 1 shown.

[0022] Weight loss percentage = (weight before the experiment-weight af...

Embodiment 3

[0026] Example 3. Preparation of Ligustrazine Mesylate Tablets

[0027] It can be prepared according to the general process of the tablet, such as the preparation of 45mg / tablet of ligustrazine mesylate tablets

[0028] prescription:

[0029]

[0030] Process: Take ligustrazine mesylate, microcrystalline cellulose, and sodium carboxymethyl starch, mix uniformly, add 2% hydroxypropyl methyl cellulose to prepare soft material, granulate with 16 mesh sieve, dry at 60°C for 4 hours, Turn it over from time to time, use a 16-mesh sieve to size the dry granules, add magnesium stearate and mix evenly, then press to obtain a tablet.

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Abstract

The invention relates to a ligustrazine salt, in particular to ligustrazine mesylate and a pharmaceutical composition and use of the same. The ligustrazine mesylate of the invention has better stability than ligustrazine phosphate and ligustrazine hydrochloride.

Description

Technical field [0001] The present invention relates to a salt of ligustrazine, in particular, the present invention relates to a mesylate salt of ligustrazine and its pharmaceutical composition and use. Background technique [0002] The chemical name of ligustrazine is: 2,3,5,6-tetramethylpyrazine, and its structural formula is as follows: [0003] [0004] Ligustrazine is a classic vasodilator. It has multiple mechanisms of action such as promoting NO release, anti-oxygen free radicals, and calcium antagonism. Both animal pharmacological experiments and clinical applications have confirmed that it has obvious effects of expanding blood vessels and promoting microcirculation. Chuanxiong Phosphate Zine, injections, and tablets have been included in the 2005 edition of the Chinese Pharmacopoeia (page 868 of the 2005 edition of the second edition of the Chinese Pharmacopoeia). Ligustrazine has a variety of pharmacological effects on the cardiovascular system and is widely used. C...

Claims

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Application Information

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IPC IPC(8): C07D241/12A61K31/496A61K9/20A61K9/48A61P9/08
Inventor 王鹏
Owner 沈阳华泰药物研究有限公司
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