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Acegastrodine compound as well as preparation method, preparation and application thereof
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A technology of acetylgastrodin and its compounds, which is applied in the field of acetylgastrodin compounds and their preparation, can solve problems such as the stable existence of gastrodin, increase the safety risk of acetylgastrodin, limit the clinical use of gastrodin, etc., and achieve drug efficacy and Improved safety, simplified preparation and post-treatment process, and improved bioavailability
Active Publication Date: 2017-10-24
KPC PHARM INC
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[0004] In the 1980s, Kunming Pharmaceutical Group Co., Ltd. carried out structural transformation of gastrodin, and exclusively developed highly active acetylgastrodin with high fat solubility and positive therapeutic effects on central nervous system, cardiovascular and cerebrovascular system diseases. (Acetagastrodin), because the stability of acetylgastrodin is relatively poor, in order to solve t
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[0032] The preparation method of the acetylgastrodin compound of the present invention is prepared by reacting acetylgastrodin and urea in an organic solvent system, and the organic solvent is alcohols, ketones, alkyl nitriles and cyclic ethers. one or more.
[0033] The mass ratio of acetylgastrodin and urea is 6-10:1.
[0034] The alcohols are ethanol; the ketones are acetone.
[0035] The preparation of the acetylgastrodin compound of the present invention is prepared by adding pharmaceutically acceptable auxiliary materials to the acetylgastrodin compound to prepare powders, granules, tablets, capsules and pills.
[0036] The application of the acetylgastrodin compound in the present invention is the application of the acetylgastrodin compound in the preparation of drugs for the prevention / treatment of cardiovascular and cerebrovascular diseases.
[0037] The present invention will be further described below with specific implementation case:
[0038] In the following e...
Embodiment 1
[0058] Preparation of acetylgastrodin and urea cocrystal compound:
[0059] Dissolve 4.54g of acetylgastrodin in 20mL of ethanol, add 0.6g of urea, heat to 60°C, stir at 60°C for 60min, then cool down to 5°C, filter after the reaction, wash the obtained solid with ethanol, and dry , to collect the solid. After testing, the solid obtained in this embodiment is eutectic crystal form A, and its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , and its TGA figure is shown in figure 2 ,That 1 H NMR picture as image 3 .
Embodiment 2
[0061] Preparation of acetylgastrodin and urea cocrystal compound:
[0062] Dissolve 4.54g of acetylgastrodin in 20mL of ethanol, add 0.6g of urea, heat to 60°C, stir at 60°C for 60min, then cool down to 5°C, and naturally volatilize the ethanol solvent after the reaction, the obtained solid Wash with ethanol and dry. After testing, the solid obtained in this example is consistent with the crystal form obtained in Example 1, which is eutectic crystal form A.
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Abstract
The invention discloses an acegastrodine compound as well as a preparation method, a preparation and application thereof. The acegastrodine compound is eutectic crystal of a compound in a formula (I) and urea, wherein the structural formula of the compound in the formula (I) is as shown in the specification (I). The preparation method is reaction of acegastrodine and the urea in an organic solvent system, wherein an organic solvent is one or more of alcohols, ketones, alkyl nitrile and cyclic ethers. The preparation is powder, a granule, a tablet, a capsule or a pill prepared by adding pharmaceutically acceptable auxiliary materials to the acegastrodine compound. The application is an application of the acegastrodine compound in preparation of drugs for preventing/treating cardiovascular and cerebrovascular diseases. The eutectic crystal of the acegastrodine and the urea is high in solubility and is beneficial to improvement of the drug absorption efficiency and improvement of the bioavailability of the drugs, and is of great significance in improvement of the curative effects and the security of the drugs.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an acetylgastrodin compound and its preparation method, preparation and application. Background technique [0002] Acetyl gastrodin: English name is Acetagastrodin, CAS: 105054-56-6, molecular formula: C21H26O11, molecular weight: 454.42, chemical name: 4-hydroxymethylbenzene-2ˊ, 3ˊ, 4ˊ, 6ˊ-tetra-ο-acetyl-β -D-glucopyranoside. [0003] Gastrodin is extracted from the dried root of the orchid plant Gastrodia elata, and the origin of the raw material is Yunnan. It has good sedative and sleeping effects, and can relieve neurasthenia, insomnia, and headache symptoms. The traditional Chinese medicine Gastrodia elata can treat headache, dizziness, limb numbness, convulsions and convulsions. Clinical application: treatment of vertebral-basilar artery insufficiency; treatment of vestibular neuronitis; treatment of vertigo. [0004] In the 1980s, Kunming Pharmaceutical Gr...
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