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Flavonoid compound, preparation method and application thereof

A compound and composition technology, applied in the field of medicinal chemistry, can solve the problems of carrier materials such as limited drug loading capacity, adverse effects on drug safety and stability, failure to improve the water solubility of dehydrated icariin, etc., to achieve improved Bioavailability, broadening the dosage form of clinical application, and improving the effect of water solubility

Inactive Publication Date: 2015-05-06
周亚伟
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above method fails to improve the water solubility of dehydrated icariin itself, and the carrier material has a limited ability to load the drug, and the introduction of various solvents or carrier materials will adversely affect the safety and stability of the drug, and The preparation process is complex and the cost is high, which limits its popularization and application

Method used

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  • Flavonoid compound, preparation method and application thereof
  • Flavonoid compound, preparation method and application thereof
  • Flavonoid compound, preparation method and application thereof

Examples

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preparation example Construction

[0055] Preparation and identification of embodiment 1 formula II compound

[0056] 1. Sources of raw materials and reagents

[0057] Table 1 Sources of raw materials and reagents

[0058]

[0059]

[0060] 2, the preparation of L-carnitine acid chloride

[0061] According to the preparation method of Example 2 disclosed in Chinese Patent No. 200810014212.X, the L-carnitine acid chloride was prepared. Take 3g (0.015mol) of L-carnitine hydrochloride, add 10ml of trifluoroacetic acid, stir to dissolve, add 4.3mL of acetyl chloride in portions at 0°C, raise the temperature to 45-50°C after dropping, and keep the reaction for 20 hours. After the reaction, take it out and cool to room temperature, add 100ml of acetone, stir for 2 hours, filter, add 100ml of diethyl ether to the filtrate, stir until a white precipitate precipitates, put it in the refrigerator for 12 hours. After taking it out, stir for 1 hour, filter, and dry to obtain 5.36 g of white solid, which is acetyl-...

Embodiment 4

[0090] Preparation of formula II compound tablet

[0091] Take 50g of the compound of formula II, grind it and pass it through an 80-mesh sieve, add 50g of microcrystalline cellulose and mix evenly, add 2% hypromellose as a binder to make a soft material, granulate and dry, add a disintegrant 4% sodium carboxymethyl starch and 0.5% magnesium stearate as a lubricant, mixed evenly, and compressed into tablets. Each tablet contains 0.05g of the compound of formula II, administered orally, 3 times a day, 1 tablet each time.

Embodiment 5

[0093] The preparation of formula II compound injection

[0094] Take 100g of the compound of formula II, add an appropriate amount of water for injection to dissolve, add the prepared amount of 0.02% activated carbon, stir for 5-10min, filter, dilute the filtrate to about 10L, add sodium chloride to adjust the osmotic pressure to isotonicity, and adjust the pH to 7.5- 8.0, ultrafiltration, potting into 1000 vials (10ml / vial), sterilized, and packaged to obtain the compound injection of formula II. Injection administration, 2 times a day, 1 stick each time.

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Abstract

The invention relates to a water soluble derivative of anhydroicaritin and a preparation method thereof, in particular to a flavonoid compound, a preparation method and application thereof. The derivative on the one hand retains the anhydroicaritin's pharmacological activity for treatment of coronary heart disease, cerebral ischemia and cerebral infarction, also improves the water solubility of anhydroicaritin, thus being widely applicable to solutions, injections or granules and other various pharmaceutical preparations for clinical use, and providing a new drug choice for clinical prevention and / or treatment of coronary heart disease, cerebral ischemia or cerebral infarction. In addition, the preparation method of the compound provided by the invention or its derivative or salt is simple, thus being convenient for industrial popularization and application.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a water-soluble derivative of dehydrated icariin and a preparation method thereof, and the application of the compound as an active substance in the preparation of drugs for treating coronary heart disease, cerebral infarction and cerebral infarction. Background technique [0002] Dehydrated icaritin (AICA, anhydroicaritin), also known as cycloicaritin (CIT, cycloicaritin), chemical name 5-dihydroxy-2-(4-methoxy-phenyl)-8,8- Dimethyl-9,10-dihydro-8H-pyrano[2,3-f]chromene-flavone belongs to flavonoids, the structural formula is: [0003] [0004] Dehydrated icariin can be isolated from traditional Chinese medicine Epimedium or prepared by hydrolysis of icariin. Invention patent CN1919191B discloses the application of dehydrated icariin in the preparation of drugs for the prevention and treatment of coronary heart disease and cerebral infarction. The administratio...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/352A61P9/00A61P9/10
CPCC07D493/04
Inventor 周亚伟
Owner 周亚伟
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