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Colchicin derivative, preparation method and application thereof

A technology for colchicine and derivatives, which is applied in the field of medicine and achieves the effects of convenient storage and transportation, good dissolution performance, and easy absorption into blood circulation

Active Publication Date: 2013-08-14
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Published literature has only reported colchicine derivatives—colchicine (C 21 h 24 N 2 o 5， Molecular weight: 384.43), so far, there is no published literature at home and abroad to report the crystalline hydrate C of the following structure 21 h 24 N 2 o 5 ·nH 2 O, n=2.5~3.5] and its preparation method and use

Method used

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  • Colchicin derivative, preparation method and application thereof
  • Colchicin derivative, preparation method and application thereof
  • Colchicin derivative, preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Example 1 Preparation of colchicamine trihydrate Put 3 grams of colchicine and 50 ml of concentrated ammonia water in a three-necked flask, stir to dissolve, control the temperature at 25-40 ° C, stir for 12 hours, concentrate under reduced pressure, and use two Extract three times with 300ml of methyl chloride, concentrate the organic layer under reduced pressure, crystallize with 1ml of ethanol, 2ml of water, 25ml of petroleum ether and dichloromethane under negative pressure, place it below 0°C, wait for the solid precipitation to complete, and filter with suction , the precipitate was washed twice with water, filtered with suction, and the obtained solid was recrystallized with 1ml of solvent ethanol, 20ml of chloroform, 2ml of water, and 20ml of petroleum ether. Dry at about ℃ for 4 hours to obtain about 1.9g of yellow crystals. Identification analysis: take 2mg on a white porcelain plate, add ethanol to dissolve it, add 3 drops of ferric chloride test solution, the...

Embodiment 2

[0041]Example 2 Preparation of colchicamine trihydrate Put 6 grams of colchicine and 120ml of water in a three-necked flask, stir, add 20g of ammonium bicarbonate, 12ml of concentrated ammonia water, stir, control the temperature at 25-50°C, and stir for 8 -16 hours, concentrate under reduced pressure, extract three times with 300ml of chloroform, concentrate the organic layer under reduced pressure, add 1.5ml of ethanol and 2ml of water under negative pressure, then add diethyl ether to make it slightly turbid, heat or add a little ethanol to redissolve, then add a small amount of diethyl ether, Place below 0°C, after the solid precipitation is complete, filter with suction, wash the precipitate twice with water, dissolve the solid with a small amount of ethanol under heating in a water bath, then add 3ml of water, 20ml of chloroform, and an appropriate amount of ether for recrystallization, and place below 0°C Place it, and after the precipitation is sufficient, filter it wit...

Embodiment 3

[0042] Example 3 Preparation of freeze-dried preparations Take 5 g of colchisamine hydrate (Example 1), add 15 g of mannitol, 4 g of sodium dihydrogen phosphate, 2 g of citric acid, 1 g of arginine hydrochloride, 3-hydroxypropyl β-cyclo Dextrin 10g, Tween-80 3ml, EDTA disodium 0.02g, add about 800ml of water for injection at 20-50℃, stir to dissolve, adjust the pH to 4.5-6.8 with about 1-5M citric acid and sodium hydroxide solution, Add water for injection to 1000ml, add activated carbon 0.01-0.5% (W / V), stir for 15-30min, filter, filter with 0.22 micron microporous membrane, pack in 5, 10mg / bottle, vacuum freeze-dry, press stopper, Get freeze-dried.

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Abstract

Provided are colchiceinamide hydrates, preparation methods thereof, and uses thereof for the prophylaxis or treatment of diseases of human beings or animals, such as leukaemia, breast cancer, stomach cancer, cervical carcinoma, nasopharyngeal carcinoma, actinic keratoma, basal-cell carcinoma, squamous cell skin carcinoma in situ.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides medicines—colchicine derivatives, their preparation methods and applications. Background technique [0002] Published literature has only reported colchicine derivatives—colchicine (C 21 h 24 N 2 o 5， Molecular weight: 384.43), so far, there is no published literature at home and abroad to report the crystalline hydrate C of the following structure 21 h 24 N 2 o 5 ·nH 2 O, n=2.5~3.5] and its preparation method and use. Contents of the invention [0003] What the present invention relates to are colchicine derivatives and preparation method thereof and application, further say, relate to colchicine crystalline hydrate [C 21 h 24 N 2 o 5 ·nH 2 O, n=2.5~3.5, n can be 2.5, 2.75, 3.0, 3.5 or the number between them] and its preparation method and application. [0004] The colchicamine containing crystal water obtained by the present invention has lower toxic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C233/41C07C231/24A61K31/16A61P35/00A61P35/02
CPCA61K31/165C07C233/41C07C2103/34A61P35/00A61P35/02C07C2603/34
Inventor 刘力
Owner 刘力
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