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Galanthamine pamoic acid salt and preparation method thereof

A technology of galantamine and pamolate, applied in the field of galantamine pamoate and its preparation, can solve the problems of low solubility property, stable dissolution performance, low solubility property, light resistance, poor stability and the like , to achieve the effects of excellent solubility and stability, high product yield, and improved stability

Active Publication Date: 2020-06-05
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problems of high solubility and poor stability of existing galantamine salt and galantamine hydrobromide salt, the present invention aims to provide a kind of galantamine with low solubility characteristics, good light fastness and good stability. Galantamine pamolate, the compound has low solubility, good stability and good dissolution performance, and the preparation method of the compound is simple and convenient, suitable for industrial production

Method used

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  • Galanthamine pamoic acid salt and preparation method thereof
  • Galanthamine pamoic acid salt and preparation method thereof
  • Galanthamine pamoic acid salt and preparation method thereof

Examples

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Effect test

Embodiment 1

[0033] Dissolve 1.14 g of galantamine hydrobromide in 25 mL of dimethyl sulfoxide, add dropwise 100 mL of a dimethyl sulfoxide solution containing 1.41 g of pamoic acid, and after the drop is complete, stir and react at 25°C for 6 hours; The liquid was cooled to 0-5°C and stood at this temperature for 24 hours, vacuum filtered, and vacuum-dried at 50°C for 12 hours to obtain a light yellow powder with a yield of 78.55% and a purity of 99.91%.

Embodiment 2

[0035] Dissolve 1.14g of galantamine hydrobromide in 25mL of N,N-dimethylformamide, add dropwise 150mL of N,N-dimethylformamide solution containing 2.57g of pamoic acid, dropwise, at 60°C Stir the reaction for 2 hours; after the reaction, cool the reaction solution to 0-5°C and let it stand at this temperature for 48 hours, vacuum filter, and vacuum-dry at 50°C for 12 hours to obtain a light yellow powder with a yield of 75.28% and a purity of is 99.87%.

Embodiment 3

[0037] Dissolve 1.14 g of galantamine hydrobromide in 15 mL of 1,3-dimethyl-2-imidazolinone, and add dropwise 1,3-dimethyl-2-imidazolidinone containing 1.17 g of pamoic acid Solution 150mL, after dripping, stirred at 15°C for 10 hours; put the reaction solution in an environment of 0-5°C for 24 hours, filtered it with suction, and dried it under vacuum at 50°C for 2 hours to obtain a light yellow powder with a yield of 72.35 %, the purity is 99.83%.

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Abstract

The invention provides a galanthamine pamoic acid salt and a preparation method thereof, the compound has a structure shown in formula I, and has good dissolution characteristic and good stability, and a tablet prepared by using the compound as an active ingredient has slow dissolution performance and embodies an excellent slow release effect. In addition, the galanthamine pamoic acid salt provided by the invention has the advantages of simple preparation process, high product yield and high purity, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a galantamine pamolate, a preparation method thereof and its application in pharmacy. Background technique [0002] Galantamine was first isolated by Mashkovsky, a pathologist in the former Soviet Union, from the Amaryllidaceae plant Snowdrop woerneri. As a second-generation AchE inhibitor, galantamine mainly acts on the catalytic site of AchE. The structure-activity relationship is as follows: (1) the hydroxyl group in the molecular structure forms a hydrogen bond with Glu199 in AchE, and the double bond of the cyclohexene ring forms a hydrogen bond with Glu199 in AchE. Trp84 in AChE forms a p-p bond, thereby inhibiting AchE; (2) The modification of the N-terminal alkylation in the molecular structure is conducive to approaching the bottom of the catalytic site of AchE, which plays a very important role in the inhibition of AchE. [0003] The compound of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/107A61K31/55A61P25/28
CPCC07D491/107A61P25/28
Inventor 杜丽平朱鹏
Owner LUNAN PHARMA GROUP CORPORATION
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