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L-aspartic acid L-amlodipine crystal form, preparation method and use thereof

A technology of L-amlodipine and aspartic acid, which is applied in the field of medicine, can solve the problems of lack of research reports on L-aspartic acid and L-amlodipine, and achieve the effect of high purity

Active Publication Date: 2015-12-02
GUANGDONG XIANQIANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there is no research report on the crystal form of L-aspartic acid levamlodipine at home and abroad

Method used

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  • L-aspartic acid L-amlodipine crystal form, preparation method and use thereof
  • L-aspartic acid L-amlodipine crystal form, preparation method and use thereof
  • L-aspartic acid L-amlodipine crystal form, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 20.5g of levoamlodipine and 200mL of methanol into a 1000ml reaction flask, then add 7.3g of L-aspartic acid, and stir at room temperature for 16h; the reaction system is heated to reflux for 4h, filtered while it is hot, and the filtrate is added with 200ml of ethyl acetate to cool down Stir and crystallize at 0-10°C; filter and dry the wet product in vacuum to obtain 25 g of light yellow crystals. The purity measured by HPLC is 99.9%, and the X-diffraction spectrum of this crystal form is shown in figure 1 , see the infrared spectrum figure 2 .

Embodiment 2

[0027] Add 20.5g of levoamlodipine and 200mL of ethanol into a 1000ml reaction flask, then add 7.3g of L-aspartic acid, and stir at room temperature for 14h; the reaction system is heated to reflux for 5h, filtered while it is hot, and the filtrate is added with 200ml of ethyl acetate to cool down Stir and crystallize at 5-10°C; filter and dry the wet product in vacuum to obtain 22 g of light yellow crystals. The purity determined by HPLC is 99.9%, and its X-diffraction spectrum and infrared spectrum are similar to those of Example 1.

Embodiment 3

[0029] Add 20.5g of levamlodipine and 200mL of ethyl acetate into a 1000ml reaction flask, then add 7.3g of L-aspartic acid, and stir at room temperature for 12h; the reaction system is heated to reflux for 7h, filtered while hot, and 200ml of ethyl acetate is added to the filtrate , cooled to 5-10°C, stirred and crystallized; filtered, and the wet product was vacuum-dried to obtain 26g of light yellow crystals. The purity determined by HPLC is 99.7%, and its X-diffraction spectrum and infrared spectrum are similar to those in Example 1.

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to an L-levamlodipine aspartate crystal form, as well as a preparation method and application thereof. According to the L-levamlodipine aspartate crystal form, Cu-K alpha radiation is used, and characteristic peaks of X-ray diffraction at 3.7+ / -0.2 degrees, 10.9+ / -0.2 degrees, 12.3+ / -0.2 degrees, 13.1+ / -0.2degrees, 13.9+ / -0.2 degrees, 18.3+ / -0.2 degrees, 21.4+ / -0.2 degrees, 23.6+ / -0.2 degrees, 24.1+ / -0.2 degrees and 25.2+ / -0.2 degrees are indicated by an angle 2-theta.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to 4S-(-)-3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-1,4 - Crystal form, preparation method and use of dihydro-6-methyl-3,5-pyridinedicarboxylate (L)-aspartate (ie L-aspartic acid L-amlodipine). Background technique [0002] Amlodipine, whose structural formula is shown in formula 1, is a new generation of calcium ion antagonist, which was developed by Pfizer in 1986 and first listed in the UK in 1990. The product is IstinTabS. It went on the market in my country in 1993 under the trade name Norvasc. Amlodipine effectively overcomes the shortcomings of the second-generation calcium ion antagonists diltiazem and nifedipine that are unstable in reducing blood pressure and have large adverse reactions. Amlodipine is clinically used for the treatment of hypertension and stable angina pectoris, and has the characteristics of remarkable curative effect, stable onset of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/90C07C229/24C07C227/30A61K31/4422A61P9/12
CPCC07D211/90
Inventor 郑玉春孙晔张志生杜丽丽王雪志彭如清
Owner GUANGDONG XIANQIANG PHARMA