Eutectic of nifedipine and isonicotinamide

A technology of nifedipine and isonicotinamide, which is applied in the field of co-crystal of nifedipine and isonicotinamide and its preparation, can solve problems such as skin damage and generation of impurities, achieve easy crystallization process, good reproducibility, and preparation The effect of simple method

Active Publication Date: 2018-11-13
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, with the deepening of research, it is found that the dihydropyridine ring in the structure of this type of drug is easily oxidized into a pyridine ring, resulting in impurities, which have a certain harmful effect on the skin

Method used

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  • Eutectic of nifedipine and isonicotinamide
  • Eutectic of nifedipine and isonicotinamide
  • Eutectic of nifedipine and isonicotinamide

Examples

Experimental program
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Effect test

Embodiment 1

[0066] Co-crystal of nifedipine and isonicotinamide

[0067] At room temperature, form a saturated solution of isonicotinamide (12.2g) in 200mL of methyl isobutyl ketone solution, filter and take out the supernatant, add nifedipine (46.1g) powder to it, and suspend until it forms Supersaturated state, centrifugation and filtration, to obtain the co-crystal of nifedipine and isonicotinamide (33.6g). The prepared co-crystal was characterized by X-ray single crystal diffraction. The X-ray single crystal diffraction structure diagram of the co-crystal of nifedipine and isonicotinamide is shown in figure 1 , The results of X-ray single crystal diffraction showed that the molar ratio of nifedipine and isonicotinamide was 1:1. The crystal form of the co-crystal of nifedipine and isonicotinamide is monoclinic, and the space group is P2 1 / n, the cell parameters are: α=90°; β=90.080(5)°; γ=90°, the unit cell volume is

[0068] Also adopt X-ray powder diffraction (XRPD), therm...

Embodiment 2

[0070] Co-crystal of nifedipine and isonicotinamide

[0071] At room temperature, form a saturated solution of nifedipine (34.6g) in 200mL of methyl isobutyl ketone solution, filter the supernatant, add isonicotinamide (12.2g) powder to it, and suspend until it forms Supersaturated state, centrifugation and filtration to obtain a co-crystal of nifedipine and isonicotinamide (35.1 g).

Embodiment 3

[0073] Co-crystal of nifedipine and isonicotinamide

[0074] At room temperature, form a saturated solution of isonicotinamide (30.5g) in 250mL of methanol solution, filter and take out the supernatant, add nifedipine (86.5g) powder to it, suspend until supersaturated state is formed, centrifuge and filtration to obtain a co-crystal of nifedipine and isonicotinamide (90.6 g).

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Abstract

The invention relates to an eutectic of nifedipine and isonicotinamide and a preparation method and an application thereof. The eutectic of nifedipine and isonicotinamide is characterized by X-ray single crystal diffraction analysis, X-ray powder diffraction analysis, thermogravimetric analysis, differential scanning calorimetry, infrared spectroscopy and the like, and the eutectic is found to have the advantage of higher light stability than the nifedipine. The preparation method of the eutectic of nifedipine and isonicotinamide is simple, can be easily controlled, is good in reproducibility,and can obtain the stable eutectic of nifedipine and isonicotinamide.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and crystallization technology, in particular to a co-crystal of nifedipine and isonicotinamide and a preparation method and application thereof. Background technique [0002] The chemical name of Nifedipine is: 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate (1 ,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester), its chemical structure is as follows: [0003] [0004] Nifedipine is the first dihydropyridine calcium ion blocker antihypertensive drug launched in 1975. The drug mainly inhibits extracellular calcium ion influx by blocking calcium ion channels on the membranes of cardiac muscle and vascular smooth muscle cells. , so that the intracellular calcium ion concentration is reduced, thereby achieving the effect of lowering blood pressure. However, with the deepening of research, it is found that the dihydropyridine ri...

Claims

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Application Information

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IPC IPC(8): C07D211/90C07D213/81A61K31/4422A61K47/22A61P9/00A61P9/12
CPCA61K47/22C07B2200/13C07D211/90C07D213/81A61K31/4422A61P9/00A61P9/12
Inventor 梅雪锋余琦慧王建荣
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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