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Co-crystal of nifedipine and isonicotinamide

The technology of nifedipine and isonicotinamide is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, drug combinations, etc., which can solve the problems of skin damage, generation of impurities, etc., and achieves easy crystallization process, Good reproducibility and simple preparation method

Active Publication Date: 2021-11-02
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Co-crystal of nifedipine and isonicotinamide
  • Co-crystal of nifedipine and isonicotinamide
  • Co-crystal of nifedipine and isonicotinamide

Examples

Experimental program
Comparison scheme
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 a co-crystal of nifedipine and isonicotinamide, its preparation method and application. The co-crystal of nifedipine and isonicotinamide was comprehensively characterized by means of X-ray single crystal diffraction analysis, X-ray powder diffraction analysis, thermogravimetric analysis, differential scanning calorimetry analysis, and infrared spectroscopy, and it was found that the Compared with nifedipine, the co-crystal has the advantage of higher light stability. The preparation method of the co-crystal of nifedipine and isonicotinamide is simple, easy to control and good in reproducibility, and stable co-crystal of nifedipine and isonicotinamide can be obtained.

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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Patent Type & Authority Patents(China)
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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