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Eutectic crystal of nicorandil and 1-hydroxy-2-naphthoic acid, and preparation method and application thereof

A technology of nicorandil and naphthoic acid, which is applied to the co-crystal of nicorandil and 1-hydroxy-2-naphthoic acid and its preparation field, can solve problems such as deterioration, achieve low cost, good reproducibility, The effect of chemical stability improvement

Active Publication Date: 2020-09-01
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

[0007] Through the study on the stability of nicorandil, it is found that it is prone to intramolecular nucleophilic substitution reaction [NAGAI H, KIKUCHI M, NAGANO H, et al. The stability of nicorandil in aqueous solution. I. Kinetics and mechanism of decomposition of N -(2-hydroxyethyl)nicotinamide nitrate(ester)in aqueous solution.Chemical and pharmaceuticalbulletin,1984,32(3):1063-1070.], thus deteriorating

Method used

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  • Eutectic crystal of nicorandil and 1-hydroxy-2-naphthoic acid, and preparation method and application thereof
  • Eutectic crystal of nicorandil and 1-hydroxy-2-naphthoic acid, and preparation method and application thereof
  • Eutectic crystal of nicorandil and 1-hydroxy-2-naphthoic acid, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Suspension Preparation of Co-crystals of Nicorandil and 1-Hydroxy-2-Naphthoic Acid

[0050] Weigh 22.3g of Nicorandil crude drug, weigh 15.6g of 1-hydroxy-2-naphthoic acid, add 1L of water, and stir at room temperature to obtain a co-crystal 31.9 g of Nicorandil and 1-hydroxy-2-naphthoic acid g, yield 75.8% (based on Nicorandil charging amount).

[0051] The eutectic of Nicorandil and 1-hydroxyl-2-naphthoic acid prepared in Example 1 was analyzed by X-ray powder diffraction (XRPD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) And after infrared (IR) spectroscopic solid chemical method characterization, the results are shown in figure 1 , 2, 3 and 4.

Embodiment 2

[0053] Suspension Preparation of Co-crystals of Nicorandil and 1-Hydroxy-2-Naphthoic Acid

[0054] Weigh 22.3g of Nicorandil crude drug, weigh 18.8g of 1-hydroxy-2-naphthoic acid, add 1L of water, and stir at 4°C to obtain a co-crystal of Nicorandil and 1-hydroxy-2-naphthoic acid 36.0g, the yield is 85.5% (based on the charging amount of Nicorandil).

Embodiment 3

[0056] Suspension Preparation of Co-crystals of Nicorandil and 1-Hydroxy-2-Naphthoic Acid

[0057] Weigh 21.1g of Nicorandil bulk drug, weigh 9.4g of 1-hydroxy-2-naphthoic acid, add 1L of water, and stir at 4°C to obtain a co-crystal of Nicorandil and 1-hydroxy-2-naphthoic acid 16.0g, the yield is 40.1% (based on the charging amount of Nicorandil).

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Abstract

The invention relates to a eutectic crystal of nicorandil and 1-hydroxy-2-naphthoic acid, and a preparation method and application thereof. The eutectic crystal of the nicorandil and the 1-hydroxy-2-naphthoic acid is comprehensively characterized by applying analysis means such as X-ray diffraction analysis, thermogravimetric analysis, differential scanning calorimetry analysis, infrared spectroscopy and the like. Through stability test and comparison, the eutectic crystal has more excellent damp-heat stability compared with a nicorandil raw material medicine, and the safety, effectiveness andquality controllability of the medicine are improved.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and crystallization technology, in particular to a co-crystal of nicorandil and 1-hydroxy-2-naphthoic acid, a preparation method and application thereof. Background technique [0002] Nicorandil, also known as Nicorandil, Nicotinate, its chemical name is: N-(2-hydroxyethyl)nicotinamide nitrate, N-[2-(nitrooxy)ethyl] -3-pyridinecarboxamide, its chemical structure is shown in the following formula (a): [0003] [0004] Nicorandil is a drug with a dual mechanism of action for the treatment of coronary heart disease and angina pectoris. It not only has the characteristics of nitrate drugs, but also is an ATP-sensitive potassium ion channel opener. Nicorandil contains a nitrate side chain, which can release NO in the body. By activating guanylate cyclase in vascular smooth muscle cells, it can promote the discharge of intracellular calcium ions, expand coronary blood vessels, and con...

Claims

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Application Information

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IPC IPC(8): C07D213/82C07C51/43C07C51/42C07C65/11A61P9/12A61P9/10A61P9/00A61K31/192A61K31/455
CPCC07D213/82C07C65/11A61P9/12A61P9/10A61P9/00C07B2200/13
Inventor 梅雪锋郭春阳张奇王建荣
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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