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Eutectic crystal of nicorandil and salicylic acid as well as preparation method and application of eutectic crystal

A technology of nicorandil and salicylic acid, which is applied in the co-crystal of nicorandil and salicylic acid and its preparation field, can solve the problem of deterioration and achieve low cost, good reproducibility and easy process control Effect

Active Publication Date: 2020-08-25
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 salicylic acid as well as preparation method and application of eutectic crystal
  • Eutectic crystal of nicorandil and salicylic acid as well as preparation method and application of eutectic crystal
  • Eutectic crystal of nicorandil and salicylic acid as well as preparation method and application of eutectic crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Suspension preparation of co-crystals of Nicorandil and salicylic acid

[0051] Take by weighing nicorandil crude drug 47.0g, take by weighing salicylic acid crude drug 20.4g, add 1L water, stir at room temperature, obtain the eutectic 43.4g of nicorandil and salicylic acid, yield 55.9% (in terms of nicorandil) Kedier dosing meter).

[0052] For the cocrystal of Nicorandil and salicylic acid prepared in Example 1, X-ray powder diffraction (XRPD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and infrared (IR) After characterization by spectroscopic solid-state chemistry, the results are shown in figure 1 , 2, 3 and 4.

Embodiment 2

[0053] Example 2: Suspension preparation of co-crystals of Nicorandil and salicylic acid

[0054] Take by weighing 47.0g of Nicorandil bulk drug, take by weighing 20.4g of salicylic acid bulk drug, add 1L of water, stir at 4°C to obtain 43.4g of the eutectic of Nicorandil and salicylic acid, yield 61.7% (with Nicorandil dosing meter).

Embodiment 3

[0055] Embodiment 3: suspension prepares the eutectic of nicorandil and salicylic acid

[0056] Take by weighing 42.2g of Nicorandil bulk drug, 13.8g of salicylic acid bulk drug, add 0.7L of water, stir at 4°C, obtain 30.2g of the eutectic of Nicorandil and salicylic acid, yield 43.3% ( Based on the dosage of Nicorandil).

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Abstract

The invention provides a eutectic crystal of nicorandil and salicylic acid as well as a preparation method and application of the eutectic crystal. According to the invention, the eutectic crystal ofnicorandil and salicylic acid is comprehensively characterized by using 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 active pharmaceutical ingredient, and the safety, effectiveness and quality controllability of the medicine are improved.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry and crystallization technology, and specifically relates to a co-crystal of nicorandil and salicylic acid as well as its preparation method and application. Background technique [0002] Nicorandil, also known as Nicorandil, Nicotinate, chemical name: 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 continu...

Claims

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Application Information

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IPC IPC(8): C07D213/82C07C65/10C07C51/42C07C51/43A61K31/455A61P9/12A61P9/10A61P9/00
CPCC07D213/82C07C65/10C07C51/42C07C51/43A61P9/12A61P9/10A61P9/00C07B2200/13
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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