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Acetaminophen-ibuprofen pharmaceutical co-crystal and preparation method thereof

A technology for paracetamol and acetaminophen, which is applied in the field of pharmaceutical crystal forms, can solve problems such as unsatisfactory crystal solubility, and achieve the effects of avoiding crystal form transformation, reducing interference effects, and simple and effective operation.

Active Publication Date: 2022-02-11
HEBEI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a paracetamol-ibuprofen drug co-crystal and preparation method thereof, to solve the problem of unsatisfactory solubility of existing ibuprofen drug crystals

Method used

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  • Acetaminophen-ibuprofen pharmaceutical co-crystal and preparation method thereof
  • Acetaminophen-ibuprofen pharmaceutical co-crystal and preparation method thereof
  • Acetaminophen-ibuprofen pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Put 0.015mol of acetaminophen and 0.015mol of ibuprofen into a 50mL Erlenmeyer flask, inject 25mL of methanol solvent, seal the Erlenmeyer flask with a rubber stopper, put it into a constant temperature oscillator at 25°C for 5 days, and take out the mixed solution. After filtering, the obtained white crystals are paracetamol-ibuprofen drug cocrystals.

[0026] Carry out product detection, detection method is powder diffraction, scanning electron microscope, infrared spectrum, thermogravimetry and high-performance liquid chromatography detection, and the measured data are all different from the known parameters of independent piracetam and acetaminophen, so The resulting product is believed to be a co-crystal of both.

[0027] 1. Powder crystal data

[0028] The X-ray powder diffraction measurement adopts Bruker D8 advance X-ray powder diffractometer, and the measurement process uses Cu-Kα rays The working voltage and current are 40kV and 40mA, respectively, the scan...

Embodiment 2

[0043]Put 0.015mol of acetaminophen and 0.03mol of ibuprofen into a 50mL Erlenmeyer flask, inject 25mL of methanol solvent, seal the Erlenmeyer flask with a rubber stopper, put it in a constant temperature oscillator at 22°C for 10 days, and take out the mixed solution. After filtering, the obtained white crystals are paracetamol-ibuprofen drug cocrystals.

[0044] Carry out product detection, detection method is the detection of powder diffraction, scanning electron microscope, infrared spectrum, thermogravimetry and high-performance liquid chromatography data, and the result shows that it has similar performance with embodiment 1 product.

Embodiment 3

[0046] Put 0.015mol of acetaminophen and 0.0225mol of ibuprofen into a 50mL Erlenmeyer flask, inject 25mL of methanol solvent, seal the Erlenmeyer flask with a rubber stopper, put it in a constant temperature oscillator at 28°C for 4 days, and take out the mixed solution. After filtering, the obtained white crystals are paracetamol-ibuprofen drug cocrystals.

[0047] Carry out product detection, detection method is powder diffraction, scanning electron microscope, infrared spectrum, thermogravimetry and high-performance liquid chromatography data detection, and the result shows that it has similar performance with embodiment 1 product.

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Abstract

The invention provides an acetaminophen-ibuprofen pharmaceutical co-crystal and a preparation method of the acetaminophen-ibuprofen pharmaceutical co-crystal. The chemical formula of the co-crystal is C8H9NO2.C13H18O2. The preparation method comprises the following steps: putting acetaminophen and ibuprofen into a container filled with a methanol or acetonitrile solvent according to a molar ratio of 1:(1-2), conducting oscillating at a constant temperature of 22-28 DEG C for 4-10 days, taking out a mixed solution, and conducting filtering to obtain a white crystal, namely the acetaminophen-ibuprofen pharmaceutical co-crystal. The method is easy to operate and can be used for batch production and application. Meanwhile, the eutectic formation, namely acetaminophen, is introduced, so that the solubility of the ibuprofen is enhanced, and the solubility of the ibuprofen in the eutectic is obviously higher than that of an ibuprofen monomer. In addition, the acetaminophen and the ibuprofen belong to nervous system medicines, and the combination of the acetaminophen and the ibuprofen further improves the treatment effect.

Description

technical field [0001] The invention relates to the technical field of drug crystal forms, in particular to a paracetamol-ibuprofen drug co-crystal and a preparation method thereof. Background technique [0002] Ibuprofen (IBUP) belongs to nervous system drugs, has anti-inflammatory, antipyretic and analgesic effects, and is widely used in medical fields such as arthritis and wound pain. The molecular formula is C 13 h 18 o 2 , also known as ibuprofen, is insoluble in water but easily soluble in organic solvents such as ethanol, methanol, ethyl acetate, acetone, etc. Its chemical structure is as follows: [0003] [0004] Acetaminophen (APAP) belongs to the nervous system drugs, mainly treats migraine, has antipyretic and analgesic effects, and its molecular formula is C 8 h 9 NO 2 , usually white crystalline powder, the structural formula is as follows: [0005] [0006] Pharmaceutical co-crystal is based on the background of crystal engineering and supramolecul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/25C07C57/30C07C231/24C07C51/43C08G83/00
CPCC07C233/25C07C57/30C08G83/008C07B2200/13
Inventor 刘海芬闫芹芹闫军颖
Owner HEBEI UNIVERSITY
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