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Acetaminophen-piracetam 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 stability, and achieve the effects of avoiding crystal form transformation, high feasibility and improving therapeutic effect.

Active Publication Date: 2021-12-28
HEBEI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to provide a kind of paracetamol-piracetam drug co-crystal and preparation method thereof, to solve the problem of existing piracetam drug crystal Unsatisfactory stability problems

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Put 0.015mol of paracetamol and 0.025mol of piracetam 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 25°C for 5 days, and take out the mixed solution , filtered, and the obtained white crystals are paracetamol-piracetam drug cocrystals.

[0029] Carry out product detection, the detection method is the detection of powder diffraction, scanning electron microscope, infrared spectrum, thermogravimetry and differential scanning calorimetry data, the measured data is all different from the known parameters of individual piracetam and acetaminophen The same, so it is considered that the obtained product is a co-crystal of the two.

[0030] 1. Powder crystal data

[0031] 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 respec...

Embodiment 2

[0043] Put 0.015mol of acetaminophen and 0.03mol of piracetam 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 23°C for 8 days, and take out the mixed solution , filtered, and the obtained white crystals are paracetamol-piracetam drug cocrystals.

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

Embodiment 3

[0046] Put 0.015mol of paracetamol and 0.0225mol of piracetam 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 27°C for 3 days, and take out the mixed solution , filtered, and the obtained white crystals are paracetamol-piracetam drug cocrystals.

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

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Abstract

The invention provides an acetaminophen-piracetam pharmaceutical co-crystal and a preparation method thereof, wherein the chemical formula of the co-crystal is C8H9NO2.C6H10N2O2. The preparation method comprises the following steps: putting acetaminophen and piracetam into a container filled with a methanol or acetonitrile solvent according to a molar ratio of 1:(1.5-2), oscillating at a constant temperature of 23-27 DEG C for 3-8 days, taking out a mixed solution, and filtering to obtain a white crystal, namely the acetaminophen-piracetam pharmaceutical co-crystal. According to the invention, the method is simple to operate and can be applied on a large scale; by introducing a co-crystal forming substance acetaminophen, the thermal stability of piracetam is enhanced, and the co-crystal weight loss temperature is obviously higher than that of a piracetam monomer; and acetaminophen belongs to nervous system drugs, and the combination of the acetaminophen and piracetam 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-piracetam drug co-crystal and a preparation method thereof. Background technique [0002] The chemical name of Piracetam is 2-oxo-1-pyrrolidinylacetamide, and its structural formula is as follows: [0003] [0004] Piracetam (PINA) is a new drug for promoting thinking and memory. It has a protective effect on brain hypoxic damage and promotes the recovery of damaged brain. Memory loss and mild to moderate brain dysfunction caused by various reasons. [0005] Drug co-crystal is based on the background of crystal engineering and supramolecular chemistry theory, combined with intermolecular forces, through molecular recognition and self-assembly, the drug active ingredient (API) and co-crystal former (CCF) which are solid at room temperature ) complexed at a fixed stoichiometric ratio to obtain new crystals. Although there are some reports about co-cry...

Claims

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Application Information

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IPC IPC(8): C07C233/25C07D207/27A61P29/00A61P25/00A61P9/10A61P25/28A61P9/00
CPCC07C233/25C07D207/27A61P29/00A61P25/00A61P9/10A61P25/28A61P9/00C07B2200/13
Inventor 刘海芬程广澳赵慧波李彦磊
Owner HEBEI UNIVERSITY
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