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Aripiprazole pharmaceutical co-crystal and preparation method thereof

An aripiprazole and drug technology, applied in the field of aripiprazole drug co-crystal and preparation thereof, can solve the problems of adverse reactions, poor solubility of aripiprazole, etc., and achieve the advantages of reducing solubility and muscle irritation. Effect

Active Publication Date: 2021-07-13
JIANGSU OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aripiprazole has a better clinical effect, but there are also application defects. When it is used at a normal therapeutic dose, a series of adverse reactions will occur, such as headache, anxiety, insomnia, akathisia, etc.
In addition, the solubility of aripiprazole is poor, and the solubility of the most soluble form in water is reported to be 0.045 mg / L at 25 °C

Method used

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  • Aripiprazole pharmaceutical co-crystal and preparation method thereof
  • Aripiprazole pharmaceutical co-crystal and preparation method thereof
  • Aripiprazole pharmaceutical co-crystal and preparation method thereof

Examples

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preparation example Construction

[0019] The preparation method of aripiprazole drug co-crystal, the method is a grinding method, which specifically includes the following steps: putting aripiprazole and resveratrol into a mortar for grinding in equimolar amounts, and adding a ketone or alkyl nitrile solvent before grinding , manual grinding for 30min, in Vacuum-dried to obtain the drug co-crystal of aripiprazole.

[0020] The mass ratio of aripiprazole to resveratrol is 1:1. The co-crystal of aripiprazole and resveratrol is used in the preparation of various antipsychotic drugs, and the schizophrenia includes positive symptoms, negative symptoms, cognitive impairment and bipolar disorder.

[0021] The instrument that detects drug eutectic structure and performance among the present invention is as follows:

[0022] 1. X-ray powder diffractometer, produced by PANalytical Company in the Netherlands, model X’Pert PRO MPD, Cu-K(α), tube voltage 40kV, tube current 40mA, scanning speed 2° / min;

[0023] 2. Diffe...

Embodiment 1

[0027] Accurately weigh 224 mg (0.5 mmol) of aripiprazole and 114 mg (0.5 mmol) of resveratrol, place them in a mortar, add acetonitrile dropwise and grind for 30 min to obtain a white powder, dry in vacuum at 50°C for 4 h, and collect the solid, namely It is the co-crystal of aripiprazole and resveratrol (ARI-RSV).

Embodiment 2

[0029] Accurately weigh 224mg (0.5mmol) of aripiprazole and 114mg (0.5mmol) of resveratrol, put them in a mortar, add methyl isobutyl ketone dropwise and grind for 30min to obtain a white powder, and dry in vacuum at 50°C for 4h , to collect the solid, which is the co-crystal of aripiprazole and resveratrol (ARI-RSV).

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Abstract

The invention discloses an aripiprazole pharmaceutical co-crystal and a preparation method thereof. The aripiprazole pharmaceutical co-crystal is formed through intermolecular hydrogen bonds by taking aripiprazole as an active pharmaceutical ingredient and resveratrol as a precursor. The preparation method of the aripiprazole pharmaceutical co-crystal comprises the following steps: grinding aripiprazole and resveratrol in a mortar with equal mole, adding a ketone or alkyl nitrile solvent before grinding, manually grinding for 30 minutes, and drying in vacuum to obtain the aripiprazole pharmaceutical co-crystal. A powder dissolution experiment of aripiprazole and resveratrol shows that the dissolution rate of aripiprazole is slowed down in an acetic acid buffer solution with the pH value of 4.0 and a phosphoric acid buffer solution with the pH value of 6.8, and a potential slow release effect is shown, so that the muscle injection prepared from the aripiprazole eutectic crystal can be used for treating schizophrenia in a long-acting manner, can be used for preventing and treating the schizophrenia, and reduces the muscle irritation.

Description

technical field [0001] The invention relates to the field of drug co-crystals, in particular to an aripiprazole drug co-crystal and a preparation method thereof. Background technique [0002] At room temperature, active pharmaceutical ingredients exist in various solid forms, such as polymorphs, solvates, hydrates, co-crystals, amorphous forms, and salts. The efficacy of a drug depends largely on the physical and chemical properties of the drug itself and the selected dosage form, and the different solid forms of the drug have an impact on the solubility, stability, dissolution rate and bioavailability of the drug; drug co-crystals are based on Principles of supramolecular chemistry, that is, molecular recognition and supramolecular self-assembly through intermolecular synergy. The active pharmaceutical ingredient (API) self-assembles with a suitable cocrystal former (CCF) through hydrogen bonds, or non-covalent bonds with saturation and directionality (such as van der Waal...

Claims

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Application Information

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IPC IPC(8): C07D215/22C07C39/21C07C37/84A61P25/18
CPCC07D215/22C07C39/21A61P25/18
Inventor 郝超刘文文陈寅张桂森
Owner JIANGSU OCEAN UNIV
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