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A kind of aripiprazole medicine co-crystal and preparation method thereof
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A technology for aripiprazole and drugs, applied in the field of aripiprazole drug co-crystal and its preparation, can solve the problems of poor solubility and adverse reactions of aripiprazole, and achieve the goal of reducing solubility and muscle irritation Effect
Active Publication Date: 2022-04-08
广西鲲宇药业有限公司
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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
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[0018] A preparation method of aripiprazole drug co-crystal, the method is a grinding method, specifically comprising the following steps: putting aripiprazole and resveratrol in equal molar amounts into a mortar and grinding, adding ketone or alkyl Nitrile solvent, manual grinding for 30 minutes, and vacuum drying at 40-60°C to obtain the drug co-crystal of aripiprazole.
[0019] A use of aripiprazole drug co-crystal in the preparation of antipsychotic drugs, the psychosis is schizophrenia, and the schizophrenia is positive symptoms, negative symptoms, cognitive impairment and bipolar affective disorder.
[0020] The instrument that detects drug eutectic structure and performance among the present invention is as follows:
[0021] 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;
[0022] 2. Differential scanning calorimeter, German Netzsch company, m...
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 drug co-crystal and a preparation method thereof. Using aripiprazole as an active pharmaceutical ingredient and resveratrol as a precursor, the aripiprazole and white Veratrol co-crystals. The preparation method is as follows: equimolar aripiprazole and resveratrol are put into a mortar for grinding, ketone or alkyl nitrile solvent is added before grinding, manually ground for 30 minutes, and vacuum-dried at 40-60 DEG C to obtain aripiprazole. azole drug co-crystals. The powder dissolution experiment of aripiprazole and resveratrol showed that the dissolution rate of aripiprazole slowed down in both the acetate buffer solution of pH=4.0 and the phosphate buffer solution of pH=6.8, showing a potential sustained release effect. Therefore, by preparing the aripiprazole co-crystal into an intramuscular injection, it may be possible to achieve a long-term treatment of schizophrenia and reduce the effect of muscle stimulation.
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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