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Aripiprazole-acetylsalicylate and preparation method thereof
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A technology of acetylsalicylate and aripiprazole, applied in the field of chemical synthesis and drug crystallization, can solve the problems of limited clinical use and low success rate
Active Publication Date: 2022-05-20
TIANJIN UNIV
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However, if a non-pharmaceutical ligand is used to synthesize the salt form of aripiprazole, the real clinical application will be limited; if a pharmaceutically acceptable ligand or other drugs are used to participate in the formation of the salt form of aripiprazole, both It has pharmaceutical significance, but also needs to be able to form hydrogen bond assembly with aripiprazole molecules, the selection of ligands and possible potential hydrogen bond assembly methods need to be carefully considered, and the success rate of preparation will be low.
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Embodiment 1
[0041] 22.4 mg of aripiprazole and 9.01 mg of acetylsalicylic acid (molar ratio 1:1) were placed in a 4 mL sample bottle, and added to 2 mL of acetonesolvent (the ratio of solid to liquid was 15.7 mg solid / 1 mL solvent). Stir at 15°C for suspension reaction crystallization, centrifuge after 24 hours to obtain white crystals, dry at 25°C to obtain white powder. The powder X-raydiffraction pattern of the product is represented by diffraction angle 2θ at 9.14°, 9.72°, 10.69°, 12.63°, 15.05°, 16.11°, 17.41°, 17.95°, 18.60°, 19.75°, 20.11°, 20.69° , 21.73°, 22.24°, 22.47°, 24.49°, 25.23°, 26.17°, 26.92°, 27.23°, 28.76°, 30.03°, 33.15° have characteristic peaks, and figure 1 Consistent, the DSC spectrum has a characteristic endothermic peak at 114.61 ° C, which is consistent with image 3 Consistent, confirm that the obtained product is the aripiprazole-acetylsalicylate type crystal.
Embodiment 2
[0043] Put 22.4mg of aripiprazole and 18.02mg of acetylsalicylic acid (molar ratio 1:2) into a 4mL sample bottle, and add 2mL of acetonitrilesolvent (the ratio of solid to liquid is 20.2mg solid / 1mL solvent). Stir at 20°C for suspension reaction crystallization, centrifuge after 24 hours to obtain white crystals, dry at 25°C to obtain white powder. The powder X-raydiffraction pattern of the product is represented by diffraction angle 2θ at 9.15°, 9.73°, 10.69°, 12.64°, 15.06°, 16.11°, 17.42°, 17.97°, 18.62°, 19.77°, 20.13°, 20.69° , 21.74°, 22.26°, 22.49°, 24.48°, 25.25°, 26.19°, 26.94°, 27.25°, 28.77°, 30.04°, 33.16° have characteristic peaks, and figure 1 Consistent, the DSC spectrum has a characteristic endothermic peak at 114.50 ° C, which is consistent with image 3 Consistent, confirm that the obtained product is the aripiprazole-acetylsalicylate type crystal.
Embodiment 3
[0045] Put 448mg of aripiprazole and 270.24mg of acetylsalicylic acid (molar ratio 1:1.5) into a 20mL sample bottle, and add 18mL of acetonitrile solvent (the ratio of solid to liquid is 39.9mg solid / 1mL solvent). Stir at 30°C for suspension crystallization, centrifuge after 36 hours to obtain white crystals, and dry at 30°C to obtain white powder. The powder X-ray diffraction pattern of the product is represented by diffraction angle 2θ at 9.15°, 9.71°, 10.68°, 12.60°, 15.01°, 16.09°, 17.39°, 17.93°, 18.52°, 19.73°, 20.11°, 20.74° , 21.69°, 22.18°, 22.49°, 24.43°, 25.23°, 26.10°, 26.83°, 27.21°, 28.80°, 30.01°, 33.09° have characteristic peaks, and figure 1 Consistent, the DSC spectrum has a characteristic endothermic peak at 114.72 ° C, which is consistent with image 3 Consistent, confirm that the obtained product is the aripiprazole-acetylsalicylate type crystal.
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Abstract
The invention relates to aripiprazole-acetylsalicylate and a preparation method thereof. The molecular formula of the salt type is C 32 h 35 N 3 o 6 Cl 2 , with a relative molecular mass of 628.53; at the same time, it provides two simple and repeatable preparation methods, the suspension reaction crystallization method or the grinding reaction crystallization method, which are suitable for industrial production of the salt formation of aripiprazole and acetylsalicylic acid. Compared with the solubility and dissolution rate of aripiprazole, the salt type is greatly improved: the maximum equilibrium concentration of aripiprazole in the dissolution test of pH 4.0 acetate buffer medium is 290 μg / ml, which is required to reach the equilibrium concentration. The time was 6 hours, and it was 315 micrograms / ml after forming the salt, and 1 hour. Compared with acetylsalicylic acid, the hygroscopic stability has been improved to a certain extent: at 95% relative humidity, the weight gain of acetylsalicylic acid is 2.5%, and the weight gain of products after salt formation is less than 0.25%.
Description
technical field [0001] The invention belongs to the technical field of chemical synthesis and drugcrystallization, and specifically relates to aripiprazole-acetylsalicylate and a preparation method. Background technique [0002] The improvement of physicochemical properties of poorly soluble drugs is an important step in the drug development process. As an important branch in the field of crystalengineering, pharmaceutical multi-component crystals (co-crystals, salts and solvates) can realize the optimization of the physical and chemical properties of the API without changing the main chemical structure formula and pharmaceutical action mechanism of the pharmaceutical active ingredient (API). regulation. New drug research and development companies usually form APIs to improve pharmaceutical properties such as solubility, dissolution rate, hygroscopicity, stability, and bioavailability by forming salt forms. [0003] Aripiprazole is a new type of anti-schizophrenia drug, ...
Claims
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