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Isonicotinamide and acipimox eutectic crystal II and preparation method thereof

A technology of isonicotinamide and co-crystal, which is applied in the field of co-crystal of acipimox and isonicotinamide and its preparation, can solve the problem of low solubility and stability of acipimox co-crystal, and the lipid-lowering effect needs to be improved , Affect drug absorption and other issues, achieve good therapeutic effect, good solid state stability, and good lipid-lowering effect

Active Publication Date: 2020-12-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the stability of the obtained co-crystal has been improved, it still needs to be improved, and the solubility of the co-crystal is low, which affects the absorption of drugs in the human body
[0008] The solubility and stability of the acipimox co-crystal in the prior art are not high, and the lipid-lowering effect after the human body takes it also needs to be improved

Method used

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  • Isonicotinamide and acipimox eutectic crystal II and preparation method thereof
  • Isonicotinamide and acipimox eutectic crystal II and preparation method thereof
  • Isonicotinamide and acipimox eutectic crystal II and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Add 154.1mg of acipimox and 244.2mg of isonicotinamide into 26.4ml of acetonitrile and 4.4ml of purified water mixed solvent, heat to 65°C and stir under reflux for 10 hours, slowly cool down to 15°C, and then stand for crystallization for 30 hours, filtered, and vacuum-dried at 50° C. for 10 h to obtain isonicotinamide acipimox eutectic crystal Form II with a yield of 96.33%. After determination, its X-ray powder diffraction pattern and figure 1 Basically the same.

Embodiment 2

[0059] Add 154.1mg of acipimox and 183.2mg of isonicotinamide into 12.3ml of methanol and 3.1ml of purified water mixed solvent, heat to 45°C and stir under reflux for 10 hours, slowly cool down to 5°C, and then stand for crystallization for 20 hours, filtered, and vacuum-dried at 50° C. for 10 h to obtain isonicotinamide acipimus eutectic crystal Form II with a yield of 95.80%. After determination, its X-ray powder diffraction pattern and figure 1 Basically the same.

Embodiment 3

[0061] Add 154.1 mg of acipimox and 366.3 mg of isonicotinamide into 41.1 ml of acetonitrile and 5.1 ml of purified water mixed solvent, heat to 70°C and stir under reflux for 10 hours, slowly cool down to 20°C, and then stand for crystallization for 60 hours, filtered, and vacuum-dried at 50° C. for 10 h to obtain isonicotinamide acipimus eutectic crystal Form II with a yield of 95.37%. After determination, its X-ray powder diffraction pattern and figure 1 Basically the same.

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Abstract

The invention belongs to the technical field of medicines, and particularly provides an isonicotinamide and acipimox eutectic crystal II, a preparation method thereof and application thereof in preparation of hypolipidemic drugs. The isonicotinamide and acipimox eutectic crystal II prepared by the method is radiated by Cu-K alpha, and an X-ray diffraction pattern expressed by 2theta has characteristic peaks at 10.9 + / -0.2 degrees, 22.0 + / -0.2 degrees, 23.5 + / -0.2 degrees and 26.5 + / -0.2 degrees. The isonicotinamide and acipimox eutectic crystal prepared by the preparation method disclosed by the invention is good in stability in a medium, high in product purity, high in bioavailability and better in drug effect. The method is simple in preparation process and has a good industrial application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and specifically relates to a co-crystal of acipimox and isonicotinamide, a preparation method and application thereof. Background technique [0002] The new salt type of drug co-crystal refers to the introduction of a new co-crystal substance (CCF) through proton transfer, which self-assembles with the active ingredient of the drug (APT) under the force of hydrogen bonds to form a supramolecular crystal with a fixed stoichiometric ratio. While retaining the pharmacological effects of the drug itself, it can also modify the physical and chemical properties of the drug, such as improving the stability of the drug, reducing its hygroscopicity, improving solubility, and improving bioavailability. It is a drug co-crystal in the pharmaceutical industry. The application provides broad development prospects. In recent years, the study of pharmaceutical co-crystals has attracted more and mor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/24C07D213/81A61K31/4965A61K31/4409A61P3/06
CPCC07D241/24C07D213/81C07B2200/13
Inventor 翟立海李玲郭立红王金朋
Owner LUNAN PHARMA GROUP CORPORATION
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