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Acipimox urea eutectic crystal

A technology of acyclolimus and urea, which is applied in the field of acyclolimus-urea co-crystal, can solve the problems of low yield, less crystalline co-crystal structure, and no characterization parameters are mentioned, and achieves high solubility and hygroscopicity. Low, good stability

Pending Publication Date: 2021-07-16
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are many relevant reports about acipimox, but mainly about its preparation, preparation, physical and chemical properties and pharmacological properties. There are few reports on the crystal structure, patents US2005239803A1, CN 103508963 A, etc. have all reported the preparation method of acipimox, patent CN86103304-2 obtains the acipimox precipitate of crystal shape, is hydrate acipimox, and the productive rate is relatively high. Low
In the previous reports, there were few reports on the acipimus cocrystal cocrystal, and the crystallographic characterization parameters of the acipimus cocrystal were not mentioned

Method used

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  • Acipimox urea eutectic crystal
  • Acipimox urea eutectic crystal
  • Acipimox urea eutectic crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Add 154.1mg of acipimox (1mmol) and 126.1mg of urea (2.1mmol) into 20ml of methanol, heat and stir to dissolve, reflux for 10 hours, slowly lower the temperature to 2-4°C, and stand for crystallization under temperature control for 48 hours, filtered, washed the filter cake with acetonitrile, and vacuum-dried at 50°C for 12 hours to obtain urea-acipimus eutectic with a yield of 97.33% and a purity of 99.95%.

Embodiment 2

[0058] Add 154.1mg of acipimox, 123.1mg of urea (2.05eq)) into 30ml of mixed solvent (18ml of methanol + 12ml of ethyl acetate), heat and stir to dissolve, reflux for 12 hours, and slowly cool down to 1-5°C, The crystallization was carried out under temperature control for 45 hours, filtered, the filter cake was washed with acetone, and vacuum-dried at 70° C. for 8 hours to obtain urea acipimus eutectic with a yield of 96.56% and a purity of 99.94%.

Embodiment 3

[0060] Add 154.1mg of acipimox and 129.1mg of urea (2.15eq) into 23.5ml of ethyl acetate, heat and stir to dissolve, reflux for 7 hours, slowly lower the temperature to 5-10°C, and stand for crystallization under temperature control for 60 hours , filtered, washed the filter cake with acetonitrile, and vacuum-dried at 60°C for 10 h to obtain urea-acipimus eutectic with a yield of 95.98% and a purity of 99.89%.

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PUM

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Abstract

The invention belongs to the technical field of medicine, and particularly provides an acipimox urea eutectic crystal, a preparation method thereof and application of the acipimox urea eutectic crystal in preparation of lipid-lowering drugs, prepared acipimox urea is radiated by Cu-K[alpha], an X-ray diffraction pattern expressed by 2[theta] has characteristic peaks at least at 20.8 + / -0.2 degrees, 22.5 + / -0.2 degrees and 28.1 + / -0.2 degrees, and the acipimox urea eutectic crystal prepared by the invention is high in solubility, low in hygroscopicity and good in stability, and has a relatively good industrial application prospect.

Description

technical field [0001] The invention belongs to the technical field of organic drug eutectics, in particular to an acipimus urea eutectic. Background technique [0002] Drug co-crystals are based on the principle 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 Waals forces of aromatic hydrocarbons or benzene rings, π- π conjugation and halogen bond) to form a new structure, that is, drug co-crystal. It is based on hydrogen bonds, and neither needs to form new covalent bonds nor destroy existing covalent bonds. 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, reducing its hygroscopicity, impr...

Claims

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Application Information

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IPC IPC(8): C07D241/24A61K31/4965A61P3/06
CPCC07D241/24A61P3/06C07B2200/13
Inventor 翟立海夏祥来张明明梁茂征刘忠
Owner LUNAN PHARMA GROUP CORPORATION
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