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Fenofibric acid choline salt crystal form and preparation method thereof

A kind of technology of fenofibrate acid choline salt and crystal form, which is applied in the new crystal form of fenofibrate acid choline salt and its preparation field, and can solve the problem that there is no report on the crystal form of dexmethylphenidate hydrochloride, fenofibrate The problems of stability and poor bioavailability of choline fibrate acid salts can achieve the effect of good controllability, good reproducibility and high bioavailability

Inactive Publication Date: 2015-05-20
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing fenofibric acid choline salt has poor stability and bioavailability, which cannot meet the growing market demand, and so far, there is no crystal form report of dexmethylphenidate hydrochloride

Method used

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  • Fenofibric acid choline salt crystal form and preparation method thereof
  • Fenofibric acid choline salt crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Preparation of fenofibric acid choline salt crystal form: dissolve the crude product of fenofibric acid choline salt in a mixed solvent of isopropanol and water (85:15 by volume), add it to the reaction bottle, stir and heat up to reflux , keep stirring until completely dissolved, add fenofibric acid choline salt crude product or activated carbon with 1% mass of other crystal forms, keep stirring and decolorize for 30 minutes, filter while hot, cool the filtrate to 25°C, slowly stir and grow the crystal overnight, filter , the filter cake was rinsed with isopropanol, the solid was collected, and vacuum-dried at 50°C for 24 hours to obtain the fine product of fenofibric acid choline salt - white crystals; its X-ray powder diffraction (XRPD) pattern was as follows figure 1 As shown, its differential thermal / thermogravimetric analysis (DSC / TG) spectrum is as follows figure 2 as shown, 1 H-NMR (D 2 O, 400MHz) δ: 7.386 (d, J=8.8Hz, 2H), 7.292 (d, J=8.4Hz, 2H), 7.112 (d, J...

Embodiment 2

[0028] Preparation of fenofibric acid choline salt crystal form: dissolve the crude fenofibric acid choline salt in a mixed solvent of isopropanol and water (volume ratio 80:20), add it to the reaction bottle, stir and heat up to reflux , keep stirring until completely dissolved, add fenofibric acid choline salt crude product or activated carbon with 1% mass of other crystal forms, keep stirring and decolorize for 30 minutes, filter while hot, cool the filtrate to 25°C, slowly stir and grow the crystal overnight, filter , the filter cake was rinsed with isopropanol, the solid was collected, and vacuum-dried at 50° C. for 24 hours to obtain the fine product of fenofibric acid choline salt—white crystals, whose XRPD, DSC, and TG patterns were the same as those in Example 1.

Embodiment 3

[0030] Preparation of fenofibric acid choline salt crystal form: dissolve the crude fenofibric acid choline salt in a mixed solvent of isopropanol and water (volume ratio 90:10), add it to the reaction bottle, stir and heat up to reflux , keep stirring until completely dissolved, add fenofibric acid choline salt crude product or activated carbon with 1% mass of other crystal forms, keep stirring and decolorize for 30 minutes, filter while hot, cool the filtrate to 25°C, slowly stir and grow the crystal overnight, filter , the filter cake was rinsed with isopropanol, the solid was collected, and vacuum-dried at 50° C. for 24 hours to obtain the fine product of fenofibric acid choline salt—white crystals, whose XRPD, DSC, and TG patterns were the same as those in Example 1.

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Abstract

The invention belongs to the field of pharmacy and in particular relates to a novel crystal form of a fenofibric acid choline salt and a preparation method thereof. The X-ray powder diffraction spectrum of the fenofibric acid choline salt crystal form has characteristic peaks at the following d values: 7.161, 5.555, 4.772, 4.692, 4.609, 4.438, 4.201, 3.696, 3.576, 3.411, 2.984 and 2.783. The method for preparing the fenofibric acid choline salt crystal form comprises the following steps: dissolving a crude product or a crystal form of the fenofibric acid choline salt in a mixed solvent of isopropanol and water, and crystallizing, thereby obtaining the crystal form. The fenofibric acid choline salt crystal form is high in stability, and the preparation method is high in controllability and high in reproducibility and is suitable for large-scale pharmaceutical production.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a new crystal form of fenofibric acid choline salt and a preparation method thereof. Background technique [0002] Fenofibric acid choline salt (choline fenofibrate), CAS number: 856676-23-8, its capsule (Abbott, trade name Trilipix) was listed in the United States in 2008. Fenofibric acid choline salt is a double salt formed by the combination of fenofibric acid (fenofibric acid), a metabolite of fenofibrate in the body, and choline, and its solubility is significantly higher than that of fenofibrate under alkaline conditions. Fenofibric acid choline salt can reduce low-density lipoprotein (LDL) and triglyceride levels in the body, increase high-density lipoprotein (HDL) levels, and can also be used in combination with other stinoids to improve hyperlipidemia symptoms. The existing fenofibric acid choline salt has poor stability and bioavailability and cannot meet the growin...

Claims

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Application Information

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IPC IPC(8): C07C69/708C07C67/52C07C215/40C07C213/10
CPCC07C51/43C07C59/90C07C213/10C07C215/40
Inventor 牛冰刘杰李世文
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD
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