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Fenbufen eutectic and preparation method and application thereof

A monoclinic and molecular technology, applied in organic chemistry methods, separation/purification of carboxylic acid compounds, organic chemistry, etc., can solve problems such as poor oral absorption and poor solubility, and improve solubility and bioavailability , low cost, simple process effect

Active Publication Date: 2017-09-22
NAT INST FOR FOOD & DRUG CONTROL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, fenbufen belongs to BCS Ⅱ drugs, and its solubility is poor, which makes its oral absorption not ideal

Method used

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  • Fenbufen eutectic and preparation method and application thereof
  • Fenbufen eutectic and preparation method and application thereof
  • Fenbufen eutectic and preparation method and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0037] The preparation method of the fenbufen co-crystal includes a solvent-assisted grinding method or a suspension method.

[0038] The solvent-assisted grinding method specifically includes the following steps: Feed the raw material fenbufen and the amino acid eutectic reagent at a molar ratio of 3:1 to 1:4, add the solvent dropwise, mix and grind for 10 to 300 minutes at a temperature of 10°C to 50°C, The fenbufen co-crystal was obtained.

[0039] When the amino acid co-crystal reagent is L-histidine, the solvent is selected from one of methanol, ethanol, water, acetonitrile, acetone, dimethyl sulfoxide, ethyl acetate and n-butanol.

[0040] When the amino acid co-crystal reagent is L-proline, the solvent is selected from ethanol, methanol, water, dimethylsulfoxide, dichloromethane, methanol-dimethylsulfoxide, water-dimethylsulfoxide-acetonitrile, and water- One of tetrahydrofuran-ethanol.

[0041] The suspension method specifically includes the following steps: take the...

example 1

[0046] Weigh 200.1mg fenbufen and 122.9mg L-histidine, add dropwise a small amount of dichloromethane, acetonitrile or n-butanol, grind for 20-300min, and dry to obtain fenbufen / L-histidine co-crystal .

example 2

[0048] Weigh 300.9 mg of fenbufen and 183.0 mg of L-histidine, add dropwise a small amount of dimethyl sulfoxide, methanol or water, grind for 20-300 minutes, and dry to obtain the fenbufen / L-histidine co-crystal.

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Abstract

The invention provides fenbufen eutectic that is formed by bonding the pharmaceutical active ingredient fenbufen to an amino acid eutectic reagent by means of intermolecular hydrogen bonding; the amino acid eutectic reagent is L-histidine or L-proline. The invention also discloses a preparation method of the fenbufen eutectic; the preparation method comprises: using fenbufen and eutectic reagents as raw materials, and subjecting the raw materials to solvent-assisted grinding or suspending. 'Gold standard'-monocrystal X-ray diffraction determination of eutectic inspection for the fenbufen eutectic proves that the fenbufen eutectic is formed by connecting via noncovalent hydrogen bonds and is not salt but pharmaceutical eutectic; all acquired pharmaceutical eutectics are subjected to structural characterization by TGA (thermal gravimetric analysis), DSC (differential scanning calorimetry), infrared spectrometry, powder X-ray diffraction and other means, and the results prove that a novel form of eutectic is formed. Through the fenbufen eutectic, the problem that raw fenbufen has poor water solubility is solved; the fenbufen eutectic has better water solubility; the development of pharmaceutical clinical research of fenbufen is facilitated.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a fenbufen co-crystal for improving the solubility of a fenbufen crude drug, a preparation method and an application thereof. Background technique [0002] As early as the 19th century, it was reported that quinhydrone was a typical eutectic, but it did not attract people's attention at that time, and there were not many application reports until the 1970s and 1980s. According to statistics, as of February 20, 2017, a total of 368 patent applications involving drug co-crystal technology were retrieved in Scifinder. At present, there have been many reports on the formation principle of co-crystals, most of which are supramolecular assembly mechanisms. ) and their synergy to form molecular aggregates. [0003] The solid forms of drugs generally include salts, polymorphs, hydrates, solvates, amorphous forms, and cocrystals, and crystalline drugs are often sele...

Claims

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Application Information

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IPC IPC(8): C07C51/43C07C59/84C07D233/64C07D207/16
CPCC07B2200/13C07C51/43C07C59/84C07D207/16C07D233/64
Inventor 杨化新卢忠林何兰陈颖刘睿
Owner NAT INST FOR FOOD & DRUG CONTROL
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