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Dipfluzine-p-hydroxybenzoic acid eutectic crystal and preparation method thereof

A technology of p-hydroxybenzoic acid and difluzine, which is applied in the field of medicine and can solve the problems of reduced bioavailability and low solubility of drugs

Inactive Publication Date: 2016-05-25
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Poor solubility may result in reduced drug bioavailability, especially as a solid dosage form

Method used

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  • Dipfluzine-p-hydroxybenzoic acid eutectic crystal and preparation method thereof
  • Dipfluzine-p-hydroxybenzoic acid eutectic crystal and preparation method thereof
  • Dipfluzine-p-hydroxybenzoic acid eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041]Accurately weigh 0.2mmol (83mg) difluzine dissolved in 5mL ethanol to obtain an ethanol solution with an analytical balance, accurately weigh an aqueous solution of 0.3mmol (41mg) p-hydroxybenzoic acid dissolved in 5mL water with an analytical balance, and mix the ethanol solution and the aqueous solution After stirring for 10 minutes, filter in a 25mL small beaker to obtain 10mL of saturated ethanol-water mixed solution; place the small beaker in a 250mL beaker filled with 50mL of acetonitrile, seal the large beaker with plastic wrap, and leave crystals to separate out after 20 days at room temperature, namely A co-crystal of difluzine-p-hydroxybenzoic acid was obtained.

[0042] The bisfluzine-p-hydroxybenzoic acid cocrystal obtained in the above-mentioned embodiment 1 is subjected to structural characterization and performance testing through the above-mentioned equipment:

[0043] Such as figure 1 As shown, two protonated difluzine molecules, two deprotonated p-hydr...

Embodiment 2

[0049] Accurately weigh 0.1mmol (41.5mg) difluzine and 0.15mmol (20.5mg) p-hydroxybenzoic acid in 5mL ethanol and 5mL water respectively with an analytical balance, mix the ethanol solution and water solution and stir for 10 minutes, filter in 25mL small In a beaker, 10 mL of ethanol-water mixed solution was obtained; the small beaker was placed in a large beaker (250 mL) filled with 50 mL of acetonitrile, the large beaker was sealed with plastic wrap, and crystals were precipitated after standing at room temperature for 35 days to obtain diphenfluazine-p-hydroxyl Co-crystal of benzoic acid.

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Abstract

The invention discloses a novel dipfluzine medicine eutectic crystal and a preparation method thereof. According to the preparation method, a dipfluzine raw medicine is selected as medicine API, p-hydroxybenzoic acid is selected as a medicine precursor, the prepared dipfluzine medicine eutectic crystal is of a monoclinic system, and the space group is P2(1), wherein a is equal to 26.150(9) angstroms, b is equal to 10.936(3) angstroms, c is equal to 11.963(3) angstroms, beta is equal to 97.49(1) degrees, V is equal to 3391.95(396) cubic angstroms, and z is equal to 2. A vapor diffusion method is utilized in the preparation process of the medicine eutectic crystal, a selected small-cup solvent is a mixed solvent of ethanol and water, a selected big-cup solvent is acetonitrile, and dipfluzine has different solubilities in the selected solvents, so that crystals can be separated in the volatile transfer process of the solvents. The dipfluzine-p-hydroxybenzoic acid eutectic crystal disclosed by the invention is different from X-ray powder diffraction, DSC and infrared spectrum of a physical mixture of dipfluzine and p-hydroxybenzoic acid crystals, and the solubility and dissolving behavior of the medicine eutectic crystal prepared by virtue of the preparation method are obviously improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a difluzine-p-hydroxybenzoic acid co-crystal formed by combining difluzine and p-hydroxybenzoic acid at a molar ratio of 2:3 and a preparation method thereof. Background technique [0002] In the development of drugs, problems such as poor solubility, poor dispersibility, low bioavailability, and stability of active pharmaceutical ingredients (API) are the main factors that plague the pharmaceutical industry, and are the main factors that restrict the development of a drug. Currently, approximately 90% of candidate small molecule APIs are poorly soluble drugs. Poor solubility may result in reduced drug bioavailability, especially as a solid dosage form drug. Improving the solubility of poorly soluble drugs is an urgent problem that needs to be solved. It has become an issue that researchers are paying more and more attention to, and it is also an important aspect of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/104C07C69/84C07C67/52
CPCC07B2200/13C07C67/52C07C69/84C07D295/104
Inventor 王静林玉龙郭伟杨彩琴
Owner HEBEI MEDICAL UNIVERSITY
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