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Salicylic acid organic medicine eutectic and preparation method thereof

An organic drug, salicylic acid technology, applied in the direction of organic chemistry methods, active ingredients of salicylic acid, organic chemistry, etc., can solve problems such as adverse effects on product quality and damage to crystal forms

Inactive Publication Date: 2017-11-03
YUNNAN POLICE COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most manufacturers rely on pulverization to obtain fine crystals, but the pulverization destroys the crystal form and the pulverization process has an adverse effect on product quality

Method used

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  • Salicylic acid organic medicine eutectic and preparation method thereof
  • Salicylic acid organic medicine eutectic and preparation method thereof
  • Salicylic acid organic medicine eutectic and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation of embodiment 1 salicylic acid organic drug cocrystal

[0027] Add 0.1mmol salicylic acid and 0.2mmol 4,4'-bipyridine to a mixed solvent consisting of 4ml water and 2ml ethanol and place in a eutectic container, stir at room temperature for 2 hours; after the stirring stops, place the eutectic container in an oven at 80°C It was taken out after standing in the middle for 20 hours, and massive and flaky colorless crystals were precipitated after cooling down to room temperature, and the molar yield was 85%.

Embodiment 2

[0028] The preparation of embodiment 2 salicylic acid organic medicine eutectic

[0029] Add 0.1mmol salicylic acid and 0.2mmol 4,4'-bipyridyl into a mixed solvent consisting of 4ml water and 2ml methanol and place in a eutectic container, stir at room temperature for 2 hours; after the stirring stops, place the eutectic container in an oven at 80°C Take it out after standing in the middle for 20 hours, after cooling down to room temperature, massive and flaky colorless crystals are precipitated, and the molar yield is 80%.

Embodiment 3

[0030] The preparation of embodiment 3 salicylic acid organic drug cocrystal

[0031] Add 0.1mmol salicylic acid and 0.2mmol 4,4'-bipyridine to a mixed solvent consisting of 4ml water and 2ml acetone and place in a eutectic container, stir at room temperature for 2 hours; after the stirring stops, place the eutectic container in an oven at 80°C Take it out after being left in the middle for 20 hours, and after cooling down to room temperature, blocky and flaky colorless crystals are precipitated, and the molar yield is 88%.

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Abstract

The invention relates to salicylic acid organic medicine eutectic and a preparation method of the eutectic. The preparation method comprises the steps of taking salicylic acid as an active ingredient of a medicine, taking 4,4'-dipyridyl as an eutectic precursor, putting salicylic acid, 4,4'-dipyridyl, water, alcohol, methanol or acetone into an eutectic vessel, placing the eutectic vessel on a stirrer, performing room temperature stirring for 2h, placing the eutectic vessel in a 40-100 DEG C oven for 10-40h after stirring stop, taking the eutectic vessel out, and performing cooling to a room temperature until lumpy and flaky clear crystal is separated out. The eutectic inherits pharmacological activity of salicylic acid, and has obvious improvement in solubility, stability and bioavailability of salicylic acid.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to a novel salicylic acid organic drug co-crystal and a preparation method thereof. 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 (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, conjugated interaction and halogen bond) to form a new structure, that is, drug co-crystal. In November 2011, the FDA issued the "Guidance Forlndustry: Regulatory Classificat1n Of Pharmaceutical Cocrystals", pointing out that when a drug forms a cocrystal with an excipient, the drug cocrystal can be managed as a...

Claims

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Application Information

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IPC IPC(8): C07D213/22C07C65/10A61K31/60A61K31/444A61P35/00A61P29/00A61P19/06A61P7/02A61P11/00A61K8/49A61K8/368A61Q19/00
CPCA61K8/368A61K8/4953A61K31/444A61K31/60A61K2800/10A61K2800/524A61Q19/00C07B2200/13C07C65/10C07D213/22A61K2300/00
Inventor 邓临新倪春明骆寒青李斌
Owner YUNNAN POLICE COLLEGE
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