Indole-5-carboxylic acid organic pharmaceutical cocrystal and preparation method thereof

A technology of organic drugs and carboxylic acids, which is applied in the field of indole-5-carboxylic acid organic drug co-crystal and its preparation, can solve the problems of less research, achieve good application prospects, improve drug efficacy and bioavailability, physical and chemical The effect of property improvement

Inactive Publication Date: 2018-06-22
YUNNAN AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At this stage, foreign research on drug co-crystals has gradually increased and deepened, while domestic research on it is still relatively small

Method used

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  • Indole-5-carboxylic acid organic pharmaceutical cocrystal and preparation method thereof
  • Indole-5-carboxylic acid organic pharmaceutical cocrystal and preparation method thereof
  • Indole-5-carboxylic acid organic pharmaceutical cocrystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] A preparation method of indole-5-carboxylic acid organic drug co-crystal:

[0033] Add 0.1mmol of indole-5-carboxylic acid and 0.1mmol of 4,4'-bipyridyl into a mixed solvent consisting of 3ml of water and 3ml of ethanol and place in a eutectic container, stir at room temperature for 2h; after the stirring stops, place the eutectic container in Place it in an oven at 80°C for 10 hours and take it out. After cooling down to room temperature, rod-shaped and block-shaped light yellow crystals are precipitated. The molar yield is 80%, and the obtained crystal particles are moderate in volume and in the form of small particles.

Embodiment 2

[0035] A preparation method of indole-5-carboxylic acid organic drug co-crystal:

[0036] Add 0.1mmol of indole-5-carboxylic acid and 0.1mmol of 4,4'-bipyridine into a mixed solvent consisting of 3ml of water and 3ml of methanol and place in a eutectic container, stir at room temperature for 2h; after the stirring stops, place the eutectic container in Place it in an oven at 80°C for 10 hours and take it out. After cooling down to room temperature, rod-shaped and block-shaped light yellow crystals are precipitated. The molar yield is 85%, and the obtained crystal particles are moderate in volume and in the form of small particles.

Embodiment 3

[0038] A preparation method of indole-5-carboxylic acid organic drug co-crystal:

[0039] Add 0.1mmol of indole-5-carboxylic acid and 0.1mmol of 4,4'-bipyridine into a mixed solvent consisting of 3ml of water and 3ml of acetone and place in a eutectic container, stir at room temperature for 2h; after the stirring stops, place the eutectic container in Place it in an oven at 80°C for 20 hours and then take it out. After cooling down to room temperature, rod-shaped and block-shaped light yellow crystals are precipitated. The molar yield is 78%, and the obtained crystal particles are moderate in volume and in the form of small particles.

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Abstract

The invention relates to an indole-5-carboxylic acid organic pharmaceutical cocrystal and a preparation method thereof and belongs to the technical field of organic pharmaceutical cocrystal. The method comprises steps as follows: indole-5-carboxylic acid is taken as an active pharmaceutical ingredient, and 4,4'-bipyridyl is taken as a cocrystal precursor; indole-5-carboxylic acid and 4,4'-bipyridyl are placed in a cocrystal container together with water and ethanol, methanol or acetone; the cocrystal container is arranged on a stirrer, and stirring is performed at room temperature for 1-4 h; after stirring, the cocrystal container is placed in a drying oven at 40-100 DEG C for 10-40 h and then is taken out, and after the temperature is reduced to the room temperature, rodlike and blocky pale yellow crystal is separated out. The cocrystal inherits pharmacological activity of indole-5-carboxylic acid, has obvious improvement in the aspects of solubility, stability and bioavailability andhas better application prospect.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to an indole-5-carboxylic 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 type of structure. 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 used as a "preparation in...

Claims

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Application Information

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IPC IPC(8): C07D209/08C07D213/22C07D213/127A61P35/00A61P37/02
CPCC07D209/08C07B2200/13C07D213/127C07D213/22
Inventor 李崧秦向东张娅玲杨姝赵红梅马俊蓉赵艳赵蕾卜玉涛
Owner YUNNAN AGRICULTURAL UNIVERSITY
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