Unlock instant, AI-driven research and patent intelligence for your innovation.

Preparation method of rebamipide eutectic

A technology of rebamipide and constant temperature cultivation, applied in the field of preparation of rebamipide co-crystals

Active Publication Date: 2013-09-04
BEIJING INSTITUTE OF TECHNOLOGYGY
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But no one has synthesized the co-crystal of rebamipide so far

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of rebamipide eutectic
  • Preparation method of rebamipide eutectic
  • Preparation method of rebamipide eutectic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1~3

[0043] Embodiments 1-3: Preparation of rebamipide / sodium ion ethanol co-crystal

[0044] Add rebamipide, absolute ethanol and saturated aqueous sodium hydroxide solution into the autoclave, seal the autoclave and place it in a programmed temperature-controlled oven, cultivate for 3 to 5 days, pour out the liquid in the autoclave, and the solvent will naturally Obtain rebamipide / sodium ion ethanol cocrystal after volatilization;

[0045] Among them, the mass of rebamipide (mg): the volume of absolute ethanol (ml): the volume of saturated sodium hydroxide aqueous solution (ml)=35~75:10~15:1~2.

[0046] The cultivation process includes a uniform temperature rise stage from room temperature to constant temperature culture temperature, a constant temperature culture stage and a uniform temperature drop stage from constant temperature culture temperature to room temperature; the uniform temperature rise stage is 1 to 3 hours, and the uniform temperature drop stage is 7 to 10 hours. ...

Embodiment 4~6

[0049] Embodiments 4-6: Preparation of rebamipide / pentaerythritol co-crystal

[0050] Add rebamipide, pentaerythritol and absolute ethanol into the autoclave, seal the autoclave and place it in a programmed temperature-controlled oven, cultivate it for 3 to 5 days, pour out the liquid in the autoclave, and obtain Rebamipide after the solvent evaporates naturally. Bappet / Pentaerythritol co-crystal;

[0051] Among them, the mass (mg) of rebamipide: the volume (ml) of absolute ethanol: the mass (mg) of pentaerythritol=45~75:10~15:3.5~7.

[0052] The cultivation process includes a uniform temperature rise stage from room temperature to constant temperature culture temperature, a constant temperature culture stage and a uniform temperature drop stage from constant temperature culture temperature to room temperature; the uniform temperature rise stage is 1 to 3 hours, and the uniform temperature drop stage is 7 to 10 hours. The rest of the time is the stage of constant temperature cu...

Embodiment 7~9

[0054] Examples 7-9: Preparation of rebamipide / rebamipide co-crystal

[0055] Add rebamipide, absolute ethanol and distilled water into the autoclave, seal the autoclave and place it in a programmed temperature-controlled oven, cultivate it for 2 to 5 days, pour out the liquid in the autoclave, and obtain rebamipide after the solvent evaporates naturally. Bamipide / Rebamipide eutectic;

[0056] Among them, the mass of rebamipide (mg): the volume of absolute ethanol (ml): the volume of distilled water (ml) = 35-65: 10-15: 3.5-8.

[0057] The cultivation process includes a uniform temperature rise stage from room temperature to constant temperature culture temperature, a constant temperature culture stage and a uniform temperature drop stage from constant temperature culture temperature to room temperature; the uniform temperature rise stage is 1 to 3 hours, and the uniform temperature drop stage is 7 to 10 hours. The rest of the time is the stage of constant temperature cultiva...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
Login to View More

Abstract

The invention relates to a preparation method of rebamipide eutectic and belongs to the field of medicine development. The method comprises the following steps: rebamipide, eutectic composition (CCF) and solvent is added into a high pressure kettle, the high pressure kettle is placed into a procedure temperature control drying oven after being sealed, after 2 to 5 days of cultivation, liquid inside the high pressure kettle is poured out, and rebamipide eutectic is obtained after natural volatilization of solvent. Through single-crystal structure testing, XPRD, DSC, infrared and nuclear magnetism, characterization to the obtained eutectic is obtained, and that a novel crystal form which is different from reactant rebamipide is proved to be obtained. The eutectic is used for carrying out an ulcer inhibition test on rats with damaged gastric mucosa caused by alcohol, and the experimental result shows the favorable drug effect of the obtained eutectic.

Description

technical field [0001] The invention relates to a preparation method of rebamipide co-crystal, belonging to the field of drug development. Background technique [0002] Rebamipide, alias rebamipide, rebamipide, chemical name 2-(4-chlorobenzamido)-3-(1,2-dihydro-2-oxo-4-quinoline base) propionic acid or 2-(4-chlorobenzamido)-3-(1,2-dihydro-2-oxo-4-quinolyl)propionic acid, the structural formula is as follows: [0003] [0004] Rebamipide is odorless, bitter, white crystalline powder, slightly soluble in methanol and ethanol solvents, almost insoluble in water, its substance number identification (CAS) number: 90098-04-7, its preparation method see JP- B-63-35623. [0005] Rebamipide can improve the subjective and objective symptoms of some diseases, and can be used for the treatment of ulcerative colitis (see Kazuya Makiyama, "Rebamipide enema therapy for the treatment of ulcerative colitis"), for stomatitis (JP2839847) , can promote saliva secretion (WO2005011811), and...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/227C07C31/08C07C29/78C07C31/24A61P1/04
Inventor 王晓莹胡长文迟瑛楠王晓鸽马承伟
Owner BEIJING INSTITUTE OF TECHNOLOGYGY