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

Mosapride organic acid salt

A technology of organic acid salt and organic acid, applied in the field of mosapride organic acid salt and preparation thereof, can solve the problems of low dissolution rate, low solubility, undisclosed impurity structure and the like, and achieves good stability and good stability Effect

Pending Publication Date: 2022-06-07
LUNAN PHARMA GROUP CORPORATION
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are few reports on the crystal forms of mosapride. The crystal forms disclosed in the prior art include the mosapride ethanol solvate reported in the patent JP2011225491A, the mosapride monohydrate crystal form reported in the patent KR20090044694A and the patent The citric acid dihydrate reported in WO2011107903A1 has low solubility in hydrochloric acid solution at pH 1.0, and often encounters the problem of low dissolution or even failure in the actual production of mosapride citrate oral solid preparations
[0005] For the study on the stability of mosapride, "The Stability of Mosapride Citrate by HPLC Method" Clinical Rational Drug Use, Volume 8, Issue 8A, August 2015, reported that mosapride solid was exposed to 4500Lx light After 10 days, there was no obvious degradation, and the main peak decreased by about 10.0% under high temperature for 3 hours and oxidation for 5 hours, but the specific impurity structure was not disclosed

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
  • Mosapride organic acid salt
  • Mosapride organic acid salt
  • Mosapride organic acid salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] 2.5 g of mosapride and 1.8 g of 5-sulfosalicylic acid were dissolved in 120 mL of mixed solvent (40 mL of methanol, 40 mL of acetone and 40 mL of ethanol), heated to 60°C, dissolved, filtered, and the temperature was controlled to 6-9°C Crystallize for 45 hours, filter, rinse the filter cake with methanol, and dry the filter cake at 60° C. for 15 hours to obtain 3.62 g of mosapride 5-sulfosalicylate methanolate. The yield is 93.50%, and the purity is 99.97%.

Embodiment 2

[0099] 2.5 g of mosapride and 1.65 g of 5-sulfosalicylic acid were dissolved in 160 mL of mixed solvent (32 mL of methanol, 50 mL of acetone and 78 mL of ethanol), heated to 56°C, dissolved, filtered, and analyzed at a temperature of 1 to 5°C. The crystals were crystallized for 30 hours, filtered, and the filter cake was rinsed with methanol, and the filter cake was dried at 50 °C for 12 hours to obtain 3.59 g of mosapride 5-sulfosalicylate methanolate. The yield was 92.62%, and the purity was 99.95%.

Embodiment 3

[0101] 2.5 g of mosapride and 1.95 g of 5-sulfosalicylic acid were dissolved in 250 mL of mixed solvent (125 mL of methanol, 80 mL of acetone and 45 mL of ethanol), heated to 64°C, dissolved, filtered, and analyzed at 6-9°C under temperature control. Crystallize for 60 hours, filter, rinse the filter cake with methanol, and dry the filter cake at 55°C for 20 hours to obtain 3.58 g of mosapride 5-sulfosalicylate methanolate. The yield was 92.41%, and the purity was 99.93%.

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

No PUM Login to View More

Abstract

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a mosapride organic acid salt and a preparation method thereof.The mosapride organic acid salt is formed by mosapride and 5-sulfosalicylic acid or sulfamic acid, specifically, a methyl alcohol compound of mosapride 5-sulfosalicylic acid, a mosapride sulfamic acid trihydrate, a methyl alcohol compound of mosapride 5-sulfosalicylic acid or a methyl alcohol compound of mosapride 5-sulfosalicylic acid or a methyl alcohol compound of mosapride sulfamic acid trihydrate or a methyl alcohol compound of mosapride 5-sulfosalicylic acid or sulfamic acid. The mosapride organic acid salt provided by the invention has high solubility and good stability, is helpful for improving bioavailability, and has important value for optimization and development of mosapride preparations.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, in particular to a mosapride organic acid salt and a preparation method thereof. Background technique [0002] Mosapride has the trade name Gasmotin@ and the chemical name is (+ / -)-4-amino-5-chloro-2-ethoxy-N-[4-fluorobenzyl)-morpholine-2 -ylmethyl]benzamide citrate dihydrate. by Brand marketed for gastrointestinal symptoms associated with chronic gastritis (heartburn, nausea / vomiting). Mosapride stimulates serotonin 5-HT4 receptors in the gastrointestinal plexus, which increases the release of acetylcholine, thereby enhancing gastrointestinal motility and gastric emptying. [0003] Mosapride is currently approved for the treatment of gastrointestinal symptoms associated with chronic gastritis, including heartburn, nausea, vomiting, and gastroesophageal reflux disease (GERD). Mosapride is also in Phase III clinical trials for the treatment of gastrointestinal dumping syndrome or ...

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): C07D265/30C07C309/60C07C303/44
CPCC07D265/30C07C309/60C07B2200/13
Inventor 夏祥来翟立海张朝花陈直金
Owner LUNAN PHARMA GROUP CORPORATION