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Mosapride citrate related substances and preparation method thereof

A technology of mosapride citrate and related substances, which is applied in the field of pharmaceutical analytical chemistry, can solve the problems of rare reports and achieve definite curative effect

Pending Publication Date: 2020-06-16
CHENGDU KANGHONG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although there are many reports in the prior art on the detection of related substances of mosapride citrate by HPLC, reports on related substances of mosapride citrate with confirmed structures are rare

Method used

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  • Mosapride citrate related substances and preparation method thereof
  • Mosapride citrate related substances and preparation method thereof
  • Mosapride citrate related substances and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The preparation of embodiment 1 related substance

[0045] Step 1: Take mosapride citrate raw material and citric acid in the same weight ratio and place at 105°C for 17 hours to obtain crude impurities;

[0046] Step 2: After dissolving with 20% acetonitrile aqueous solution, add double water to dilute to prepare a solution with a concentration of 0.03 g / ml, and filter through a 0.45 μm filter membrane to prepare a test solution as an impurity;

[0047] Step 3: the test solution gained in step 2 is entered into a preparative high-performance liquid phase chromatograph for separation; sample size 100ml, flow rate 250ml / min, detection wavelength 274nm, with acetonitrile-0.1% acetic acid aqueous solution (1:1) as mobile phase, Two target peaks were collected, target peak 1 came out at about 14.1min, and target peak 2 came out at about 15.6min. When the two target peaks were detected by the UV detector, start the column to collect fractions and enrich the sample solution ...

Embodiment 2

[0049] The LC-MS detection of embodiment 2 related substance I and related substance II

[0050] 1. Test instrument: WatersAcquity UPLC Q-TOF Prenier MS Thermo LTQ

[0051] 2. Liquid chromatography conditions

[0052] Chromatographic column: silica gel bonded with octadecylsilane (3μm, 150×4.6mm)

[0053] Mobile Phase A: Acetonitrile

[0054] Mobile phase B: 0.1% formic acid in water

[0055] Flow rate: 1ml / min

[0056] Column temperature: 30°C

[0057] Detection wavelength: 274nm

[0058] Gradient elution program:

[0059] time min Flow rateml / min Acetonitrile% 0.1% formic acid in water 0 1.0 15 85 20 1.0 25 75 25 1.0 90 10 35 1.0 90 10 36 1.0 15 85 48 1.0 15 85

[0060] 3. Mass Spectrometry Conditions

[0061] The solution coming out of the UV detector was split, and the flow rate into the mass spectrometer was 0.2ml / min, electrospray ionization, positive ion mode detection, and nitrogen as sheath gas, auxili...

Embodiment 3

[0065] The proton nuclear magnetic resonance spectrum of embodiment 3 related substance I and related substance II ( 1 H-NMR) spectrum

[0066] 1. Chemical structural formula and hydrogen atom number

[0067]

[0068] 2. Test equipment and conditions

[0069] Test instrument: BrukerAVII-400MHz nuclear magnetic resonance instrument

[0070] Test conditions: TMS internal standard, DMSO as test solvent

[0071] 3. Test results

[0072] For the spectrum of substance I see figure 1 , figure 2 ; For the spectrum of the substance II, see image 3 , Figure 4 .

[0073] The 1H NMR (400MHz, DMSO) of the related substance I was 8.0 (s, 1H), 7.84 (s, 1H), suggesting that it was the hydrogen signal on the benzene ring, and it was 2, 3, 5, 6 four-substituted stupid, 7.35 ( m, 2H), 7.15 (m, 2H) suggest that the compound also has a 1,4 disubstituted benzene ring structure, with a symmetrical structure, 1.4 (t, J = 6.9Hz, 3H), 4.14 (q, J = 6.9Hz , 2H) prompts to contain ethoxy ...

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Abstract

The invention provides two related substances of mosapride citrate, wherein the two related substances of mosapride citrate are easily generated by mosapride citrate under the conditions of high temperature, high humidity and the like. The invention further provides a detection method of the two related substances, and application of the two related substances as impurity reference substances in detection of related substances in mosapride citrate and mosapride citrate preparations, so that a new direction is provided for improving the quality standard of raw material medicine and preparationsof mosapride citrate and obtaining mosapride citrate which is safe, reliable and exact in curative effect.

Description

technical field [0001] The invention provides a related substance of mosapride citrate and a preparation method thereof. The related substance can also be used for quality analysis of mosapride citrate and its preparation, and belongs to the field of pharmaceutical analytical chemistry. Background technique [0002] Mosapride Citrate (Mosapride Citrate, trade name Gasmotin) is a new type of gastric motility drug developed by Dainippon Pharmaceutical Co., Ltd. It is a potent and selective 5-HT4 receptor agonist and is clinically used to treat chronic gastritis , Functional dyspepsia, reflux esophagitis and relief of a series of gastrointestinal symptoms associated with surgery. The chemical name of mosapride citrate is: 4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobenzyl)-2-morpholinyl]methyl}benzyl Amide citrate, its chemical structural formula is: [0003] [0004] Molecular formula: C 21 h 25 ClFN 3 o 3 ·C 6 h 8 o 7 2H 2 O, molecular weight: 650.05. [0005] The ...

Claims

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Application Information

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IPC IPC(8): C07D265/30G01N30/02G01N30/74G01N30/06
CPCC07D265/30G01N30/02G01N30/74G01N30/06G01N2030/027
Inventor 柯潇陶莲春白晓春
Owner CHENGDU KANGHONG PHARMA GRP
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