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Medicine hydrate for treating dyspepsia and preparation method of medicine hydrate

A technology for indigestion and hydrate, which is applied in the field of medicine, can solve the problems that cannot be achieved, and achieve the effects of improving dissolution rate, improving bioavailability, yield and high purity

Inactive Publication Date: 2017-09-19
HUNAN QIWEI TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Invention After a large number of experimental studies, it was found that the acotiamide hydrochloride hydrate in the prior art has various technical problems such as stability, hygroscopicity, solubility, fluidity, and dissolution rate, and the prior art has also been solved by studying the crystal form. Its solubility, dissolution rate, hygroscopicity and other problems, but can not achieve the ideal state

Method used

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  • Medicine hydrate for treating dyspepsia and preparation method of medicine hydrate
  • Medicine hydrate for treating dyspepsia and preparation method of medicine hydrate
  • Medicine hydrate for treating dyspepsia and preparation method of medicine hydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Embodiment 1, the preparation of acotiamide hydrochloride hydrate

[0061] (1) under the sound field that frequency is 30KHz, output power is 50W, with the stirring velocity of 200 rev / mins, acotiamide hydrochloride crude product is added to volume be 6 times of acotiamide hydrochloride crude product weight while stirring. In the mixed solution of formamide and water, the volume ratio of formamide and water is 3.5:4.5, heat up and stir until dissolved;

[0062] (2) With the stirring speed of 200 revs / min, while stirring, add the n-butanol that volume is 3 times of acotiamide hydrochloride crude product weight;

[0063] (3) After adding n-butanol, under a sound field with a frequency of 20KHz and an output power of 15W, the temperature is lowered to 0-2°C at 3°C / hour, the crystal is grown for 4-6 hours, washed, and vacuum-dried to obtain albinohydrochloride Cotiamide hydrate 99.95g, yield 99.95%, purity 99.999%.

[0064] The X-ray powder diffraction spectrogram that th...

Embodiment 2

[0065] Embodiment 2, the preparation of acotiamide hydrochloride hydrate

[0066] (1) under the sound field that frequency is 25KHz, output power is 60W, with the stirring velocity of 260 revs / min, acotiamide hydrochloride crude product is added to the volume that is 5 times of acotiamide hydrochloride crude product weight while stirring. In the mixed solution of formamide and water, the volume ratio of formamide and water is 3.5:4.5, heat up and stir until dissolved;

[0067](2) With a stirring speed of 260 revs / min, adding volume while stirring is n-butanol that is 2 times of the crude product weight of acotiamide hydrochloride;

[0068] (3) After adding the n-butanol solution, under a sound field with a frequency of 15KHz and an output power of 20W, the temperature is lowered to 0-2°C at 2°C / hour, the crystal is grown for 4-6 hours, washed, and vacuum-dried to obtain hydrochloric acid Acotiamide hydrate 99.90g, yield 99.90%, purity 99.998%.

[0069] The X-ray powder diffr...

Embodiment 3

[0070] Embodiment 3, the preparation of acotiamide hydrochloride hydrate

[0071] (1) under the sound field that frequency is 25KHz, output power is 40W, with the stirring velocity of 150 rev / mins, acotiamide hydrochloride crude product is added to volume be 7 times of acotiamide hydrochloride crude product weight while stirring. In the mixed solution of formamide and water, the volume ratio of formamide and water is 3.5:4.5, heat up and stir until dissolved;

[0072] (2) With the stirring speed of 150 revs / min, while stirring, add the n-butanol that volume is 4 times of acotiamide hydrochloride crude product weight;

[0073] (3) After adding the n-butanol solution, under a sound field with a frequency of 15KHz and an output power of 10W, the temperature is lowered to 0-2°C at 4°C / hour, the crystal is grown for 4-6 hours, washed, and vacuum-dried to obtain hydrochloric acid Acotiamide hydrate 99.88g, yield 99.88%, purity 99.999%.

[0074] The X-ray powder diffraction spectru...

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Abstract

The invention belongs to the technical field of medicine and discloses a medicine hydrate for treating dyspepsia and a preparation method of the medicine hydrate. The disclosed medicine hydrate is an acotiamide hydrochloride hydrate and is high in purity and good in hydrothermal stability, an X-ray powder diffraction spectrum shown with 2 theta + / - 0.2 degree diffraction angles shows feature diffraction peaks at 5.2248 degrees, 6.1056 degrees, 6.6649 degrees, 9.3738 degrees, 12.3428 degrees, 15.1198 degrees, 17.2123 degrees, 23.3487 degrees, 24.1078 degrees, 24.4568 degrees, 25.2179 degrees, 26.0846 degrees, 27.1325 degrees, 28.7654 degrees and 29.9326 degrees, and completely different from the prior art, the X-ray powder diffraction spectrum measured with Cu-K alpha rays is shown in Figure 1.

Description

technical field [0001] The invention belongs to the technical field of medicine and discloses a drug hydrate for treating dyspepsia and a preparation method thereof, in particular to acotiamide hydrochloride hydrate and a preparation method thereof. Background technique [0002] Acotiamide hydrochloride hydrate, jointly developed by Japan's Zeli Shinyaku Co., Ltd. and Anstelles Pharmaceutical Co., Ltd., was first listed in Japan on June 6, 2013. The trade name is Chemical name: N-[2-(diisopropylamino)ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-4-thiazolecarboxamide hydrochloride compound, molecular formula: C 21 h 30 N 4 o 5 S·HCl·3H 2 O; Molecular weight: 541.06, its structure is as shown in formula (I): [0003] [0004] Functional dyspepsia is the most common digestive system disorder in clinical practice. In recent years, the incidence of functional dyspepsia has increased year by year. Epidemiological surveys in Europe and the United States show that 19...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/56
CPCC07B2200/13C07D277/56
Inventor 朱社凤
Owner HUNAN QIWEI TECH CO LTD