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Acotiamide hydrochloride hydrate crystal form and preparation method thereof

A technology of acotiamide hydrochloride trihydrate and acotiamide hydrochloride, which is applied in the field of medicine, can solve problems such as affecting drug efficacy and differences, and achieves the effects of good repeatability, single crystal form and stable properties

Inactive Publication Date: 2014-08-13
HANGZHOU XINBOSI BIOMEDICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For pharmaceutical compounds, their physical and chemical stability under different storage conditions are very important, and different crystal forms may have significant differences in biochemical properties such as stability, solubility, and bioavailability, thus affecting drug efficacy

Method used

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  • Acotiamide hydrochloride hydrate crystal form and preparation method thereof
  • Acotiamide hydrochloride hydrate crystal form and preparation method thereof
  • Acotiamide hydrochloride hydrate crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Take 3.0 g of acotiamide hydrochloride hydrate and put it into 12.0 g of 20% aqueous methanol solution, and heat to reflux until dissolved. Cool to 20°C and filter. The filter cake was air-dried at 50°C until the moisture content was <8%. Place it in the air at room temperature until the water content is 9.8%-10.5%, to obtain 2.31 g of type A crystalline acotiamide hydrochloride hydrate with a yield of 77.0%.

Embodiment 2

[0036] Take 2.0 g of acotiamide hydrochloride anhydrate and put it into 8.0 g of 40% isopropanol aqueous solution, and heat to reflux until dissolved. Cool to 20°C and filter. The filter cake was air-dried at 50°C until the moisture content was <8%. Place in the air at room temperature until the water content is 9.8%-10.5%, to obtain 2.0 g of type A crystalline acotiamide hydrochloride hydrate with a yield of 90.0%.

Embodiment 3

[0038] Take 3.0 g of acotiamide hydrochloride hydrate and put it into 12.0 g of 20% acetonitrile aqueous solution, and heat to reflux until dissolved. Cool to 20°C and filter. The filter cake was air-dried at 50°C until the moisture content was <8%. Place in the air at room temperature until the water content is 9.8%-10.5%, to obtain 2.59 g of type A crystalline acotiamide hydrochloride hydrate with a yield of 86.3%.

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Abstract

The invention relates to a crystal form of an acotiamide hydrochloride hydrate shown as a chemical formula (I) and a preparation method thereof. Specifically, the present invention discloses an acotiamide hydrochloride hydrate of crystal form A and a preparation method thereof, and the XRPD characteristic peak is shown as in a figure 1. The preparation method of the acotiamide hydrochloride hydrate of crystal form A provided by the invention is safe, simple and strongly operable, the prepared acotiamide hydrochloride hydrate of crystal form A has single crystal form, stable property and good repeatability, and suitable for drug development.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a new crystal form of acotiamide hydrochloride hydrate and a preparation method thereof. Background technique [0002] Acofide hydrochloride hydrate, jointly developed by Japan's Zari Shinyaku Co., Ltd. and Anstelles Pharmaceuticals, was first launched in Japan on June 6, 2013, with the trade name Acofide?. Chemical name: N-[2-(diisopropylamino)ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-4-thiazolecarboxamide hydrochloride compound. Its structure is shown in formula (I): [0003] [0004] The indications of acotiamide hydrochloride hydrate are the prevention and treatment of epigastric discomfort, nausea, vomiting, heartburn, anorexia, flatulence, chronic gastritis, reflux esophagitis and post-gastrectomy syndrome. [0005] Functional dyspepsia is the most common digestive system disorder in clinical practice. In recent years, the incidence of functional dyspepsia ha...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426
CPCC07D277/56
Inventor 杜焕达丁建圣郑阳峰王万青刘艳华
Owner HANGZHOU XINBOSI BIOMEDICAL CO LTD
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