Acotiamide hydrochloride dihydrate crystal, and preparation method and applications thereof

A technology of acotiamide hydrochloride and dihydrate, which is applied to the crystal form of acotiamide hydrochloride dihydrate and the field of preparation thereof, and can solve the problem that no literature mentions the crystal form of acotiamide hydrochloride dihydrate and its preparation. Preparation method, no mention of crystal form spectral data and drug application, etc., to achieve the effects of stable chemical properties, stable properties and high yield

Active Publication Date: 2016-04-13
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, no literature has mentioned the crystal form and preparation method of acotiamide hydrochloride dihydrate, let alone the characteristic peaks and spectral data of the crystal form and its drug-related applications

Method used

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  • Acotiamide hydrochloride dihydrate crystal, and preparation method and applications thereof
  • Acotiamide hydrochloride dihydrate crystal, and preparation method and applications thereof
  • Acotiamide hydrochloride dihydrate crystal, and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Add 20.0 g of acotiamide hydrochloride trihydrate and 200 mL of ethanol into the reaction flask, raise the temperature to reflux, stir for 30 min, and naturally cool to room temperature with stirring to crystallize, filter, and dry the filter cake at 60 ° C to obtain 16.6 g of hydrochloric acid Acotiamide dihydrate has a yield of 83.0% and a purity of 99.86%.

[0070] Measure the X-ray powder diffraction pattern, such as figure 1 The detailed parameters are shown in Table 2, showing the position of the diffraction peak: 2θ value (°); the relative intensity of the diffraction peak: peak height (Height%).

[0071] The X-ray diffraction parameter of the crystal form of acotiamide hydrochloride dihydrate of table 2

[0072]

[0073]

[0074] Differential thermal analysis and thermogravimetric analysis are carried out to the prepared acotiamide hydrochloride dihydrate, wherein the DCS collection of illustrative plates is as follows image 3 , TG spectrum such as Fi...

Embodiment 2

[0078] The stability of acotiamide hydrochloride dihydrate obtained in Example 1 was investigated, and acotiamide hydrochloride trihydrate was used as a contrast. The test results are shown in Table 3:

[0079] Table 3 Stability test results of acotiamide hydrochloride dihydrate prepared in Example 1 of the present invention

[0080]

[0081] The test results show that the crystal form of acotiamide hydrochloride dihydrate of the present invention has stable physical and chemical properties, has no obvious hygroscopicity in the influencing factor test and accelerated test, and the crystal form does not change.

Embodiment 3

[0083] Investigate the solubility of acotiamide hydrochloride dihydrate crystal form of the present invention, measure the solubility of acotiamide hydrochloride dihydrate in a series of buffer solutions within the physiological pH range, use acotiamide hydrochloride trihydrate crystal Type is control, and the test results are shown in Table 4:

[0084] Table 4 Solubility Test Results

[0085]

[0086] The test results show that the dihydrate crystal form of acotiamide hydrochloride of the present invention is compared with the original marketed acotiamide hydrochloride trihydrate crystal form, and the solubility in three pH ranges in the two media is similar, indicating that the dihydrate crystal form The solubility is better than that of the trihydrate crystal form.

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PUM

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Abstract

The invention belongs to the field of crystal drug, and especially relates to an acotiamide hydrochloride dihydrate crystal, and a preparation method and applications thereof. The chemical properties of the acotiamide hydrochloride dihydrate crystal are stable; no obvious hygroscopicity is detected in influence factor tests and acceleration tests, and crystal form is not changed; and the content of related substance is low. The solubility of the acotiamide hydrochloride dihydrate crystal is slightly higher, and the dissolution rate of prepared tablets is slightly higher. The preparation method of the acotiamide hydrochloride dihydrate crystal is simple; no complex equipment is needed; preparation period is short; and product yield is 83% or higher.

Description

technical field [0001] The invention relates to the field of crystalline drugs, in particular to a crystalline form of acotiamide hydrochloride dihydrate and a preparation method and application thereof. Background technique [0002] Acotiamide hydrochloride trihydrate, 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 The chemical name is N-[2-[bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]thiazole-4- Formamide hydrochloride trihydrate, the English name is AcotiamideHydrochlorideHydrate, and its structural formula is as formula I. [0003] [0004] Acotiamide hydrochloride trihydrate is the first drug approved globally for the treatment of functional dyspepsia, which can inhibit the activity of peripheral acetylcholinesterase. Acetylcholine is a neurotransmitter that plays an important role in the regulation of gastrointestinal motility, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/56A61K31/426A61P1/14
CPCC07D277/56
Inventor 王东张宪美谈敦潮方胜邹德超赵大龙王珂
Owner BEIJING COLLAB PHARMA
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