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Itakaline hydrochloride A crystal form and preparation method thereof

A crystal form, Carlin technology, applied in the field of medicine, can solve problems such as easy crystal transformation, unfavorable drug storage and transportation, and instability

Active Publication Date: 2022-03-15
江苏恩华赛德药业有限责任公司 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

CN1250519C disclosed ertacarline hydrochloride is recrystallized with 1: 1 isopropanol-cyclohexane, and the white solid that obtains is detected by X-RAY, is called crystal form I; The crystalline form of ertacarline hydrochloride obtained by the deuterated ertacarline hydrochloride crystallization process is also the crystalline form I; in-depth research has found that the crystalline form I is unstable under high humidity and high temperature conditions, and it is easy to crystallize, which is not conducive to the development of drugs. storage and transport

Method used

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  • Itakaline hydrochloride A crystal form and preparation method thereof
  • Itakaline hydrochloride A crystal form and preparation method thereof
  • Itakaline hydrochloride A crystal form and preparation method thereof

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Embodiment Construction

[0021] In the specification and claims of the present application, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. However, for a better understanding of the present invention, definitions and explanations of some related terms are provided below. In addition, when the definitions and explanations of terms provided in this application are inconsistent with the meanings commonly understood by those skilled in the art, the definitions and explanations of terms provided in this application shall prevail.

[0022] During the heating process of DSC, the melting endothermic peaks of DSC are double peaks, the first one is peak 1, the second one is peak 2, the peak value of peak 1: 231.7 ℃, the starting point: 227.1 ℃, the ending point: 233.3 ℃ ; Peak value of peak 2: 236.5°C, start point: 234.5°C, end point: 242.2°C.

[0023] The crystal form A of itacarline hydrochloride provided by the pr...

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Abstract

The present invention relates to a crystal form A of ertacarline hydrochloride and a preparation method thereof. The crystal form A of ertacarline hydrochloride obtained in the present invention has good crystal form stability and chemical stability, and has good bioavailability It can be better used in clinical treatment.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the A crystal form of etakaline hydrochloride and a preparation method thereof. Background technique [0002] Iptakalim hydrochloride (iptakalim) is a new class of K ATP Opening agent, is a new type of antihypertensive drug, CN1250519C discloses the structure of ertacarline hydrochloride and its colorless solid obtained through recrystallization, Chinese Journal of Medicinal Chemistry, Volume 14, No. 3, 2004, deuterium-labeled ertacarline hydrochloride The structural formula of ertacarin hydrochloride disclosed in the synthesis of lin and its mass spectrometry cleavage pathway is as follows: [0003] . [0004] The crystal structure of the pharmaceutical active ingredient often affects the chemical stability of the drug. Different crystal forms, preparation methods and storage conditions may lead to changes in the crystal structure of the compound, sometimes accompanied by...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C211/08C07C209/84A61K31/131A61P9/12
CPCC07C211/08C07C209/84A61P9/12C07B2200/13
Inventor 任婷王国海杨盼侯媛媛杨永林陈亮
Owner 江苏恩华赛德药业有限责任公司
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