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Novel crystalline form of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex

A receptor antagonist, neutral endopeptidase technology, applied in the field of new crystal forms of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex, can solve the problem of stability and fluidity. Different compressibility and other problems, to achieve the effect of good stability and high water solubility

Active Publication Date: 2015-11-11
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, its stability, fluidity, and compressibility may also be different. These physical and chemical properties have a certain impact on the application of drugs.

Method used

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  • Novel crystalline form of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex
  • Novel crystalline form of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex
  • Novel crystalline form of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The LCZ696 crystal I was called 1G in the container, adding 6ml tetrahydrofurate to dissolve, slowly add this solution to 60ml cycane at room temperature, and slowly stir for 24h.Crystal II.

[0021] X-ray powder diffraction (XRPD)

[0022] The Rigakuultimaiv powder diffraction instrument is used to obtain the XRPD diagram of the LCZ696 crystal II. The instrument is irradiated with CU-Kα, and the D / Texultra detector is performed at room temperature.The scanning range is from 5 ° to 45 ° from 2θ, and the scanning speed is 20 ° / minute.

[0023] Table 1

[0024]

[0025] LCZ696 Crystal II infrared spectrum

[0026] The AgilentCary630 (ATR-FTIR) spectrum (AGILENTCARY630) was used to obtain the infrared absorption spectrum. -1 , The error range is 2cm -1 )),:,

[0027] 742 (M), 699 (M), 556 (W), 526 (W).

[0028] Elemental analysis

[0029] Element analysis obtains the following measurement values of the element in the sample.Within the error range, the element analysis result...

Embodiment 2

[0037] The LCZ696 crystal I was called 1G in the container, adding 6ml tetrahydrofurate to dissolve, slowly add this solution to the 60ml methyl unclein ether at room temperature, slowly stir for 24h, filter and vacuum dryer after drying and vacuum.The products obtained are the same as the embodiment 1.

Embodiment 3

[0039] The LCZ696 crystal I was called 1G in the container, adding 6ml isot butanol to dissolve, slowly add this solution to the 60ml methyl unclein ether at room temperature, slowly stir up for 24h, filter and vacuum dryer after drying and vacuum.The product obtained by the detection is the same as the embodiment 1.

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Abstract

The present invention discloses a novel crystalline form of an angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex. The novel crystalline form of the supramolecular complex has high water solubility and good stability. Experiments show that the moisture absorption and intrinsic dissolution extent and speed are superior to those of a conventional crystalline supramolecular complex.

Description

Technical field [0001] The invention involves a new crystal type and its preparation method of an ultra -molecular complex of a vascular tension antagonist (ARB) and a neutral endptides (NEP) inhibitor. Background technique [0002] The vascular tensioned body antagonist (ARB) and the neutral endptides (NEP) inhibitors provided by the present invention: [3- (1s, 3R) -1-linked benzene-4-base methyl group-3-ethyroxyl radio-1-clone aminosyl group) Pleorenic acid-(s) -3'-methyl-2 '-(pentraogl group {2"- (tetrazole-5-base negative ion)Lianzhen-4'-radio} amino) butadic acid] Sodium and half-five aqueous compounds (or "LCZ696").LCZ696 is developed by Norwatus, Switzerland, and can be used to treat hypertension and heart failure (acute and chronic). Its structure is shown in type A: [0003] [0004] WO2007056546 opens a crystal type of LCZ696, which is characterized by the X-ray powder diffraction diagram determined by SCINTAGXDS2000 powder diffraction meter to include the following l...

Claims

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Application Information

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IPC IPC(8): C07D257/04C07C233/47C07C231/24
CPCC07B2200/13C07C231/24C07C233/47C07D257/04
Inventor 任国宾齐明辉洪鸣凰刘岩陈景艳
Owner EAST CHINA UNIV OF SCI & TECH
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