Trimetazidine oxalate and preparation method and application thereof

A technology of trimetazidine and oxalate, applied in the field of medicine, can solve the problems of trimetazidine hydrochloride, poor hygroscopicity, poor hygroscopicity, influence on the quality of finished tablets, etc., so as to improve the fluidity and reduce the hygroscopic rate. , the effect of improving hygroscopicity

Active Publication Date: 2019-08-30
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

[0007] The purpose of the present invention is to overcome the fluidity of existing trimetazidine hydrochloride, poor ta

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  • Trimetazidine oxalate and preparation method and application thereof
  • Trimetazidine oxalate and preparation method and application thereof
  • Trimetazidine oxalate and preparation method and application thereof

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Embodiment Construction

[0037] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0038] The present embodiment provides a kind of trimetazidine oxalate, its molecular formula is C 16 h 24 N 2 o 7 , the trimetazidine oxalate is obtained by reacting trimetazidine and oxalic acid at a molar ratio of 1:1. The specific preparation process is as figure 1 shown.

[0039] Weigh about 5g of trimetazidine hydrochloride crude drug in a small beaker, add 5mL of ultrapure water to dissolve. Slowly add 10% sodium hydroxide solution dropwise to adjus...

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Abstract

The invention provides trimetazidine oxalate. The molecular formula of trimetazidine oxalate is C16H24N2O7. Trimetazidine oxalate is obtained by reacting trimetazidine with oxalic acid in a molar ratio of 1:1. The repose angle of trimetazidine oxalate is less than that of trimetazidine hydrochloride, the surface morphology of trimetazidine oxalate is flake-shaped, and trimetazidine oxalate improves the fluidity and hygroscopicity of a drug compared to prismatic crystals of trimetazidine hydrochloride bulk drug. At the same time, the tensile strength of trimetazidine oxalate reaches a maximum value of 3.99 MPa at 150 MPa, and is significantly higher than the tensile strength of trimetazidine hydrochloride under the same pressure, so that the tableting performance of the drug is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a trimetazidine oxalate and a preparation method and application thereof. Background technique [0002] Trimetazidine hydrochloride protects the energy metabolism in ischemic and hypoxic cardiomyocytes, prevents the decrease of intracellular ATP levels, ensures the function of ion pumps while maintaining the intracellular environment, and improves the normal transport of transmembrane sodium-potassium pumps. Animal experiments have shown that trimetazidine hydrochloride helps maintain energy metabolism in ischemic and hypoxic myocardial cells, and can also reduce the size of solid myocardial infarction without any direct hemodynamic effects. Controlled trials in patients with angina pectoris have shown that it can increase coronary blood flow reserve in humans, treat myocardial ischemia induced by slow exercise, limit rapid blood pressure fluctuations without causing...

Claims

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Application Information

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IPC IPC(8): C07D295/096C07C55/07C07C51/41C07C51/43A61K31/495A61K9/20A61P9/10A61P9/04A61P9/00
CPCA61K9/2059A61K9/2095A61P9/00A61P9/04A61P9/10C07B2200/13C07C51/412C07C51/43C07C55/07C07D295/096
Inventor 葛月宾
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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