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A kind of trimetazidine oxalate and its preparation method and application

A technology of trimetazidine and oxalate, which is applied in the field of medicine, can solve the problems of trimetazidine hydrochloride fluidity, poor tabletability and hygroscopicity, and affect the quality of finished tablets, so as to improve fluidity and reduce moisture absorption rate , the effect of increasing the specific surface area

Active Publication Date: 2021-05-07
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Abstract
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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 tabletability and hygroscopicity, and the problem that it is made into tablets and affects the quality of finished tablets

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  • A kind of trimetazidine oxalate and its preparation method and application

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Embodiment Construction

[0038] 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.

[0039] The present embodiment provides a kind of trimetazidine oxalate, its molecular formula is C 18 h 26 N 2 o 11, the trimetazidine oxalate is obtained by reacting trimetazidine and oxalic acid in a molar ratio of 1:2. The specific preparation process is as figure 1 shown.

[0040] 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 adj...

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Abstract

The invention provides a kind of trimetazidine oxalate, its molecular formula is C 18 h 26 N 2 o 11 , the trimetazidine oxalate is obtained by reacting trimetazidine and oxalic acid in a molar ratio of 1:2. The angle of repose of the trimetazidine oxalate is smaller than that of trimetazidine hydrochloride, and its surface morphology is flaky, which improves the fluidity and moisture absorption of the drug compared with the prismatic crystals of the trimetazidine hydrochloride bulk drug At the same time, the tensile strength of the trimetazidine oxalate reaches a maximum value of 4.66MPa at 150MPa, which is significantly higher than the tensile strength of trimetazidine hydrochloride under the same pressure, which improves the tableting performance of the drug.

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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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/096C07C55/07C07C51/41A61K31/495A61K9/20A61K47/38A61K47/26A61K47/02A61P9/00A61P9/04A61P9/10
CPCA61K9/2009A61K9/2018A61K9/2054A61P9/00A61P9/04A61P9/10C07B2200/13C07C55/07C07D295/096
Inventor 葛月宾
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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