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Trimetazidine oxalate and preparation method and application thereof

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

Active Publication Date: 2019-08-09
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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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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  • 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

[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 15 h 23 N 2 o 5, the trimetazidine oxalate is obtained by reacting trimetazidine and oxalic acid at a molar ratio of 2:1. 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 adju...

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Abstract

The invention provides trimetazidine oxalate. The molecular formula of the trimetazidine oxalate is C15H23N2O5, and the trimetazidine oxalate is obtained through a reaction of trimetazidine and oxalicacid in a molar ratio of 2:1. The angle of repose of the trimetazidine oxalate is smaller than that of trimetazidine hydrochloride, the surface appearance of the trimetazidine oxalate is flaky, and compared with a prismatic crystal of the trimetazidine hydrochloride bulk drug, the fluidity and hygroscopicity of the drug are improved; the tensile strength of the trimetazidine oxalate reaches the maximum value of 2.60 MPa at 350 MPa, and is significantly higher than that of the trimetazidine hydrochloride under the same pressure, and the flake formation 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): C07D295/096A61K31/495C07C55/07C07C51/41A61P9/10A61P9/04A61P9/00
CPCA61P9/00A61P9/04A61P9/10C07C51/412C07D295/096C07C55/07
Inventor 葛月宾
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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