Trimetazidine hydrochloride sustained release tablet taking glyceryl behenate as framework material and preparation method of trimetazidine hydrochloride sustained release tablet

Abstract

The invention belongs to the field of sustained-release drug preparations, and particularly relates to a trimetazidine hydrochloride sustained release tablet taking glyceryl behenate as a framework material and a preparation method of the trimetazidine hydrochloride sustained release tablet. According to the main technical scheme disclosed by the invention, a sustained-release preparation is prepared from trimetazidine hydrochloride as an effective component, only glyceryl behenate as a sustained-release framework material and auxiliary materials such as a small amount of release speed regulator. According to the trimetazidine hydrochloride sustained release tablet provided by the invention, an in vitro release rate experiment shows that the drug release is not affected by the pH environment, compared with commercially available 'vasorel' (trimetazidine dihydrochloride tablet), the trimetazidine hydrochloride sustained release tablet has good similarity (f2 is greater than 65); and the Beagle pharmacokinetic experiment in dogs shows that the trimetazidine hydrochloride sustained release tablet has bioequivalence in comparison with 'vasorel'. One trimetazidine hydrochloride sustained release tablet provided by the invention is taken twice a day, and the trimetazidine hydrochloride sustained release tablet is convenient to take, has good medicine compliance in patients, and is capable of keeping steady state plasma concentration for a long period of time. The preparation method disclosed by the invention is simple and stable in process, and is easily put into volume production.

Description

Technical field: [0001] The invention belongs to the field of sustained-release pharmaceutical preparations, and relates to a new dosage form of trimetazidine hydrochloride, which is used for the preventive treatment of angina pectoris and the auxiliary symptomatic treatment of dizziness and tinnitus. Trimetazidine hydrochloride slow-release tablet with glyceride as skeleton material and preparation method thereof. Background technique: [0002] Trimetazidine dihydrochloride, chemical name: 1-(2,3,4-trimethoxybenzyl)piperazine hydrochloride, is the first drug acting on the metabolism of cardiomyocytes, and the first 3-ketoacyl-CoA thiolase (3-KAT) inhibitor. Trimetazidine hydrochloride can inhibit fatty acid β-oxidation, accelerate the activation of pyruvate dehydrogenase (PDH), increase the oxidation of myocardial glucose and lactic acid, optimize myocardial energy metabolism, protect the production process of adenosine triphosphate, and reduce intracellular acidosis and ...

AI Technical Summary

Problems solved by technology

Hydrophilic gel material HPMC is the most commonly used sustained-release matrix material. Sustained-release tablets prepared with it as the matrix material have a burst release effect in the early stage of release, which seriously affects the sustained-release effect, especially for some drugs that require precise administration or dosage. The effect of smaller drugs is more obvious; the drug release process also changes due to changes in the pH of the gastrointestinal tract. Therefore, the application of HPMC sustained-release preparations is limited, and it is often used in combination with other matrix materials

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