Sustained-release micro-pellet of trimetazidine and preparation process thereof

Abstract

The invention relates to a slow-release micro drop whose active component is Humeitashen or other salt, wherein it is formed by element and film layer that controlling the drug release, whose weight ratio is 20:1-5:1; the Humeitashen content of element is 10-60%. The invention mainly uses protrusion method to prepare drop, and uses fluidize bed to pack.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and specifically relates to a sustained-release pellet containing an active ingredient trimetazidine or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] The chemical name of trimetazidine is 1-(2,3,4-trimethoxybenzyl)piperazine, and its structural formula is as follows: [0003] [0004] Trimetazidine can form a salt with acid. At present, its dihydrochloride has been widely used clinically at home and abroad, mainly for the preventive treatment of angina pectoris, and the auxiliary symptomatic treatment of vertigo and tinnitus. With the gradual deepening of clinical research, trimetazidine is expected to become the first-line anti-myocardial ischemia drug. [0005] Trimetazidine belongs to the class of other antianginal cardiovascular drugs. Trimetazidine prevents the decrease of intracellular ATP level by...

AI Technical Summary

Problems solved by technology

There are two disadvantages in the formation process of the controlled-release film: one is that the film-forming temperature of the film material is high, and a large amount of plasticizer must be added to promote the film-forming process, and the plasticizer has a great influence on the release behavior of the drug, which is very unfavorable. It is beneficial to maintain a stable drug release curve; the second is that if the water dispersion coating of the above-mentioned film material is used, heat treatment must be carried out at 40°C to 60°C for more than 24h after completion, which not only makes the process complicated, but also greatly increases the production cost. Drug stability is also unfavorable

[0024] The currently commercially available trimetazidine hydrochloride tablets (trade name: Wanshuangli) are rapidly absorbed after oral administration, and reach the peak plasma level in less than 2 hours. The elimination half-life is about 6 hours. It needs to be taken at least 3 times a day. Therefore, the blood drug concentration in the body is prone to "peak and valley" phenomenon, which not only maintains the effective blood drug concentration for a short time, but also has serious side effects and poor patient compliance.

Especially when taking the medicine at night, the time interval until the morning is long, and the blood drug concentration is very low in the morning, so the drug effect cannot be exerted smoothly

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