Trimetazidine hydrochloride mono-layer osmotic pump controlled release tablet and preparation method thereof

Abstract

The invention provides a trimetazidine hydrochloride mono-layer osmotic pump controlled release tablet and a preparation method thereof. The tablet is composed of a core, a coating membrane, and pores. The core comprises the following components, by weight percentage: 10-25% of trimetazidine hydrochloride, 8-35% of an osmotic pressure active substance, 16-50% of a suspension, 12-47% of a filler, and 0.5-1.5% of a lubricant. The coating membrane comprises, every 100 tablets: 1-10g of a pore forming agent, 1-10g of a plasticizer, 10-40g of a film forming material, and a proper amount of an solvent. The weight gain of the coating membrane is 4-10% of the weight of the core. The diameter of each pore is in a range of 0.6-1.2 mm. According to the trimetazidine hydrochloride mono-layer osmotic pump controlled release tablet, the auxiliary materials are high in security; the release accords with zero-level release; stability of a plasma concentration can be maintained; frequency of medicine administration for a patient is reduced; and the toxic and side effect of the medicine is minimized. The preparation method is simple, and the raw materials are less, so that the preparation method is suitable for industrial production.

Description

technical field [0001] The invention relates to a trimetazidine hydrochloride single-layer osmotic pump controlled-release tablet and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Angina pectoris is a common cardiovascular disease, which is caused by coronary artery atherosclerosis and stenosis, coronary artery insufficiency, temporary myocardial ischemia and hypoxia, and a group of comprehensive symptoms with precordial pain as the main clinical manifestation. It is a kind of coronary heart disease with the highest incidence rate, which seriously threatens the health and life of human beings. Trimetazidine hydrochloride is a new drug against myocardial ischemia, its chemical name is 1-[(2,3,4-trimethylphenyl)methyl]-piperazine dihydrochloride, and its relative molecular mass is 339.3 . Its mechanism of action is to improve cardiac function by inhibiting myocardial fatty acid β oxidation and promoting glu...

AI Technical Summary

Problems solved by technology

To ensure adequate plasma concentrations, a dosing regimen of 3 times a day is most often required during treatment, causing significant inconvenience to patients

Trimetazidine hydrochloride is absorbed quickly in the body and has a half-life of about 6 hours. After taking it, it can reach a high plasma concentration in a short period of time, but the blood concentration is very low when the next medication is taken, especially in the most severe ischemia. In the morning, the curative effect of ordinary dosage forms is poor, and the side effects are relatively large for patients

[0004] Invention patent CN102133195A is the sustained and controlled release pellets of trimetazidine hydrochloride, but there are problems such as cumbersome methods, complicated process, and long preparation cycle, and the patent does not indicate its release in vitro; invention patent CN104473905A is trimetazidine hydrochloride skeleton control type sustained-release pellet capsules, the process is simple, but the release is faster in the early stage, and the release rate is not constant; the invention patents CN103385861A and CN102885795A are trimetazidine hydrochloride sustained-release tablets, which use a sustained-release matrix material, and there is a burst release in the early stage. The drug rate is not constant; the invention patent CN103550183A is a trimetazidine hydrochloride osmotic pump controlled-release tablet, which uses an adhesive and the preparation process is relatively complicated; the invention patent CN103735538A is a double-layer trimetazidine hydrochloride osmotic pump controlled-release tablet , because trimetazidine hydrochloride has good water solubility, it is not necessary to make a double-layer push-pull osmotic pump, and the double-layer osmotic pump needs to be drilled on the side of the drug-containing layer when drilling, which is not conducive to industrial production

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