Long-acting sustained-release pellet and preparation method thereof

Abstract

The invention discloses a long-acting sustained-release pellet and a preparation method thereof. The long-acting trimetazidine hydrochloride sustained-release pellet comprises a drug-containing core and a sustained-release coating layer from inside to outside sequentially, wherein an optional isolation coating layer is arranged between the drug-containing core and the sustained-release coating layer; the isolation coating layer accounts for 0-15 percent of the mass of the drug-containing core, and the sustained-release coating layer accounts for 5-30 percent of the mass of the drug-containing core; a gastrointestinal adhesive is contained in the sustained-release coating layer. According to the trimetazidine hydrochloride sustained-release pellet, the prescription is meticulously designed, the drug-containing core is uniformly coated by utilizing the sustained-release coating material, so that slow and uniform drug release of the drug-containing core can be maintained, the active component releasing speed can be reduced, the time for reaching the peak can be postponed, the pellet can be constantly and stably released in 24 hours, the blood concentration stability can be maintained, and the phenomenon of insufficient blood concentration in morning ischemia can be avoided. The administration frequency can be reduced to once a day, and the compliance of patients can be improved.

Description

technical field [0001] The invention relates to a sustained-release preparation, in particular to a long-acting trimetazidine hydrochloride sustained-release pellet with a sustained-release time of up to 24 hours. The invention also relates to a preparation method of the preparation. Background technique [0002] Trimetazidine Dihydrochloride (TMZ), as a new class of effective drugs for the prevention and treatment of angina pectoris, has been widely used in many countries and regions, and has a good effect on the treatment of angina pectoris. The ordinary tablet of trimetazidine hydrochloride entered my country in 2000, and now the product has been listed in the National Essential Drug List. [0003] Trimetazidine hydrochloride is 1-(2,3,4-trimethylphenyl)piperazine dihydrochloride, with a molecular weight of 339.3 and a molecular formula of C 14 h 22 N 2 o 3· 2HCl, very soluble in water. The absorption rate of trimetazidine hydrochloride in the body is fast, and the ...

AI Technical Summary

Problems solved by technology

The pellets of this invention patent contain two kinds of pellets: immediate-release pellets and sustained-release pellets. Due to the inconsistency of the wrapping materials and wrapping thicknesses of the instant-release pellets and the sustained-release pellets, there are differences in bulk density and volume size, which will inevitably lead to The drug content of the pellets is different, which affects the stability of the therapeutic effect

[0009] These sustained-release preparations are convenient for patients to use to a certain extent, but due to gastric emptying and normal metabolism of the human body, the time that oral sustained-release preparations stay in the body after taking is generally less than 10h, which has also led to existing oral sustained-release preparations. Need to be taken at least twice a day to ensure adequate blood levels

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