Sustained-release preparation for treating Alzheimer's disease and preparation method thereof

Abstract

The invention discloses a sustained-release preparation for treating Alzheimer's disease and a preparation method thereof. The sustained-release preparation is composed of a sustained-release tablet core and an immediate-release outer layer, and the immediate-release outer layer wraps the sustained-release tablet Core; by the weight of each tablet, the sustained-release tablet core is mainly prepared from the raw and auxiliary materials of the following weight: memantine hydrochloride 4.5-30mg, sustained-release material 45-160mg, lubricant 0.5-10mg, the rapid The release outer layer is mainly prepared from the following raw and auxiliary materials: 0.5-20mg of memantine hydrochloride, 330-370mg of filler, 2-15mg of lubricant, and 13-17mg of disintegrant. The sustained-release preparation prepared by the invention has quick onset, long-lasting and stable effects, and improves patient compliance.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a slow-release preparation for treating Alzheimer's disease and a preparation method thereof. Background technique [0002] Memantine hydrochloride is an N-formylaspartate receptor antagonist, which can block the pathological increase of glutamate level caused by abnormal nerve function, block calcium ion channels, and effectively regulate excitatory transmitters , to slow down the neurodegenerative process, thereby improving cognitive function, for the treatment of moderate to severe Alzheimer's type dementia (senile dementia). During the treatment of moderate and severe dementia patients with memantine, their cognitive function and behavioral ability improved significantly. As the current clinical first-line drug, memantine has few adverse reactions, good tolerance, high safety, and few drug-drug interactions, and is accepted by the majority of patients. At present, memantine hydrochl...

AI Technical Summary

Problems solved by technology

At present, memantine hydrochloride ordinary tablets sold on the domestic market can be divided into half doses according to needs at the initial stage, and taken twice a day. Most of the people who take this kind of medicine are the elderly. During the process of taking gradual doses, their vision and Dementia conditions can easily lead to inconvenient medication and wrong medication

Memantine ordinary preparations are absorbed quickly after oral administration, and the peak concentration is reached in a short period of time. Multiple administrations are then used to compensate for fluctuations in blood concentration, but this still increases the risk of side effects for patients and poor patient compliance

[0003] In the prior art, there are ① using HPMC as the matrix sustained-release material to prepare oral sustained-release tablets of memantine. However, although this preparation can achieve a sustained-release effect, the release cannot meet the required blood concentration requirements in the early stage , and the stability of the single matrix sustained-release tablet is poor, and the dissolution becomes faster after long-term storage, and even loses the sustained-release effect; ② There is also a capsule preparation composed of an immediate-release part and a sustained-release part, wherein the immediate-release part and the drug layer; the sustained-release part is composed of a blank core, a drug layer and a release-controlling layer. The purpose of regulating the release is achieved by combining different proportions of immediate-release pellets, sustained-release pellets and coating thickness, but this technology has obvious shortcomings The preparation process is complex, time-consuming and costly

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