Memantine slow-release micro-tablet capsules and preparation method thereof

Abstract

The invention belongs to the technical field of a medicine slow-release preparation, and particularly relates to slow-release micro-matrix-tablet capsules containing active components namely memantineand a preparation method of the slow-release micro-matrix-tablet capsules. When hydrochloric acid memantine slow-release capsules are taken, the dosage needs to be increased progressively, high dosage requirements are needed, the slow-release micro-matrix-tablet capsules are small in size, each of the slow-release micro-matrix-tablet capsules is about 20-30mg, 4 micro tablets are contained, 4 divided dose units are contained, and the 4 micro tablets can be loaded into small No.4 capsules, so that the slow-release micro-matrix-tablet capsules have great compliance to old people suffering fromAlzheimer's Disease( Alzheimer's Disease, AD). Therefore, if the hydrochloric acid memantine slow-release capsules can be successfully developed, the hydrochloric acid memantine slow-release capsulescan obtain good clinical advantages. Based on the reasons, the recipe of the hydrochloric acid memantine slow-release capsules is firstly researched, but the raw material of hydrochloric acid memantine is good in water solubility, development of matrix slow-release micro tablets is difficult, and the hydrochloric acid memantine is considered to be reduced to memantine (base), and then is preparedinto the memantine slow-release micro-tablet capsules, so that the difficulty of the recipe and technological design can be basically solved, and the memantine slow-release micro-tablet capsules can be successfully developed.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and in particular relates to a sustained-release micro-skeleton tablet capsule containing active ingredient memantine and a preparation method thereof. Background technique [0002] The chemical name of memantine is 1-amino-3,5-dimethylamantadine, and its structural formula is as follows: [0003] [0004] Molecular weight of memantine: 179.26, molecular weight of memantine hydrochloride: 215.76. It can be found from the Drugbank database that the solubility of memantine is 0.9 mg / mL, and the solubility of memantine hydrochloride is 35 mg / mL, which indicates that memantine is very slightly soluble in water, while memantine hydrochloride is soluble in water. [0005] Memantine hydrochloride is a novel, low-moderate affinity, voltage-dependent, non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, which can non-competitively block NMDA receptors and reduce...

AI Technical Summary

Problems solved by technology

Because micro-tablets need to be taken in capsules, in terms of dosage and filling convenience, this size and shape is the most suitable. If it is too small, it will increase the difficulty of development and production. If it is too large, it will basically enter the category of ordinary tablets and cannot be used. Reflect the superiority of microchips

[0010] The total dose of microtablet capsules should generally not exceed 50mg, because each microtablet needs to add other excipients in addition to the raw material medicine to form, so the total weight of each microtablet generally does not exceed 30mg, and higher doses of drugs are made into tablets Sub-standards can be considered, thus losing the necessity of developing microtablet capsules

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