Olanzapine orally disintegrating tablet and preparation method thereof

Abstract

The invention provides an olanzapine orally disintegrating tablet. The olanzapine orally disintegrating tablet is composed of olanzapine, microcrystalline cellulose, mannitol, fructose, colloidal silicon dioxide, a disintegrating agent and a lubricant. The composition does not contain an aspartame flavoring agent. The olanzapine orally disintegrating tablet is low in weight (high in drug loading capacity of auxiliary materials), and has reduction of production procedures and production cost. The olanzapine orally disintegrating tablet has good mechanical strength in a low hardness range while achieving rapid disintegration and rapid action. The olanzapine orally disintegrating tablet meets requirements on hardness and friability in the processes of tablet preparation, production, transportation and use.

Description

Technical field [0001] The present invention belongs to the technical field of pharmaceutical preparations, in particular it relates to orally disintegrating olanzapine tablets and its preparation method. Background technique [0002] Olanzapine (Olanzapine), chemical name 2-methyl-10- (4-methylpiperazin-1-piperazinyl) -4H- thieno [2,3-b] [1,5] benzodiazepine Zhuo, a new atypical neuroleptics, to, 5-HT receptors, and cholinergic receptors and dopamine receptors, and antagonize, antagonize D2 receptor and treatment of positive symptoms of schizophrenia ; antagonize 5-HT2A receptor and treatment of negative symptoms of schizophrenia related. [0003] It refers to an orally disintegrating tablets within 30 seconds on the surface of the tongue that can automatically particles disintegrate into numerous sweet taste and novel pharmaceutical formulations. Due to its disintegration speed, rapidly absorbed, and after taking without water, it is very suitable for some special patients (psy...

AI Technical Summary

Problems solved by technology

Mannitol dissolves quickly in the mouth and has a good taste. It is very suitable as a diluent for orally disintegrating tablets. However, in large-scale production, too much mannitol in the prescription often leads to sticking and punching during tablet compression, and poor hardness and formability As a result, the prepared orally disintegrating tablets have poor friability, which in turn leads to serious damage to the aluminum package and during transportation, which is ultimately inconvenient for patients to take

[0006] Chinese patent application number 201310451237.7 discloses an orally disintegrating olanzapine tablet and a preparation method thereof. The composition of the invention is olanzapine, microcrystalline cellulose, mannitol, cross-linked polyvinylpyrrolidone, aspartam and stearin Magnesium acid, using powder direct compression technology, is characterized in that the disintegration time limit is less than 10s, but the requirements for the amount and type of excipients are relatively high, and the drug loading of excipients is low, which is not conducive to clinical drug use and increases production costs

[0007] Chinese patent 201610583234.2 discloses an olanzapine orally disintegrating tablet and its preparation method, which is characterized in that the drug combination includes olanzapine granules and additives. The water body of polyvinylpyrrolidone and polyvinyl acetate is obtained by granulation, and then mixed with diluent, disintegrant, flavoring agent and lubricant, and then compressed into tablets. Its main feature is to improve the taste-masking performance of olanzapine, It can reduce the sticking phenomenon of mannitol, but the production process is complicated and the cost is high, and the risk of olanzapine stability is greatly increased in the wet coating process

[0008] Chinese patent application number CN200910016306.5 discloses a olanzapine orally disintegrating tablet preparation and a preparation method thereof. The composition is olanzapine, mannitol, lactose, dry binder, disintegrant, flavoring agent, lubricant; The preparation process can adopt dry direct compression technology and dry compression granulation technology, which is characterized by the use of lactose and mannitol as fillers, which reduces the risk of large-scale production splits, but has higher requirements on the amount and type of auxiliary materials. The drug loading is low and the tablet weight is large, which is not conducive to clinical drug use and increases the production cost

[0011] The orally disintegrating tablets prepared by the above-mentioned patents all have different degrees of gritty feeling and poor mouthfeel, which are not enough for patients to take comfort. In addition, there are also poor quality such as slow dissolution, content uniformity, absorbability, friability, and stability. risk, and there is also the problem of high cost caused by large tablet weight and cumbersome process

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