Mirtazapine Solid Dosage Forms

Abstract

A non-effervescent, solid dosage form containing mirtazapine, which is used to form mirtazapine pharmaceutical tablets. The dosage form contains mirtazapine, a hydrophilic component, and at least one lubricant. In some embodiments, the dosage forms contain a salivating agent. Processes for producing mirtazapine orally disintegrating tablets are also provided.

Description

[0001]The application claims the benefit of U.S. Provisional Application No. 60 / 491,279, filed Jul. 31, 2003, which is herein incorporated by reference in its entirety.BACKGROUND OF THE INVENTION [0002]1. Field of the Invention[0003]The present invention is generally related to solid dosage forms of mirtazapine for the treatment of depression and other neurological disorders and diseases.[0004]2. Related Art[0005]Mirtazapine is the common name of the isomeric compound 1,2,3,4,10,14β-hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c]benzazepine. The use of mirtazapine is well known for the treatment of depression and the symptoms associated with depression including, memory loss, changes in mood, insomnia, lethargy, increase or decrease in weight, and anxiety.[0006]Mirtazapine treats depression by antagonizing the adrenergic 5-HT2A, 5-HT3, and alpha 2 autoreceptors and alpha 2-heteroreceptors, and enhancing the release of norepinephrine and 5-HT1A-mediated serotonergic transmission. It i...

AI Technical Summary

Benefits of technology

"The patent describes a non-effervescent, solid dosage form for oral administration that does not rely on effervescence for disintegration. The dosage form includes a combination of mirtazapine and a hydrophilic component, which can be selected from a variety of options such as cellulose derivatives, polyol, and carbohydrates. The dosage form also includes a lubricant and a salivating agent. The solid dosage form has a dissolution rate of at least 75% in five mins in a medium of 0.1 N HCl with a paddle speed of 50 rpm. The invention also provides a process for making the solid dosage form."

Problems solved by technology

Unfortunately such compositions may be associated with certain disadvantages, particularly in the treatment of pediatric or geriatric patients, who may dislike or have difficulty in swallowing such compositions, or where administration of a conventional tablet, pill or capsule is not feasible.

However, a liquid preparation has shortcomings regarding difficulties in handling, especially in measuring an accurate dosage, and that it is not suitable for drugs which are unstable in a moist environment.

These dosage forms provide significant problems in terms of production, storage, transport and during consumer usage.

They are also significantly more costly to produce than conventional tablets.

However, effervescent tablets containing an alkalizing agent are usually moisture sensitive, may be incompatible with an acidic drug and require protection due to their sensitivity to humidity.

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