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Pharmaceutical composition containing antidepressant drug

IP.com Disclosure Number: IPCOM000149839D
Publication Date: 2007-Apr-10
Document File: 2 page(s) / 33K

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Pharmaceutical composition containing antidepressant drug

S(+)-1-[3-(dimethyl-amino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile in the form of pharmaceutically acceptable salt is a potent oral selective serotonin reuptake inhibitor.Tablets are available as 5 mg, 10 mg and 20 mg tablets for oral administration. Also other dosages can be prepared such as 2.5 mg, 7.5 mg, 15 mg or any other.

Tablets can be prepared using direct compression, wet granulation or dry granulation technique. The first one is popular due to its simplicity and reproducibility. Both granulation techniques are used, when the powder mixture of the tablet core components does not possess suitable flow properties, blend homogeneity and/or compressibility.

Particle size of the active ingredient was below 20 microns, therefore the granulation technique was selected, using the lactose monohydrate as the primary carrier/filler in the process of the agglomeration. Average particle size of the lactose monohydrate was below 100 microns. For this purpose for example GranuLac 230, Wyndale Milled 300 Meshor various types of Pharmatose can be used.

As an effective disintegrant, crospovidone was distributed equally to intragranular and extragranular phase. The distribution of the crospovidone enabled adequate disintegration of the tablet and granules, and subsequent dissolution of the active ingredient. Instead of crospovidone the Sodium starch glycolate or Croscarmellose Sodium could successfully take over the role of the disintegrant.

To retain the suitable flow properties, for the extragranular phase the excipients were chosen, with similar particle size as granulate. Microcrystalline cellulose Avicel®PH 200 was the optimal choice. For any other particle size distribution of granules the suitable extragranular filler could be selected. In addition to its filler properties, microcrystalline cellulose has also characteristics of the binder and disintegrant, due to its plastic properties and highly porous structure, respectively. This contributes to...