Revista Egitania Sciencia - Volume 17 | ARTICLE

Title: TECHNOLOGICAL DEVELOPMENT OF SUSTAINED RELEASE SOLID ORAL DOSAGE FORMS OF ALPRAZOLAM

Author: Andreia Melo (melo_andreiaf@hotmail.com), Cláudia Neves (cssn13@hotmail.com), Filipa Barros (filipabarros.barros@gmail.com), Sarah Pereira (sarah.pp@hotmail.com), Maximiano Ribeiro (mribeiro@ipg.pt), Paula Coutinho (coutinho@ipg.pt), André Araújo (andrearaujo@ipg.pt)

Publication: Revista Egitania Sciencia - Volume 17

Abstract:
Alprazolam is a benzodiazepine that belongs to the subgroup of anxiolytics, sedatives, and hypnotics, which constitutes the psychotropic subgroup with higher utilization levels over recent years. It acts on the central nervous system and is used mainly for the management of anxiety disorders and panic attacks that require ongoing therapeutic regimens. This shorter-acting benzodiazepine is normally prescribed in up to four doses per day for the treatment of anxiety and in more than four doses for the treatment of panic disorder. This dosage scheme can result in problems due to the lack of patient compliance and the stabilization of these pathologies. In this context, the modified release dosage forms could really be an important tool. There are two solid sustained release oral dosage forms of alprazolam, immediate and modified release, where the formerrelease the drug as soon as possiblethrough processes for rapid drug release and dissolution and the latter gradually release the drug and maintain its plasmatic concentration in therapeutic levels over a prolonged period of time after the administration of a single dose per day.
This research is focused on the exploitation of the conception of solid oral of sustained release dosage forms (tablets) containing alprazolam, by analysing their different excipients in comparison with immediate release dosage forms available on the market, and by examining the technologies behind their preparation. The excipient hydroxypropyl methylcellulose (or hypromellose) was determined to be exclusively responsible for the sustained release dosage forms. This hydrophilic polymer is resistant to disintegration caused by swelling from hydrationthat leads to formation ofa layer of gel at the surface of the tablet. The result is a barrier that controls water penetration and the release profile of the drug. The method used for this purpose was the modification of the dosage form by the incorporation of a specific excipient, a hydrophilic matrix system that has been widely used in oral controlled drug delivery systems.


Keywords: alprazolam; tablets; excipients; pharmaceutic technology; sustained release dosage forms




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