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Central Nervous System Agents in Medicinal Chemistry

Author(s): Vishal Bhatia, Ashwani K. Dhingra*, Rameshwar Dass, Bhawna Chopra and Kumar Guarve

DOI: 10.2174/1871524922666220624113719

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Formulation, Development, and in-vitro Evaluation of Escitalopram Fast Dissolving Tablets

Page: [198 - 213] Pages: 16

  • * (Excluding Mailing and Handling)

Abstract

Background: Escitalopram, a selective serotonin reuptake inhibitor (SSRI), acts by increasing the serotonin level in the brain and is used widely for the management of depression and anxiety disorders. However, the poor dissolution rate of escitalopram due to less water solubility is a consequential problem confronting the pharmaceutical industry in developing pharmaceutical dosage forms for oral delivery systems.

Objective: The present work aims to deliver a novel formulation for improving the dissolution profile and, thus, the bioavailability of escitalopram.

Methods: Fast Dissolving Tablets (FDT) are expected to enable quick drug release, which will improve the drug's dissolving profile, allowing for the initial increase in plasma concentration mandatory in an acute depression attack. The use of co-processed excipients in tablets has been shown to increase the compressibility and disintegration properties of the tablets, resulting in improved in-vitro drug release and bioavailability. As co-processed excipients, a mixture of banana powder (a natural super disintegrant with nutritional value) and microcrystalline cellulose (a highly compressible substance with good wicking and absorption capacity) was used.

Results: The tablets were made using a response surface, randomised central composite design, and a direct compression technique. The manufactured tablets were found to be released more than 95% of the drug within 10 minutes and showed an improved drug release profile than the available marketed formulation.

Conclusion: After confirming in-vivo potential, the fast release formulation exhibited impressive in-vitro findings and may prove to be a boon in treating acute depression attacks.

Keywords: Co-processed excipients, bioavailability, fast-dissolving tablets, escitalopram banana powder, microcrystalline cellulose, depression.

Graphical Abstract

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