Generic placeholder image

Central Nervous System Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5249
ISSN (Online): 1875-6166

Research Article

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

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

Volume 22, Issue 3, 2022

Published on: 21 September, 2022

Page: [198 - 213] Pages: 16

DOI: 10.2174/1871524922666220624113719

Price: $65

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
[1]
Kumari, M.S.; Prasanthi, C.H.; Bhargavi, C.H.S.; Kumari, M.P.; Ushasri, S. Reassessment of novel co-processed multifunctional excipient. Int. Res. J. Pharm. Appl. Sci., 2013, 3, 122-128.
[2]
The IPEC excipient information package (EIP) template and user guide 2009. Available from: www.ipec-europe.org/UPLOADS/Excipients_Insight_nov09_final(1) (Accessed August 23, 2021).
[3]
Shangraw, R.F. Emerging trends in the use of pharmaceutical excipients. Pharm. Technol., 1997, 21, 36-42.
[4]
Rosenzweig-Lipson, S.; Beyer, C.E.; Hughes, Z.A.; Khawaja, X.; Rajarao, S.J.; Malberg, J.E.; Rahman, Z.; Ring, R.H.; Schechter, L.E. Dif-ferentiating antidepressants of the future: Efficacy and safety. Pharmacol. Ther., 2007, 113(1), 134-153.
[http://dx.doi.org/10.1016/j.pharmthera.2006.07.002] [PMID: 17010443]
[5]
Dhingra, A.K.; Chopra, B.; Dass, R.; Mittal, S.K. A review of medicinal plants possessing antidepressant potential. Indian Drugs, 2016, 53(6), 5-17.
[http://dx.doi.org/10.53879/id.53.06.10436]
[6]
Schulz, V. Safety of St. John’s Wort extract compared to synthetic antidepressants. Phytomedicine, 2006, 13(3), 199-204.
[http://dx.doi.org/10.1016/j.phymed.2005.07.005] [PMID: 16428030]
[7]
Dhingra, D.; Sharma, A. A review on antidepressant plants. Nat. Prod. Rad., 2006, 5(2), 144-152.
[8]
Lide, D.R. CRC Handbook of Chemistry and Physics, 85th ed; CRC Press, 2005.
[9]
Sowjanya, G.; Devi, T.; Sri, V.V.; Pratyusha, V.; Venkata, L.N.; Seshagiri, R.J. Development and validation of UV spectroscopic methods for simultaneous estimation of ciprofloxacin and tinidazole in tablet formulation. Int. Curr. Pharm. J., 2012, 1(10), 317-321.
[http://dx.doi.org/10.3329/icpj.v1i10.11849]
[10]
Eraga, S.O.; Arhewoh, M.I.; Uhumwangho, M.U.; Iwuagwu, M.A. Characterisation of a novel, multifunctional, co-processed excipient and its effect on release profile of paracetamol from tablets prepared by direct compression. Asian Pac. J. Trop. Biomed., 2015, 5(9), 768-772.
[http://dx.doi.org/10.1016/j.apjtb.2015.07.008]
[11]
Chougule, A.S.; Dikpati, A.; Trimbake, T. Formulation development techniques of co-processed excipients. J. Adv. Pharm. Sci., 2012, 2, 231-249.
[12]
Elkhodairy, K.A.; Hassan, M.A.; Afifi, S.A. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm. J., 2014, 22(1), 53-61.
[http://dx.doi.org/10.1016/j.jsps.2013.01.009] [PMID: 24493974]
[13]
Rane, D.R.; Gulve, H.N.; Patil, V.V.; Thakare, V.M.; Patil, V.R. Formulation and evaluation of fast dissolving tablet of albendazole. Int. Curr. Pharm. J., 2012, 1(10), 311-316.
[http://dx.doi.org/10.3329/icpj.v1i10.11848]
[14]
Madan, J.R.; Dagade, R.H.; Awasthi, R.; Dua, K. Formulation and solid state characterization of carboxylic acid-based co-crystals of tinidazole: An approach to enhance solubility. Polim. Med., 2018, 48(2), 99-104.
[http://dx.doi.org/10.17219/pim/105609] [PMID: 31033260]
[15]
Banker, G.S.; Anderson, N.R. The Theory and Practice of Industrial Pharmacy; Lachman, L.; Lieberman, H.A; Kanig, J.L., Ed.; Varghese Publishing House: Mumbai, 1990, pp. 296-302.
[16]
The Unit States Pharmacopoeial Convention. United States of Pharmacopeia-National Formulary; USP 30- NF 25 2007; Rockville, MD, USA;, 2007.
[17]
Patel, S.; Patel, M. Development of directly compressible co-processed excipient for dispersible tablets using 32 full factorial design. Int. J. Pharm. Pharm. Sci., 2009, 1, 125-148.
[18]
Banker, G.S.; Anderson, N.R. The Theory and Practice of Industrial Pharmacy; Lachman, L.; Lieberman, H.A; Kanig, J.L., Ed.; Varghese publishing house: Mumbai, 1987, pp. 293-299.
[19]
Thahera, P.D.; Latha, A.K.; Shailaja, T.; Nyamathulla, S.; Uhumwangho, M.U. Formulation and evaluation of Norfloxacin gastro retentive drug delivery systems using natural polymers. Int. Curr. Pharm. J., 2012, 1(7), 155-164.
[http://dx.doi.org/10.3329/icpj.v1i7.10809]
[20]
Khan, K.A. The concept of dissolution efficiency. J. Pharm. Pharmacol., 1975, 27(1), 48-49.
[http://dx.doi.org/10.1111/j.2042-7158.1975.tb09378.x] [PMID: 235616]
[21]
Chaudhari, P.D.; Chaudhari, S.; Kolhe, S.R.; Dave, K.V.; More, D.M. Formulation and evaluation of fast dissolving tablets of famotidine. Indian Drugs, 2005, 42, 641-649.
[22]
Kaur, M.; Mittal, A.; Gulati, M.; Sharma, D.; Kumar, R. Formulation and in vitro evaluation of fast dissolving tablets of febuxostat using co-processed excipients. Recent Pat. Drug Deliv. Formul., 2020, 14(1), 48-62.
[http://dx.doi.org/10.2174/1872211314666191224121044] [PMID: 31884935]
[23]
National Library of Medicine. National Center for Biotechnology Information., Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Escitalopram (Accessed on August 25, 2021).
[24]
Kakde, R.B.; Satone, D.D. Spectrophotometric method for simultaneous estimation of escitalopram oxalate and clonazepam in tablet dos-age form. Indian J. Pharm. Sci., 2009, 71(6), 702-705.
[http://dx.doi.org/10.4103/0250-474X.59559] [PMID: 20376230]

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy