Formulation and characterization of oral rapid disintegrating tablets of levocetirizine.

Samvedna, S; Jindal, S; Mishra, G; Madan, JR; Gupta, G; Awasthi, R; Pinto, TDJA; Dua, K; Kulkarni, GT

Formulation and characterization of oral rapid disintegrating tablets of levocetirizine.

Samvedna, S Jindal, S Mishra, G Madan, JR Gupta, G Awasthi, R Pinto, TDJA Dua, K

Kulkarni, GT

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Publication Type:: Journal Article
Citation:: Polim Med, 2018, 48 (1), pp. 31 - 40
Issue Date:: 2018-01

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Field	Value	Language
dc.contributor.author	Samvedna, S	en_US
dc.contributor.author	Jindal, S	en_US
dc.contributor.author	Mishra, G	en_US
dc.contributor.author	Madan, JR	en_US
dc.contributor.author	Gupta, G	en_US
dc.contributor.author	Awasthi, R	en_US
dc.contributor.author	Pinto, TDJA	en_US
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159	en_US
dc.contributor.author	Kulkarni, GT	en_US
dc.date.issued	2018-01	en_US
dc.identifier.citation	Polim Med, 2018, 48 (1), pp. 31 - 40	en_US
dc.identifier.issn	0370-0747	en_US
dc.identifier.uri	http://hdl.handle.net/10453/130661
dc.description.abstract	BACKGROUND: Levocetirizine, active R (-) enantiomer of cetirizine, is an orally active and selective H1 receptor antagonist used medically as an anti-allergic. Allergic rhinitis is a symptomatic disorder of the nose induced by inflammation mediated by immunoglobulin E (IgE) in the membrane lining the nose after allergen exposure. OBJECTIVES: The purpose of the present study was to prepare rapidly disintegrating tablets of levocetirizine after its complexation with β-cyclodextrin (β-CD). MATERIAL AND METHODS: Levocetirizine-β-CD complex tablets were prepared by direct compression technique using 3 synthetic superdisintegrants in different proportions. Development of the formulation in the present study was mainly based on the concentration of superdisintegrants and the properties of the drug. Nine batches of tablets were formulated and evaluated for various parameters: drug content, weight variation, water absorption ratio, wetting time, in vitro disintegration, hardness, friability, thickness uniformity, and in vitro dissolution. RESULTS: A Fourier-transform infrared spectroscopy (FTIR) study showed that there were no significant interactions between the drug and the excipients. The prepared tablets were good in appearance and showed acceptable results for hardness and friability. The in vitro disintegrating time of the formulated tablet batches was found to be 15-35 s percentage and the drug content of tablets in all formulations was found to be between 90-102%, which complied with the limits established in the United States Pharmacopeia. CONCLUSIONS: Complexation of levocetirizine with β-CD significantly improves the solubility of the drug. The disintegration time of the tablets was decreased with an increase in superdisintegrant amount. The tablets (batch CPX5) had a minimum disintegration time of 20 s and 99.99% of the drug was released within 10 min.	en_US
dc.language	eng	en_US
dc.relation.ispartof	Polim Med	en_US
dc.relation.isbasedon	10.17219/pim/99951	en_US
dc.subject.mesh	Cetirizine	en_US
dc.subject.mesh	Tablets	en_US
dc.subject.mesh	Administration, Oral	en_US
dc.subject.mesh	Chemistry, Pharmaceutical	en_US
dc.subject.mesh	Solubility	en_US
dc.subject.mesh	Hardness	en_US
dc.title	Formulation and characterization of oral rapid disintegrating tablets of levocetirizine.	en_US
dc.type	Journal Article
utslib.citation.volume	1	en_US
utslib.citation.volume	48	en_US
utslib.location.activity	Poland	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	open_access
pubs.issue	1	en_US
pubs.publication-status	Published	en_US
pubs.volume	48	en_US

Abstract:

BACKGROUND: Levocetirizine, active R (-) enantiomer of cetirizine, is an orally active and selective H1 receptor antagonist used medically as an anti-allergic. Allergic rhinitis is a symptomatic disorder of the nose induced by inflammation mediated by immunoglobulin E (IgE) in the membrane lining the nose after allergen exposure. OBJECTIVES: The purpose of the present study was to prepare rapidly disintegrating tablets of levocetirizine after its complexation with β-cyclodextrin (β-CD). MATERIAL AND METHODS: Levocetirizine-β-CD complex tablets were prepared by direct compression technique using 3 synthetic superdisintegrants in different proportions. Development of the formulation in the present study was mainly based on the concentration of superdisintegrants and the properties of the drug. Nine batches of tablets were formulated and evaluated for various parameters: drug content, weight variation, water absorption ratio, wetting time, in vitro disintegration, hardness, friability, thickness uniformity, and in vitro dissolution. RESULTS: A Fourier-transform infrared spectroscopy (FTIR) study showed that there were no significant interactions between the drug and the excipients. The prepared tablets were good in appearance and showed acceptable results for hardness and friability. The in vitro disintegrating time of the formulated tablet batches was found to be 15-35 s percentage and the drug content of tablets in all formulations was found to be between 90-102%, which complied with the limits established in the United States Pharmacopeia. CONCLUSIONS: Complexation of levocetirizine with β-CD significantly improves the solubility of the drug. The disintegration time of the tablets was decreased with an increase in superdisintegrant amount. The tablets (batch CPX5) had a minimum disintegration time of 20 s and 99.99% of the drug was released within 10 min.

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http://hdl.handle.net/10453/130661