Polymers in Medicine

Polim. Med.
Scopus CiteScore: 3.5 (CiteScore Tracker 3.6)
Index Copernicus (ICV 2023) – 121.14
MEiN – 70
ISSN 0370-0747 (print)
ISSN 2451-2699 (online) 
Periodicity – biannual

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Polymers in Medicine

2018, vol. 48, nr 1, January-June, p. 31–40

doi: 10.17219/pim/99951

Publication type: original article

Language: English

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Creative Commons BY-NC-ND 3.0 Open Access

Formulation and characterization of oral rapid disintegrating tablets of levocetirizine

Samvedn Samvedna1,A,B,C,D,F, Shammy Jindal1,A,B,F, Gaurav Mishra2,C,D,E,F, Jyotsana R. Madan3,C,D,E,F, Gaurav Gupta4,C,D,E,F, Rajendra Awasthi5,A,B,C,D,E,F, Terezinha De Jesus Andreoli Pinto6,C,D,E,F, Kamal Dua7,C,D,E,F, Giriraj T. Kulkarni5,A,C,D,E,F

1 Laureate Institute of Pharmacy, Jawalamukhi, India

2 Drug Delivery and Nanotechnology Laboratory, Bhagyoday Teerth Pharmacy College, Sagar, India

3 Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, India

4 School of Pharmaceutical Sciences, Jaipur National University, Jagatpura, India

5 Amity Institute of Pharmacy, Amity University, Noida, India

6 Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Brazil

7 Discipline of Pharmacy, Graduate School of Health, University of Technology, Sydney, Australia

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.
Conclusion. 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.

Key words

direct compression, superdisintegrants, β-cyclodextrin complex, rapidly disintegrating tablets

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