PMID- 30657656 OWN - NLM STAT- MEDLINE DCOM- 20190502 LR - 20190502 IS - 0370-0747 (Print) IS - 0370-0747 (Linking) VI - 48 IP - 1 DP - 2018 Jan-Jun TI - Formulation and characterization of oral rapid disintegrating tablets of levocetirizine. PG - 31-40 LID - 10.17219/pim/99951 [doi] AB - 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 beta-cyclodextrin (beta-CD). MATERIAL AND METHODS: Levocetirizine-beta-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 beta-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. FAU - Samvedna, Samvedn AU - Samvedna S AD - Laureate Institute of Pharmacy, Jawalamukhi, India. FAU - Jindal, Shammy AU - Jindal S AD - Laureate Institute of Pharmacy, Jawalamukhi, India. FAU - Mishra, Gaurav AU - Mishra G AD - Drug Delivery and Nanotechnology Laboratory, Bhagyoday Teerth Pharmacy College, Sagar, India. FAU - Madan, Jyotsana R AU - Madan JR AD - Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, India. FAU - Gupta, Gaurav AU - Gupta G AD - School of Pharmaceutical Sciences, Jaipur National University, Jagatpura, India. FAU - Awasthi, Rajendra AU - Awasthi R AD - Amity Institute of Pharmacy, Amity University, Noida, India. FAU - Pinto, Terezinha De Jesus Andreoli AU - Pinto TJA AD - Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao Paulo, Brazil. FAU - Dua, Kamal AU - Dua K AD - Discipline of Pharmacy, Graduate School of Health, University of Technology, Sydney, Australia. FAU - Kulkarni, Giriraj T AU - Kulkarni GT AD - Amity Institute of Pharmacy, Amity University, Noida, India. LA - eng PT - Journal Article PL - Poland TA - Polim Med JT - Polimery w medycynie JID - 7509477 RN - 0 (Tablets) RN - 6U5EA9RT2O (levocetirizine) RN - YO7261ME24 (Cetirizine) SB - IM MH - Administration, Oral MH - *Cetirizine/chemistry MH - *Chemistry, Pharmaceutical MH - Hardness MH - Solubility MH - Tablets OTO - NOTNLM OT - direct compression OT - rapidly disintegrating tablets OT - superdisintegrants OT - beta-cyclodextrin complex EDAT- 2019/01/19 06:00 MHDA- 2019/05/03 06:00 CRDT- 2019/01/19 06:00 PHST- 2019/01/19 06:00 [entrez] PHST- 2019/01/19 06:00 [pubmed] PHST- 2019/05/03 06:00 [medline] AID - 10.17219/pim/99951 [doi] PST - ppublish SO - Polim Med. 2018 Jan-Jun;48(1):31-40. doi: 10.17219/pim/99951.