~ 97 ~ The Pharma Innovation Journal 2015; 4(5): 97-99 ISSN: 2277- 7695 TPI 2015; 4(5): 97-99 © 2015 TPI www.thepharmajournal.com Received: 09-06-2015 Accepted: 27-06-2015 Jyoti Dahiya Department of Pharmaceutical Sciences, Baba Mastnath University, Asthal Bohar, Rohtak. Pawan Jalwal Department of Pharmaceutical Sciences, Baba Mastnath University, Asthal Bohar, Rohtak. Shilpi Arora Department of Pharmaceutical Sciences, Baba Mastnath University, Asthal Bohar, Rohtak. Balvinder Singh Department of Pharmaceutical Sciences, Baba Mastnath University, Asthal Bohar, Rohtak. Renu Department of Pharmaceutical Sciences, Baba Mastnath University, Asthal Bohar, Rohtak. Correspondence: Jyoti Dahiya Department of Pharmaceutical Sciences, Baba Mastnath University, Asthal Bohar, Rohtak. Formulation and Evaluation of Chewable Tablets of Loratadine by Direct Compression Method Jyoti Dahiya, Pawan Jalwal, Shilpi Arora, Balvinder Singh, Renu Abstract Since last few years, there has been an enhanced demand for more patient compliance dosage forms. For this an attempt has been made in the present work to design and evaluate chewable tablets. Chewable tablets have the advantages of both conventional tablet and liquid dosage formulation, especially in geriatric and pediatric. Oral route of administration has received more attention in the pharmaceutical field. Chewable dosage forms have been demonstrated to improve therapeutic efficacy and better bioavailability. Loratadine is a peripherally selective piperidine histamine receptor blocker, which competitively antagonizes histamine at the H1 receptor site. Histamine is amine autocoids which causes many signs and symptoms of allergy. It stimulates the cells to release chemicals that produce effects associated with allergy and commonly acts on α-adrenergic receptor or 5-HT receptor. Loratadine acts as a selective antagonist of peripheral histamine H1-receptor that serves to eliminate effects mediated by histamine (an endogenous chemical mediator released during allergic reactions) or block one type of histamine receptor (H1 receptor). Loratadine is a second-generation H1 histamine antagonist drug used to treat allergies. Loratadine is used for the symptomatic relief of allergy such as hay fever (allergic rhinitis), urticaria and seasonal allergies including sneezing, itchy and runny nose, and tearing and redness of the eyes. Keywords: Loratadine, chewable tablet, histamine receptor, urticaria etc. 1. Introduction It is a peripherally selective piperidine histamine receptor blocker, which competitively antagonizes histamine at the H1 receptor site. They lack anti-cholinergic side effect and having non-sedating property because they do not cross the blood brain barrier [1] . Loratadine is a second-generation H1histamine antagonist drug used to treat allergies [2] . Structurally, it is closely related to tri-cyclic antidepressants and distantly related to the atypical antipsychotic. It is white to off white solid. It is under the therapeutic category of tricyclic antihistamine [3] . The empirical formula of loratadine is C22H23ClN2O2. The IUPAC name of the drug is Ethyl 4-(8- chloro-5, 6-dihydro-11-H benzo [5, 6] cyclohepta (1, 2-b) pyridin-11-ylidine) 1- piperidinecarboxylate. The molecular weight is 382.883 g/mol. The melting point is 132 – 137 °C. The BCS class of the drug is class II. The structural formula of the drug is given below: N Cl N O O CH3 Fig 1: Structural representation of Loratadine Hydrochloride The half life of the drug is 8 hours. It is highly bound drug to plasma proteins (90 – 99%) and does not cross the blood brain barrier. Loratadine is metabolized by rapid isoenzyme of the Cytochrome P450 system. CYP3A4 and CYP2D6 enzymes are mainly responsible for the metabolism of drug and have rapid first pass metabolism. Approximately 40% of the dose is excreted in urine and 42% in the faeces over a period of 10 day and mainly in the form of conjugated metabolites. Approx. 27% of the dose is eliminated in the urine during the first 24 hours. About less than 1% of the active substances excreted unchanged in active form as loratadine.