Formulation And Evaluation Of Mouth Dissolving Tablet Of Loratadine

Abstract

Loratadine (Lor) is classic H1-receptor antihistamines for the relief of allergic diseases such as allergic rhinitis and urticaria. They are competitive inverse agonists of the H1 receptor that have relatively high specificity and can stabilize the receptor in inactive state. They are classified as second generation H1-receptor antihistamines due to non-sedating advantages over the first-generation products. Compared to the first-generation drugs, which rapidly get into central nervous system, Lor have higher peripheral selectivity and do not cross the blood-brain barrier. Thus, they seldom cause side effect like drowsiness or somnolence and can be taken by patients of special occupation including pilots or drivers.  To provide the patient with the most convenient mode of administration, there is need to develop a fast-disintegrating dosage form, particularly one that disintegrates and dissolves/disperses in saliva and can be administered without water, anywhere, any time. Such tablets are also called as “melt in mouth tablet.” Direct compression, freeze drying, sublimation, spray drying, tablet molding, disintegrant addition, and use of sugar-based excipients are technologies available for mouth-dissolving tablet.  The objective of the present study is to design a tablet of Loratadine for delivery through oral cavity. Fast dissolving tablet are prepared when immediate onset of action is desired. The oral transmucosal drug delivery bypasses liver and avoids presystemic elimination in the gastrointestinal tract and liver. Mouth-dissolving tablets of Loratadine were prepared by direct compression, in which different formulations were prepared with varying concentration of excipients. These tablets were evaluated for their friability, hardness, wetting time, and disintegration time; the drug release profile was studied. Direct compression batch LF3 gave far better dissolution which released 99.10±2.92% in 10 minutes.