Synthesis of the Pro-drug to Mask Bitter Taste and its Taste Evaluation

Meloxicam (MX), a nonsteroidal anti-inflammatory drug, widely used to treat arthritis, has a very bitter taste. Chemical modification of the bitter functionality was achieved by synthesis of a prodrug, meloxicam pivalate (MXP). Taste improvement was evaluated using single bottle-test rat model. It was found that palatability of MXP solution improved significantly as compared to MX. 
In mammals, taste buds are groups of 30-100 individual elongated "neuroepithelial" cells which are often embedded in special structure in the surrounding epithelium known as papillae. Just below the taste bud apex, taste cells are joined by tight junctional complexes that prevent gaps between cells. Food molecules cannot therefore squeeze between taste cells and get into the taste bud.
Taste papillae located on the tongue appear as little red dots, or raised bumps, particularly at the front of the tongue called "fungi form" papillae. There are three other kinds of papillae, foliate, circumvallates and the non-gustatory fili form. In mammals taste buds are located throughout the oral cavity, in the pharynx, the laryngeal epiglottis and at the entrance of the esophagus. Taste perception fades with age; on average, people lose half their taste receptors by time they turn 20.The sensation of taste can be categorized into five basic tastes: sweetness, sourness, saltiness, bitterness, and umami. Taste buds are able to differentiate among different tastes through detecting interaction with different molecules or ions. Sweet, umami, and bitter tastes are triggered by the binding of molecules to G protein-coupled receptors on the cell membranes of taste buds. Saltiness and sourness are perceived when alkali metal or hydrogen ions enter taste buds, respectively. As taste senses both harmful and beneficial things, all basic tastes are classified as either aversive or appetitive, depending upon the effect the things they sense have on our bodies [5].Sweetness helps to identify energy-rich foods, while bitterness serves as a warning sign of poisons.
 

Author(s): Bandoo C. Chatale

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