Abstract
Objective: The present study was aimed to formulate fast dissolving tablets (FDTs) of Aprepitant (APT) using natural and synthetic superdisintegrants with the desired onset of action, increased bioavailability by reducing the frequency of dosage and also reduce the first-pass metabolism of the drug.
 Methods: In this research, the gum isolated from cordia dichotoma was investigated as super disintegrants in fast dissolving tablets (FDTs). The aprepitant tablets were prepared separately using cordia dichotoma (natural), sodium starch glycolate and croscarmellose sodium (synthetic) as superdisintegrants by direct compression method. The tablets were evaluated for various precompression and post-compression parameters.
 Results: The optimized formulation (APT F3) of cordia dichotoma (8%) showed satisfactory physicochemical properties, minimum disintegration time (34 seconds) and highest dissolution rate (86.52%) in 10 min than the other synthetic superdisintegrants. Also, the pharmacokinetic study of the optimized formulation showed effective results as compared with marketed product of aprepitant.
 Conclusion: The developed formulation can improve the onset of action as well as improve patient compliance.
Highlights
Nausea is an unpleasant sensory and emotional experience accompanied by an autonomic driven physiological change of paller and upper GI track hyper secretion [1]
The dried polysaccharide powder isolated from cordia dichotoma was brown in color
The Fourier transform infrared spectroscopy (FTIR) spectra obtained for aprepitant showed strong absorption peak at 1704 cm−1 which specified C=O stretching, C-H stretching over the range
Summary
Nausea is an unpleasant sensory and emotional experience accompanied by an autonomic driven physiological change of paller and upper GI track hyper secretion [1]. 40% of patients who receive chemotherapy have experienced with nausea and vomiting [3, 4]. Conventional oral drug delivery systems, including solutions, suspension, tablets and capsules are difficult to administer to patients with dysphagia. Swallowing problems can be appear often in specific populations, including pediatric, elderly, nauseated patients and developmentally disabled patients. In addition to these difficulties convenience is a notable concern associated with oral antiemetics like the patients taking tablet formulations require water to ease swallowing, which is not always available [8, 9]. In addition to change in nontraditional drug delivery systems, oral delivery formulations have continued to develop to enhance the dissolution and absorption. Fast dissolving tablets (FDTs) have been designed to allow a solid dose to be rapidly dissolved in the oral cavity without the need for water [10,11,12]
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