Formulation Development and Evaluation of Taste Masked Anthelmintics Chewable Tablets by Using chewable tablet

Abstract

The aim of the current study is to develop and evaluate patient friendly taste masked anthelmintics chewable tablets for pediatrics and geriatrics use. However, the chewable tablets have to disintegrate in the mouth before swallowing, which makes the chewable tablet dosage forms inappropriate for bitter active ingredients [1]. For people with dysphasia (difficulty in swallowing), chewable tablets are an excellent alternative to conventional tablets. Chewable tablets reduce the risk of drug-induced esophagi is-when a tablet is caught in the esophagus and dissolves while remaining in contact with the sensitive esophagus lining. Chewable tablets can help to avoid this problem.These dosage forms are large in sizes which are hard for swallowing consequently, chewable tablets chewing in buccal depression earlier swallowing. Ideal characteristics of chewable tablets that incorporate easy to bite, Palatable (taste-conceal or of adequate taste) and suitable size and shape. The excipient incorporate extraordinary thought, they should be given to those materials that structure the reason for chewable tablet formulation [2]. FDA published guidance in 2018 on quality attribute considerations for chewable tablets. Schistosomiasis is a parasitic disease caused by flukes (trematodes) of the genus Schistosoma. More than 140 million people, 90% of who live in Africa, are infected with schistosomiasis. An estimated 700 million people are at risk of infection in 76 countries where the disease is considered endemic, as their agricultural work, domestic chores, and recreational activities expose them to infested water. Since no vaccine exists against schistosomiasis. Treatment of schistosomiasis has relied on the anthelmintic drug praziquantel (PZQ) for more than a generation. PZQ is the drug of choice for the treatment of schistosomiasis; it is effective against all major forms of schistosomiasis, although it is less active against juvenile than mature parasites [3]. In this study, a polymer (Eudragit® EPO) has been used as coating to overshadow the unpleasant taste of drug. The taste-masking study in human volunteers revealed that Coating solution of Eudragit EPO was applied on praziquentel granules by “granules coating technique” with help of Fluid Bed Processor GPCG 1.1 (Top Spray). This strategy is better as compared to coating of praziquentel granules with Eudragit EPO in Rapid Mixer Granulator. At high pH, formulation shows low disintegration and dissolution due to its low water solubility. Initially eudragit EPO coating on praziquantel was performed in RMG and coated granules were compressed to form taste masked chewable tablets of praziquantel.  But sensory evaluation studies shows that they were failed to mask the bitter taste of praziquantel. For this reason Eudragit coating in RMG was replaced by Eudragit coating in FBP so that more efficient coating can be achieved for the development of taste masked chewable tablets. Sensory evaluation data reveals that increasing percentage composition of eudragit coating in FBP was able to mask the bitter taste of praziquantel to significant levels. But bitterness of praziquantel was not completely masked. To mask the bitter taste of praziquantel completely additionally mannitol was added in the formulation as sweetening agent. Sensory evaluation data shows that mannitol addition in formulation aids in taste masking and bitter taste of praziquantel was completely masked. The optimized formulation of Praziquantel taste masked chewable tablets were then subjected to accelerated stability studies as stated by ICH which showed that the tablets were stable for eight weeks.  The drug release were>98% in 60 min. The key excipient in chewable tablets incorporate flavor enhancing agent and sweetening agent. In this present research work, the chewable tablets were prepared by wet granulation method [4]. Compression of chewable tablet was done by Rimek mini press tablet compression machine. The pre-compression parameters assessed for the granules produced. All these pre-compression parameters are include angle of repose, bulk density, tapped density, Carr’s index, Houser’s ratio (32°, 0.4674 g/cc, 0.5658 g/cc, 17.39 %, 1.21 respectively). Chewable tablets are evaluated by chemical and physical evaluation methods [5]. Physical methods and chemical methods that include Average weight (pass), Hardness (9 Kpa), Friability (0.10%), Thickness (6.92mm), Dissolution (97.8-98.3%), drug content (98.1%), Accelerated stability studies (no change after 8 week), Drug release kinetic (first order, 0.9955) and sensory evaluation (bitterness average value 0).