Ağızda Dağılan Tablet Formülasyonlarının In Vitro Karakterizasyonları ve Permeabiliteleri Üzerine Farklı Yardımcı Maddelerin ve Basım Tekniklerinin Etkisi

Abstract

Orally disintegrating tablets are easier and safer to administered in pediatric and geriatrics, patients with difficulty in swallowing and neurological diseases compared with conventional tablets. Orally disintegrating tablets easily disintegrate in the mouth after contact with saliva without need of drinking water or specific administration condition. Nausea and vomiting are common diseases in the clinic which limits daily life. Trimethobenzamide hydrochloride is an antiemetic drug which commonly used for acute treatment of nausea and vomiting. In the scope of this study, eighteen orally disintegrating tablet formulations of trimethobenzamide hydrochloride are developed by direct compression and freeze drying methods. All formulations except F4, F8, F15 and F16 disintegrated in distilled water and stimulated saliva (pH 6.8) within three minutes. Similarity between developed formulations and reference tablet was evaluated by calculating similarity factor, and dissolution profiles were not found similar; however dissolution of F3, F4, F11, F12, F15, F17 and F18 formulations were found higher than conventional tablet dissolution at 45 minutes. Permeability studies performed by using Caco-2 cell line proved that excipients used in the formulations increase permeability of trimethobenzamide hydrochloride. However, differences in permeability values of the formulations were not found statistically significant (p>0.05). As a result of this study, orally disintegrating formulations which are believed to contribute to the development of orally disintegrating tablet formulations of trimethobenzamide hydrochloride which has not any orally disintegrating tablet preparation on the worldwide market and literatures are proposed.