Design, Formulation and Evaluation of Physicochemical Properties of Valacyclovir Effervescent Tablet

Valacyclovir (VA) displays antiviral activity against Herpes simplex virus (HSV) and Varicella zoster virus (VZV). The aim of this study was to design, formulate and evaluate the physicochemical properties of effervescent tablets containing VA in order to facilitate pill swallowing for the pediatric, elderly and bed-ridden patients. Sixteen formulations with different amounts of effervescent base were prepared by modified direct compression for the loading of ۵۰۰ mg VA. The Design-Expert® software was then used to generate formulations using a full factorial design with four different variables: citric acid (A), sodium bicarbonate to citric acid molar ratio (B) ۶۰۰۰ (D). The prepared tablets were assessed for weight variation, hardness, thickness, friability, drug content, CO۲ content, effervescence time and pH. To improve the taste of formulations, several sweeteners and fruity essences such as raspberry and cherries were used. F۲ formulation was selected as the optimized formulation with the desirability of ۷۲.۸%. The optimized formulation had an effervescent time of ۹۸.۳۳±۳.۵۱ seconds, friability % of ۰.۵۵, pH value of ۴.۶۷±۰.۰۶, CO۲ amount of ۲۶۱.۳۳ ± ۲۰.۲۶ mg and hardness of ۷۷.۲۳±۳.۱۲ N. It, therefore, seems that optimized effervescent tablets may be helpful for the delivery of VA in the treatment of herpes simplex or herpes zoster and chikenpox. Keywords: Valacyclovir, Effervescent Tablet, Dry Granulation, Direct compression method. Please cite this article as: Somayeh Taymouri, Abolfazl Mostafavi, Sajjad Zaretaghiabadi. Design, Formulation and Evaluation of Physicochemical Properties of Valacyclovir Effervescent Tablet. Trends in Pharmaceutical Sciences. ۲۰۲۲;۸(۳):۱۳۵-۱۴۶. doi: ۱۰.۳۰۴۷۶/TIPS.۲۰۲۲.۹۵۳۸۵.۱۱۴۵.

Keywords:

Valacyclovir , Effervescent Tablet , Dry Granulation , Direct compression method