Development and characterization of acemetacin nanosuspension-based oral lyophilisates

Acemetacin is a non-steroidal anti-inflammatory drug (NSAIDs) which has an analgesic, antipyretic, and anti-inflammatory effect. The aim of the present study was to develop oral lyophilisates containing acemetacin nanosuspensions. The primary goal was to improve tablet disintegration in the mouth, make swallowing easier, and potentially improve patient compliance. Furthermore, formulating acemetacin as a nanosuspension was intended to improve dose-to-dose proportionality compared to using the drug in its naked form. The solvent-anti-solvent technique was used to develop the nanosuspension, and Soluplus® was added to stabilize acemetacin nanoparticles. The nanosuspension was concentrated using a rotary evaporator before other excipients were added. The excipients utilized were gelatin, polyvinyl pyrrolidone K90, glycine, and mannitol. They were dissolved in the concentrated nanosuspension, poured into tablet blister molds, and lyophilized to create acemetacin nanosuspension-based oral lyophilisates. The experiments were developed via a computer-based approach using Design Expert® software. For this purpose, the Box-Behnken design was used to study the effect of different formulation factors on tablet disintegration time and friability values. The selected formula F9 had the highest desirability value (0.913), and its disintegration time and friability values were 26.6 seconds and 0.938%, respectively. The dose-to-dose proportionality has substantially improved, and more than 85% of the formula F9 was released in only 8 minutes compared to the naked acemetacinbased oral lyophilisates, which only gave 24.5% in this time frame. Compatibility studies showed there was no chemical interaction between the tablet components.