Formulation and Evaluating Aprepitant Orally Disintegrating Tablets via Solid Dispersion Technique

Abstract

This study demonstrates the potential of using orally disintegrating tablets (ODTs) as a delivery vehicle for Aprepitant to manage chemotherapy-induced vomiting effectively. Preformulation studies, including identification tests, solubility profiles, and drug-excipient interaction analyses, confirmed that Aprepitant has a melting point of 254-256°C and is hydrophobic, soluble in methanol, sparingly soluble in PBS pH 6.8, and insoluble in water. Solid dispersions with PEG 6000, PEG 4000, and β-cyclodextrin enhanced the solubility and dissolution rate of Aprepitant. The optimal solid dispersion (SD4, Drug: PEG6000, 1:2 ratio) exhibited excellent drug content (99.31%), solubility (3.91 mg/ml), and cumulative drug release (97.17% in 15 minutes). ODTs were prepared using different superdisintegrants and evaluated for hardness, friability, weight variation, disintegration time, wetting time, and in vitro drug release. Results indicated uniform tablet characteristics, with formulation F3 (containing crospovidone) showing the best disintegration time (21 seconds) and rapid dissolution within 15 minutes. Stability tests on F3 revealed no significant changes under varying temperature and humidity conditions. The dissolution efficiency of disintegrants followed the order: crospovidone > sodium starch glycolate > croscarmellose sodium, indicating that the formulation is ideal for fast release and absorption of Aprepitant while reducing swallowing difficulties associated with conventional tablets.