Formulation and evaluation of fast dissolving sublingual films of rizatriptan benzoate

Abstract

Rizatriptan benzoate is anti-migraine drug which has oral bioavailability of 47% due to hepatic first pass metabolism. The present study investigated the possibility of developing fast dissolving sublingual films to provide rapid drug onset. Nine formulae were prepared with different concentrations 1%, 2%, and 3% of carboxymethyl cellulose, hydroxypropyl methylcellulose E6 and E15 as water soluble polymers, by solvent casting technique. The prepared films were subjected to characterization for thickness, weight variations, folding endurance, surface pH, disintegration time, drug content and in-vitro drug release. Compatibility between drug and polymers were studied.  Film with 1% CMC was disintegrated in time of 30 seconds with rapid drug release 100% in 120 seconds. Stability study was carried out within 90 days for formulae chosen F1, F2, F4 and F7. They were stored at 40 ^oC/45% RH and 50 ^oC/45% RH. Highest percent drug remained was detected in formula F1 which was evaluated for in vivo release studies using human volunteers. The peak serum concentration (C_max), half time (T_½), time for maximum plasma concentration (T_max) and area under curve (AUC) were calculated. T_max for the sublingual film was faster than conventional oral route.