Formulation and Evaluation of Once-Daily Sustained Release Matrix Tablets of Tolterodine Tartrate

In the present work an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by formulating sustained release matrix tablets of tolterodine tartrate a bladder-selective anti muscarinic agent with proven efficacy and tolerability in the treatment of overactive bladder (OAB). Sustained release matrix tablets of tolterodine tartrate were prepared by direct compression method using two different polymers such as HPMC K4M and Xanthan gum as rate controlling polymer in different drug:polymer ratios such as 1:5, 1:10, 1:15, 1:20 with other tablet excipients such as microcrystalline cellulose as diluent, talc, magnesium stearate as glidant and lubricant, PVP K30 as binder, lactose as taste enhancer. The formulations were evaluated for pre-compression and post-compression parameters such as hardness, thickness, weight variation, friability, drug content uniformity, in vitro drug release profiles, short term stability studies and drug excipient interactions. Results revealed that among the 10 formulations the STH3 is considered as promising formulation, displayed almost first order release kinetics, releasing more than 75% drug release in 8.15 hours and remained sustained for more than 12 hours. Short term stability studies of promising formulation STH3 indicates that there are no significant changes in dissolution parameter values after 3 weeks storage at 45±1 ̊C/75±5% RH.