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±1ËšC/75±5% RH.

Tolterodine is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Tolterodine tartrate having side effects mainly  dry mouth and other side effects like constipation ,headache ,stomach pain hence controlled release formulation  is prefer for tolterodine tartrate and this controlled release formulation is also reduced the frequency of dosing. In market control release capsules dosage form is available, we have planned, new controlled release tablet dosage form which is prepared by using multi unit particulate drug delivery system. Tolterodine Tartrate controlled release MUPS tablets were formulated by using insoluble inert starting seed or core which was prepared by using extrusion spheronization technique. use of water soluble material combined with tolterodine create greater amount of osmotic pressure causing the controlled release pellets burst and dump the drug. Hence water insoluble core pellets were used in this formulation the controlled release formulation comprised of a) water insoluble insert core b) Drug loading layer comprising of tolterodine c) Controlled release coating surrounding drug layer d) pellets mixed with conventional tablet excipients compressed into tablets. The aim of this study focused on the introduction of new alternative core for formulation of control release MUPS tablets and also studied the effect of protective plasticizer coating layer on extended release pellets prior to compression into MUPS tablets.

For the estimation of tolterodine tartrate a new simple and accurate visible spectrophotometric method was developed. The proposed method was based on the formation of yellow-orange colored complex results from complete mixing of tolterodine tartrate, methyl orange and chloroform, which shows the maximum absorption at the wave length 417 nm. The linear relationship between the absorbance and the concentration of tolterodine tartrate was in the range of 20 – 120 µg/ml with a correlation coefficient = 0.997. This new method has offered a determination of tolterodine tartrate drug without any interference with excipients indirectly with a high accuracy for the analytical results. The method was found to be simple, economic, accurate and reproducible and can be used for routine analysis of tolterodine tartrate in bulk and in pharmaceutical formulation.