Development and Evaluation of Novel Drug Delivery System of Tolterodine Tartrate

Abstract

Objective: Tolterodine tartrate (tolterodine) is used for treating overactive bladder (OAB) with symptoms of urinary frequency, urgency and leakage. Tolterodine is an antimuscarinic (anticholinergic) agent. It works by blocking a chemical that causes contractions of the bladder. Present work involved development of a novel drug delivery system of tolterodine intended to be taken once daily.Methods: Extended release (ER) pellets of tolterodine were prepared and optimized for in vitro drug release. Subsequently, these pellets were filled into a suitable sized capsule. The resulting capsules were evaluated for in vitro drug release. Optimized formulation was subjected to accelerated stability studies for 3 mo and was evaluated for description, average weight, assay and drug release.Results: The optimized ER capsule exhibited similar dissolution profile as that of the reference listed drug (RLD), with approximately 45%, 75% and more than 80% release in 3 h, 5 h and 7 h respectively. Accelerated stability studies indicated good physical and chemical stability of the formulation.Conclusion: ER formulation of tolterodine was optimized and can be used as once a day dosage, reducing the frequency of administration when compared with the immediate release formulation. The developed formulation exhibited similar behavior as that of reference formulation Detrol LA marketed in the US.

Drug Delivery Approaches for Managing Overactive Bladder (OAB): A Systematic Review

“…These studies were further screened by title and abstract, which resulted in the removal of 430 studies. Thus, 79 studies were subjected to full-text screening and finally 24 [ 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 ] were selected and considered eligible to be included in the systematic review for further reporting and analysis ( Figure 2 ). The main reasons for exclusion were a lack of focus on drug delivery and formulation development.…”

“…Therefore, the hypromellose based matrix tablet could be a suitable alternative to sustained release capsules. Patil et al, [ 62 ] also developed extended release pellets of tolterodine tartrate using mannitol as an osmotic agent along with hypromellose. These pellets were then filled into capsules of suitable sizes and the in-vitro drug release compared with Detrol LA ® ; a generic version of the tolterodine tartrate.…”

Multivariate analysis as a method to understand variability in a complex excipient, and its contribution to formulation performance

“…Aqueous dispersions of ethylcellulose are often used to overcome environmental and economic challenges associated with organic systems. Surelease® is a fully formulated aqueous dispersion system containing ethylcellulose, plasticizers and stabilizers (Leng DE, Warner, G.L 1977;Leng DE, Mossbach, W., Sigelko, W.L, Sounders, F.L., Uirumaa, R.S, 1985) and is widely used in investigational and commercial controlled release dosage forms (Jagadeesh and Bala Ramesha Chary 2011;Paul et al 2011;Vonica et al 2011;Yin et al 2011;Melegari et al 2016;Afrasiabi Garekani et al 2017;Kazlauske et al 2017;Patil and Belsare 2017).…”