Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Abstract

Abstract Background The research was aimed with an approach to formulate biphasic extended-release system of trospium chloride resulting in controlled release of drug up to 24 h with prospects of better control on urinary frequency, efficacy, tolerability, and improved patient compliance. The push–pull osmotic pump (PPOP) bi-layered tablet of trospium chloride (60 mg) was developed with the use of immediate-release polymers in the pull layer (30 mg drug) and polyethylene oxide in the push layer (remaining 30 mg drug). The tablet was formulated by compression after non-aqueous granulation, seal coating, and semipermeable coating. The tablet prepared was laser drilled to create an orifice for drug release. Results Comparative in vitro dissolution and in vivo pharmacokinetic analysis of available marketed formulations demonstrated the complete drug release within 16–18 h; hence the developed biphasic extended-release system has its great importance as it provides zero-order release up to 24 h. Conclusions The developed biphasic extended-release drug delivery system of trospium chloride provides the drug release for 24 h with effective plasma concentration in comparison with the available marketed formulation. Extended release of drug from the developed formulation provides scope for its promising application in the treatment of overactive bladder (OAB).