Abstract
The present investigation was undertaken with an objective of formulating modified release (MR) matrix tablets of Oxcarbazepine (OXC) an anti-epileptic drug, based on cellulose ether polymers like Hydroxy Propyl Methyl Cellulose (HPMC K4M and LVCR 100) and Hydroxy Propyl Cellulose (HPC JF) as drug release retardants to overcome poor patient compliance and exposure to high doses associated with currently marketed immediate release (IR) dosage forms. The tablets were prepared by direct compression process and evaluated for various physico- chemical/mechanical parameters. Among three polymers used, HPMC LVCR 100 is selected as release retardant based on the viscosity and gel formation during dissolution. The effect of different fillers like Avicel PH 101, Avicel PH 105, Pre gelatinized starch (PGS), maize starch with spray dried lactose (FLOWLAC) and Di-calcium phosphate (DCP) on OXC release was also studied and the OXC percent release at the end of 12h is in the order of DCP>FLOWLAC>Avicel PH 101>Avicel PH 105>PGS. Based on the dissolution data obtained with different fillers and keeping in view of the results from the pre compression studies, and gel layer retaining with the matrix tablets, Avicel PH 105 was selected as carrier to carry out further formulation development. Since, OXC is poorly water soluble drug, solubilizing agents like surfactants, cyclodextrins and polyethylene glycols were included in the formulations and their effect on OXC release was studied in order to achieve therapeutic effective levels. Formulations containing 20% (w/w) of Hydroxy Propyl-β-Cyclodextrin gave superior OXC release of 85.50 ± 1.62% at the end of 12hours and fulfils the regulatory requirement. The dissolution data was also evaluated for drug release kinetics and mechanisms.
Highlights
Over the past few decades several new chemical entities (NCEs) have been discovered, out of which 40% are lipophilic and poorly soluble drugs (Mudit D 2011)
The present investigation was aimed to develop twice a day oral modified release (MR) tablet dosage forms for OXC based on cellulose ether polymers like HPMC, HPC as drug release retardants
Excipients like surfactants, cyclodextrins and polyethylene glycols were included in the formulations and their effect on the OXC release was studied in order to achieve therapeutically effective levels of OXC from MR tablets
Summary
Over the past few decades several new chemical entities (NCEs) have been discovered, out of which 40% are lipophilic and poorly soluble drugs (Mudit D 2011). The ability of improving the solubility and delivery of poorly soluble drugs is very important step in formulation development. It can be enhanced through either altering the macromolecular characteristics of the drug particles, or chemical or mechanical modification of the environment surrounding the drug molecule. The present investigation was aimed to develop twice a day oral MR tablet dosage forms for OXC based on cellulose ether polymers like HPMC, HPC as drug release retardants. OXC is poorly water-soluble drug, its release from the modified release tablets is incomplete and therapeutically effective drug levels may not be achieved. Excipients like surfactants, cyclodextrins and polyethylene glycols were included in the formulations and their effect on the OXC release was studied in order to achieve therapeutically effective levels of OXC from MR tablets
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
