title: Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability.
abstract: The present investigation was aimed towards developing a beta-cyclodextrin (β-CD) solid dispersion (SD) based orally disintegrating tablet (ODT) of eslicarbazepine acetate (ESL), for improving the dissolution and providing fast onset of anti-epileptic action. Optimum ratio of ESL and β-CD was determined by Job's plot. Thereafter, solid dispersions were prepared by solvent evaporation method and evaluated for yield, assay, Differential scanning calorimetry (DSC), Fourier transform infra red spectroscopy (FTIR), X-ray diffraction (XRD), and in vitro dissolution. Optimized SD was compressed into ODT by direct compression using super disintegrants and evaluated for wetting time, drug content, in vitro drug release and in vivo studies. The results of DSC, FTIR and XRD analysis supported the formation of inclusion complex. An improved dissolution with 99.95 ± 2.80% drug release in 60 min was observed in comparison to 24.85 ± 2.96% release from a plain drug suspension. Tablets with crosspovidone as a super disintegrant showed the least disintegration time of 24.66 ± 1.52 s and higher in vitro drug release against marketed tablets. In vivo studies indicated that the formulated tablets had 2 times higher bioavailability than marketed tablets. Thus, the developed β-CD-ESL SD-ODT could provide faster onset of action and higher bioavailability, which would be beneficial in case of epileptic seizures.
authors.affiliation: TIFAC Centre of Relevance and Excellence, Centre of PG Studies and Research, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat 390002, India.
authors.forename: Samixa
authors.initials: S
authors.lastname: Desai
authors.affiliation: TIFAC Centre of Relevance and Excellence, Centre of PG Studies and Research, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat 390002, India.
authors.forename: Aditi
authors.initials: A
authors.lastname: Poddar
authors.affiliation: TIFAC Centre of Relevance and Excellence, Centre of PG Studies and Research, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat 390002, India. Electronic address: dr_krutikasawant@yahoo.co.in.
authors.forename: Krutika
authors.initials: K
authors.lastname: Sawant
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D003984:Dibenzazepines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D011208:Powders; D011817:Rabbits; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets; D013997:Time Factors; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D003984:Dibenzazepines; D011208:Powders; D013607:Tablets; D047392:beta-Cyclodextrins; C416835:eslicarbazepine acetate; C031215:betadex
keywords: Bioavailability; Eslicarbazepine acetate; Orally disintegrating tablets; Solid dispersion; β-cyclodextrin