Formulation and Evaluation of BILAYR Floating Tablet of Levetiracetam
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Author:
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HAMAD KADHUM MAARIZ, WEDAD K ALI, FATIMA A TWFEEQ
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Abstract:
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Levetiracetam is an antiepileptic drug indicated for partial-onset and monoclinic seizures. It has a short half-life 7hrs; for this reason, it is necessary to formulate a suitable dosage form to get a sustained drug release.
Aim: The objective of this work was to develop bilayer floating tablets of levetiracetam to provide an immediate release of one-third of the levetiracetam content to achieve an effective plasma concentration and the sustained release floating layer to release the drug over several hours. This floating layer has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility
Methods: Immediate release layer was prepared by using the superdisintegrant sodium starch glycolate while sustained release floating layer was prepared by using polymers; HPMC K4M, xanthan gum, ethylcellulose, carbopol 934, sodium alginate and sodium carboxymethyl cellulose (SCMC) in combination with other excipients such as sodium bicarbonate, PVP K30, avicel pH 102, spray-dried lactose (SDL) and mannitol. In this study, 14 formulas were prepared by different methods (direct compression and wet granulation) employing different polymer viscosity and concentrations in an attempt to achieve optimum floating and dissolution behavior.
Results: Formula (F8) that contain 15% (w/w) hydroxypropyl methylcellulose k4M (HPMCK4M), 15 % (w/w) ethylcellulose, 7% (w/w) sodium bicarbonate (NaHCO3). (F8) have acceptable flow properties and compressibility index and good physical properties with floating lag time (FLT) 132 seconds and total floating time (TFT) >24h with 68.5 % release of levetiracetam at the 8 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F8) showed no chemical interaction between the drug and the excipients that used in the formula.
Conclusion: It can be concluded that the selected formula (F8) can be a promising formula for the preparation of a bilayer floating tablet of levetiracetam.
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Keyword:
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Levetiracetam, antiepileptic drug, monoclinic seizures, bioavailability, bilayer floating tablets
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EOI:
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DOI:
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https://doi.org/10.31838/ijpr/2021.13.01.727
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