Solid Dispersion Approach Improving Dissolution Rate of Stiripentol: a Novel Antiepileptic Drug

Document Type: Research article

Author

College of Pharmacy, Department of Pharmaceutics, King Saud University, Riyadh, Saudi Arabia.

Abstract

Some drugs have low bioavailability due to their poor aqueous solubility and/or slow
dissolution rate in biological fluids. Stiripentol (STP) is a novel anticonvulsant drug that is
structurally unrelated to the currently available antiepileptics. It has poor aqueous solubility
and its solubility has to be enhanced accordingly. Polyethyleneglycol 6000 (PEG-6000) is
commonly utilized as a hydrophilic carrier for poorly water soluble drugs in order to improve
their bioavailability. STP and PEG-6000 binary system was obtained by physical mixture,
solvent evaporation, co-evaporation and melting methods using different weight ratios.
The properties of the prepared binary systems were evaluated using dissolution rate, phase
solubility, Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry
(DSC) and scanning electron microscope (SEM) studies. The FTIR spectroscopic studies
showed the stability of STP and absence of STP-PEG-6000 interaction. The DSC and SEM
studies indicated the amorphous state of STP in its binary systems with PEG-6000.
Dissolution profile of STP was significantly improved via complexation with PEG-6000 as
compared with the pure drug. The binary system which was prepared using melting method
showed the highest dissolution rate. The promising results of the prepared binary systems open
the avenue for further oral formulation of STP.

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