M. S. Aziz, C. Gupta, L. Tyagi
2020
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Influential Citations
6
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Journal
Indian Journal of Pharmaceutical Sciences
Abstract
Metaxalone is oxazolidin-2-one derivative, biopharmaceutics classification system class II drug, available
in the market as a central muscle relaxant drug, used to alleviate discomforts associated with severe,
painful musculoskeletal conditions. The major drawbacks associated with formulation of solid oral dosage
forms of metaxalone are its poor aqueous solubility, poor flow property and low compressibility. The
aim of present study was to develop different crystalline forms of metaxalone in order to overcome these
drawbacks and consequently enhance its dissolution and bioavailability. For this purpose two different
approaches were adopted namely cocrystallization and melt sonocrystallization. Cocrystals of metaxalonesaccharin
and metaxalone-lactic acid were prepared, with saccharin and lactic acid as coformers, by
using solvent evaporation method. Melt sonocrystallization technique was applied for preparation of melt
sonocrystallized form of metaxalone. The percentage yield, melting point, particle size, flow property,
crystallinity index, solubility and dissolution profiles of developed crystals were evaluated and compared
with original metaxalone. Further the developed forms of metaxalone were characterized by differential
scanning calorimetry, fourier transform infrared spectroscopy, X-ray diffraction and scanning electron
microscopy. The sharp peak of differential scanning calorimetry thermograms and fourier transform
infrared spectroscopy spectras indicate towards the formation of crystalline forms with retention
of characterstic functionality of original metaxalone. The particle size and crystallinity index of the
developed metaxalone crystals were significantly reduced in comparison to the original form. In addition,
there was significant enhancement in the flow and compressibility of developed crystals, as indicated by
the value of angle of repose, Carr’s index and Hausner ratio. The solubility of prepared crystals was
much higher as compared to metaxalone and progressively increased in the following order: metaxalonesaccharin<
metaxalone-lactic acid