Co-milling of oxcarbazepine with Soluplus for the enhancement of solubility and dissolution rate

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Abstract

Background and objective
Poor solubility and dissolution rates affect the bioavailability of drugs. The aim of this study was to improve the solubility and dissolution rate of a poorly soluble drug, oxcarbazepine by its mechanochemical activation via the co-milling technique.
Materials and methods
The drug and Soluplus (in two different ratios) were co-milled in a planetary ball bill. The bulk properties, solubility, and dissolution rate were determined and differential scanning calorimetry, powder X-ray diffraction, Fourier-transform infrared spectroscopy (FTIR), and laser diffraction (for particle size determination) techniques were used to characterize drug and co-milled formulations.
Results and discussion
The results have shown good compressibility and excellent flow of co-milled mixtures as compared with the drug. The solubility of the drug (0.448±2 mg/ml) was increased by 2–3-fold in co-milled mixtures while the dissolution rate of oxcarbazepine was increased up to 2.5–3 times. Both differential scanning calorimetry and powder X-ray diffraction results have shown a reduction of crystallinity while the Fourier-transform infrared spectroscopy spectra indicated no interaction. Laser diffraction studies have shown ∼5 times reduction in mean particle size.
Conclusion
The study concludes that co-milling is effective in enhancing solubility and dissolution of poor soluble drugs.

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