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Volume 31, Issue 11
  • ISSN: 1381-6128
  • E-ISSN: 1873-4286

Abstract

Background

Cocrystals are an efficient way for the delivery of low soluble drugs but when dissolved they rapidly disproportionate. To formulate the cocrystals in tablets, cocrystals must be stabilized. In this study ibuprofen-nicotinamide (IBU-NIC) cocrystals were synthesized initially by slow solvent evaporation and for bulk production by fast solvent evaporation techniques.

Methods

The cocrystals were characterized by powder X-ray diffraction (PXRD), Fourier transform infrared spectrophotometer (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and optical microscopy. The ibuprofen cocrystals showed greater solubility compared to the parent drug.

Results

Intrinsic dissolution data was utilized for efficacious screening of tablet formulations. Using hydrophilic polymers at a ratio of 6:1 (polymer to IBU-NIC cocrystal ratio), hydroxypropyl methylcellulose (F), polyvinylpyrrolidone (PVP) K-30 (F) and PVP K-90 (F3), three tablet formulations were prepared that stabilized cocrystals during dissolution. The drug release profiles after 60 minutes from formulations F (92.30), F (98.54), F (99.88) were all higher compared to the marketed brand BRUFEN® F, (79.61%) in a simulated intestinal media (0.001).

Conclusion

Significant increase in the dissolution rate of cocrystal was observed with no phase change in all formulations.

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2024-06-11
2025-04-02

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Synthesis, Characterization, and Stability Optimization of Ibuprofen Cocrystals Employing Various Hydrophilic Polymers
Curr. Pharm. Des. 31, 873 (2025); https://doi.org/10.2174/0113816128305926240530051853
/content/journals/cpd/10.2174/0113816128305926240530051853
/content/journals/cpd/10.2174/0113816128305926240530051853
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  • Article Type:     Research Article
Keyword(s): BCS class-II; bioavailability; Cocrystal; formulations; ibuprofen-nicotinamide; tabletability

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