“DEVELOPMENT AND OPTIMIZATION OF DANAZOL CO-CRYSTAL LOADED TABLET TO TREAT ENDOMETRIOSIS”

Vidya Patil

doi:10.56782/pps.525

Published : 2025-10-01

No. 2025 (Early Access)

“DEVELOPMENT AND OPTIMIZATION OF DANAZOL CO-CRYSTAL LOADED TABLET TO TREAT ENDOMETRIOSIS”

Vidya Patil

DOI: https://doi.org/10.56782/pps.525

Abstract

This study aimed to develop, optimize, and characterize Danazol co-crystal-loaded tablets to enhance solubility and dissolution, thereby improving therapeutic efficacy in the treatment of endometriosis. Danazol co-crystals were prepared using various pharmaceutically acceptable co-formers via the solvent evaporation method and characterized using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Among the systems studied, Danazol-malonic acid co-crystals (1:2 molar ratio) demonstrated the greatest solubility enhancement (11.42 ± 0.53 μg/mL), corresponding to a 13.76-fold increase compared to pure Danazol. The formation of a novel crystalline phase was confirmed by distinct XRD peaks at 2θ values of 19° and 21°. Co-crystals were incorporated into tablets using direct compression and optimized using a 3² factorial design, with sodium croscarmellose (8–24 mg) and polyvinylpyrrolidone K-30 (4–20 mg) as independent variables. The formulations were assessed for pre-compression characteristics, tablet quality parameters, disintegration time, in vitro drug release, and stability. Statistical analysis revealed strong predictive models for disintegration time (R² = 0.9971) and drug release (R² = 0.9483). The optimized formulation (VF7) containing 24 mg sodium croscarmellose and 4 mg PVP K-30 exhibited rapid disintegration (74.0 ± 3.2 s) and significantly improved dissolution (95.8 ± 2.0% at 60 min), outperforming the marketed formulation (75.2 ± 2.7%). The optimized tablets remained stable under accelerated conditions (40°C/75% RH) for three months. These findings highlight the potential of co-crystallization and formulation optimization to overcome solubility challenges, offering a promising strategy for improving the clinical performance of Danazol in endometriosis therapy.

Keywords:

Keywords: Danazol, Co – Crystallization, Solubility, enhancement, Factorial Design etc.

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Patil, V. (2025). “DEVELOPMENT AND OPTIMIZATION OF DANAZOL CO-CRYSTAL LOADED TABLET TO TREAT ENDOMETRIOSIS”. Prospects in Pharmaceutical Sciences, (2025 (Early Access). https://doi.org/10.56782/pps.525

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