PREPARATION AND SOLID-STATE CHARACTERIZATION OF KETOPROFEN-SUCCINIC ACID-SACCHARIN CO-CRYSTAL WITH IMPROVED SOLUBILITY

TEGUH IMANTO; ERINDYAH R. WIKANTYASNING; SETYO NURWAINI; MONICA AMALIA; NONNI S. SAMBUDI; NOORFIDZA Y. HARUN

doi:10.22159/ijap.2024v16i1.48829

Authors

TEGUH IMANTO Department of Pharmaceutics, Faculty of Pharmacy, Universitas Muhammadiyah Surakarta, Surakarta-57169, Indonesia https://orcid.org/0000-0002-6171-925X
ERINDYAH R. WIKANTYASNING Department of Pharmaceutics, Faculty of Pharmacy, Universitas Muhammadiyah Surakarta, Surakarta-57169, Indonesia https://orcid.org/0000-0002-8997-7322
SETYO NURWAINI Department of Pharmaceutics, Faculty of Pharmacy, Universitas Muhammadiyah Surakarta, Surakarta-57169, Indonesia
MONICA AMALIA Faculty of Pharmacy, Universitas Muhammadiyah Surakarta, Surakarta-57169, Indonesia
NONNI S. SAMBUDI Department of Chemical Engineering, Universitas Pertamina, Jakarta-12220, Indonesia https://orcid.org/0000-0002-8658-1955
NOORFIDZA Y. HARUN Department of Chemical Engineering, Universiti Teknologi PETRONAS, Seri Iskandar-32610, Perak, Malaysia

DOI:

https://doi.org/10.22159/ijap.2024v16i1.48829

Keywords:

Crystal engineering, Ketoprofen, Co-crystal, Solubility

Abstract

Objective: This study aimed to improve the solubility of Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) that belongs to the Biopharmaceutical Classification System (BCS) Class II, through co-crystallization using succinic acid and saccharin coformers in a 1:1:1 and 2:1:1 molar ratio.

Methods: The slurry method was utilized to prepare the ketoprofen co-crystals, which were then subjected to various physical-chemical characterization techniques such as melting point determination, dissolution studies, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared (FTIR) spectroscopy.

Results: The results showed that the 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) exhibited higher solubility than the solubility standard of Ketoprofen and the 2:1:1 molar ratio of the co-crystal (Formula 2). The dissolution profile (Q₃₀) of Formula 1, Formula 2, and standard Ketoprofen were 96.73±1.77, 93.09±1.16, and 70.22±4.72, respectively. These findings suggest that co-crystallization with succinic acid and saccharin conformers using the slurry method can significantly enhance the solubility of Ketoprofen.

Conclusion: The 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) was the most effective formulation among the tested samples, demonstrating the highest solubility. This research may provide valuable insights for developing novel drug formulations with improved bioavailability and therapeutic efficacy.

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