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

Imanto, T. and Wikantyasning, E.R. and Nurwaini, S. and Amalia, M. and Sambudi, N.S. and Harun, N.Y. (2024) PREPARATION AND SOLID-STATE CHARACTERIZATION OF KETOPROFEN-SUCCINIC ACID-SACCHARIN CO-CRYSTAL WITH IMPROVED SOLUBILITY. International Journal of Applied Pharmaceutics, 16 (1). pp. 275-279.

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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. © 2024 The Authors.

Item Type: Article
Additional Information: cited By 1
Uncontrolled Keywords: ketoprofen; nonsteroid antiinflammatory agent; saccharin; saccharin co crystal; succinic acid; unclassified drug, area under the curve; Article; biopharmaceutical classification system class ii; chemical interaction; classification; controlled study; crystallization; diagnostic test accuracy study; differential scanning calorimetry; drug bioavailability; drug efficacy; drug formulation; drug solubility; drug stability; drug synthesis; Fourier transform infrared spectroscopy; melting point; nonhuman; scanning electron microscopy; solid state; thermal analysis; ultraviolet spectrophotometry
Depositing User: Mr Ahmad Suhairi UTP
Date Deposited: 04 Jun 2024 14:19
Last Modified: 04 Jun 2024 14:19
URI: https://khub.utp.edu.my/scholars/id/eprint/20176

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