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Ketoprofen–FA Co-crystal: In Vitro and In Vivo Investigation for the Solubility Enhancement of Drug by Design of Expert.
- Source :
- AAPS PharmSciTech; May2022, Vol. 23 Issue 4, p1-15, 15p
- Publication Year :
- 2022
-
Abstract
- The present piece of research work is framed for improving the solubility of ketoprofen by forming co-crystal using fumaric acid as a coformer. Co-crystal of ketoprofen and fumaric acid was prepared by simple solvent-assisted grinding method, containing drug and coformer as independent variables and solubility and % drug release were assumed to be dependent variables. Differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, nuclear magnetic resonance and scanning electron microscopy techniques were used to characterize the preparation of optimized batch of co-crystal and further, evaluated for in vitro and in vivo anti-inflammatory and analgesic activities. Based on results of solubility and dissolution rate studies the formulation showed magnified improvement in both the properties on co-crystallization. The values of Gibbs free energy are negative at all levels of carrier demonstrating spontaneity of the drug solubilization process. The IC<subscript>50</subscript> value of optimized batch of co-crystal formulation and the pure drug was observed as 327.33 μg/ml and 556.11 μg/ml, respectively, demonstrating that co-crystal formulation possesses more percentage protection against protein denaturation than the drug ketoprofen. In vivo (anti-inflammatory and analgesic) activities revealed that optimized batch of co-crystal formulation delivered a rapid pharmacological response in Wistar rats and albino mice when compared with standard drug. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 15309932
- Volume :
- 23
- Issue :
- 4
- Database :
- Complementary Index
- Journal :
- AAPS PharmSciTech
- Publication Type :
- Academic Journal
- Accession number :
- 156619330
- Full Text :
- https://doi.org/10.1208/s12249-022-02253-5