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Development of Pelubiprofen Tromethamine with Improved Gastrointestinal Safety and Absorption

Pelubiprofen (PEL), which is a commercialized non-steroidal anti-inflammatory drug (NSAID), is associated with the risk of gastrointestinal (GI) adverse events following long-term exposure and has poor water-soluble properties. Here, a new pelubiprofen tromethamine (PEL-T) with improved solubility,...

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Main Authors: Ji Yeon Park (Author), Dong Ho Oh (Author), Sang-Wook Park (Author), Bo Ram Chae (Author), Chul Woo Kim (Author), Sang Heon Han (Author), Hyeon Jong Shin (Author), Soo Bin Yeom (Author), Da Yeong Lee (Author), Min Kyu Park (Author), Sang-Eun Park (Author), Jun-Bom Park (Author), Kyung-Tae Lee (Author)
Format: Book
Published: MDPI AG, 2021-05-01T00:00:00Z.
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Summary:Pelubiprofen (PEL), which is a commercialized non-steroidal anti-inflammatory drug (NSAID), is associated with the risk of gastrointestinal (GI) adverse events following long-term exposure and has poor water-soluble properties. Here, a new pelubiprofen tromethamine (PEL-T) with improved solubility, permeability, GI safety, and absorption, compared to PEL, has been developed. The nuclear magnetic resonance spectroscopy (NMR), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR) results confirmed that the PEL-T was well formed. The powder of PEL-T showed the presence of additional 6H protons at δ 3.66-3.61 in the <sup>1</sup>H NMR spectrum, and shifted the sharp endothermic peaks at 129 °C in DSC, and the spectrum of distinct absorption peaks in FT-IR. In addition, compared with PEL, PEL-T showed a significantly improved solubility in various media and an increased permeability coefficient (K<sub>p</sub>) in Caco-2 cells. Furthermore, compared to PEL oral administration, PEL-T was found to significantly reduce the damaged area in an acute gastric damage rat model. The pharmacokinetic study of the PEL-T powder showed higher maximum plasma concentration (C<sub>max</sub>) and area under the plasma concentration-time curve from 0 h to the last time point (AUC<sub>t</sub>) than those of the PEL powder. Taken together, our data suggest that PEL-T is a recommendable candidate with enhanced gastrointestinal safety and better absorption compared with commercial PEL.
Item Description:10.3390/pharmaceutics13050745
1999-4923

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