Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Febuxostat is used in the treatment of hyperuricemia and gout. Several impurities were detected in Febuxostat drug substance. Impurities were identified with the help of LC-MS/MS and were characterized after synthesis by IR and NMR. Reverse phase gradient system was used with Kromasil C18, 150mm×4.6mm, 5μm particle size column for the separation of impurities. Q-TOF mass spectrometer with electrospray ionization (ESI) source was used and operated in ESI positive mode, which gives exact mass up to four decimal places and fragmentation with mass accuracy, it is useful for the identification of impurities. Four impurities were identified as amide, sec-butyl, des-cyano and des-acid in Febuxostat drug analog. These impurities were further confirmed by NMR and FT-IR spectral data.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.jpba.2011.07.039 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Commercial and non-commercial cyclodextrin derivatives as a novel therapy to improve gout's disease and hyperuricemia.
Int J Pharm
September 2025
Dipartimento Di Chimica e NIS, Università di Torino, via P. Giuria 7, 10125 Torino, Italy.
Gout, which affects 3-6 % of Western populations, has well-established therapies but still lacks agents that directly target monosodium urate (MSU) deposits. This study investigates a novel strategy employing cyclodextrins (CDs) and hyperbranched cyclodextrin-based polymers (HBCD-Pol) to both mobilize and prevent MSU formation. Among the CDs tested, HPβ-CD exhibited the strongest uric acid (UA) complexation at 25 °C, while HBCD-Pol showed superior performance by chelating Na ions.
View Article and Find Full Text PDFFebuxostat-induced hepatocellular injury.
BMJ Case Rep
August 2025
Hoag Digestive Health Institute, Hoag Memorial Hospital Presbyterian, Newport Beach, California, USA.
Febuxostat is a non-purine xanthine oxidase inhibitor primarily used to treat gout and hyperuricaemia. Although it has a better safety profile compared to allopurinol, febuxostat has been associated with rare cases of drug-induced liver injury. We present a case of a man in his late 50s who developed liver injury after switching from allopurinol to febuxostat for gout management.
View Article and Find Full Text PDFDevelopment of Bioresponsive Poloxamer-Based Self-Nanoemulsifying System for Enhanced Febuxostat Bioavailability: Solidification Strategy Using I-Optimal Approach.
Pharmaceutics
July 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
The major limitations of self-nanoemulsifying systems include complex processing and expensive instrumentation required for solidification approaches. In this study, smart poloxamer-based solidification strategies were used to develop and optimize febuxostat-loaded formulations. A self-nanoemulsifying drug delivery system (SNEDDS) component was selected based on solubility and emulsification tests.
View Article and Find Full Text PDFContribution of Organic Anion Transporter 3 in Delayed Elimination of Methotrexate by Concomitant Administration of Febuxostat.
Biopharm Drug Dispos
August 2025
Department of Pharmacy, The University of Osaka Hospital, Osaka, Japan.
Methotrexate is an antifolate agent used for the treatment of various malignancies and is mainly secreted via human organic anion transporter 3 (hOAT3) in the proximal tubular cells. Coadministration of the xanthine oxidase inhibitor, febuxostat, in patients receiving methotrexate has been reported to be associated with an elevated risk of hematological toxicity and increased plasma methotrexate levels. Because febuxostat has an inhibitory effect against hOAT3, it may inhibit renal elimination of methotrexate via hOAT3.
View Article and Find Full Text PDFDiverse Development Approaches for Xanthine Oxidase Inhibitors: Synthetic Chemistry, Natural Product Chemistry, and Drug Repositioning.
Curr Med Chem
August 2025
Department of Pharmacy, Harbin University of Commerce, Harbin, Heilongjiang, China.
Xanthine oxidase (XOD) plays a crucial role in the biosynthesis of uric acid, and inhibiting its activity can effectively reduce the production of uric acid at its source. Currently, clinically used xanthine oxidase inhibitors (XODIs), such as allopurinol and febuxostat, are effective but associated with notable side effects. Allopurinol may induce hypersensitivity reactions, while febuxostat has been reported to potentially increase the risk of severe cardiovascular events.
View Article and Find Full Text PDF