Development and evaluation of febuxostat solid dispersion through screening method

Sohn, Jeong Sun; Choi, Jin-Seok

doi:10.1016/j.jsps.2023.101724

Cited by 5 publications

(3 citation statements)

References 28 publications

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“…such as salt formations, solid dispersion formations, and cocrystals, have been developed to improve the solubility of FBX [22][23][24][25]. Cocrystals of FBX have especially gained attention.…”

Section: Methodsmentioning

confidence: 99%

“…From physicochemical and pharmacokinetic perspectives, FBX is a poorly water-soluble and highly permeable drug belonging to the biopharmaceutics classification system (BCS) class II [ 1 , 17 , 18 , 19 , 20 , 21 ]. Thus, various formulations of FBX, such as salt formations, solid dispersion formations, and cocrystals, have been developed to improve the solubility of FBX [ 22 , 23 , 24 , 25 ]. Cocrystals of FBX have especially gained attention.…”

Section: Introductionmentioning

confidence: 99%

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Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice

Yu,

You,

Bae

et al. 2023

Pharmaceutics

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Febuxostat (FBX), a selective xanthine oxidase inhibitor, belongs to BCS class II, showing low solubility and high permeability with a moderate F value (<49%). Recently, FBX/L-pyroglutamic acid cocrystal (FBX-PG) was developed with an improving 4-fold increase of FBX solubility. Nevertheless, the in vivo pharmacokinetic properties of FBX-PG have not been evaluated yet. Therefore, the pharmacokinetic feasibility of FBX in FBX- and FBX-PG-treated rats and mice was compared in this study. The results showed that the bioavailability (F) values of FBX were 210% and 159% in FBX-PG-treated rats and mice, respectively. The 2.10-fold greater total area under the plasma concentration–time curve from time zero to infinity (AUC0-inf) of FBX was due to the increased absorption [i.e., 2.60-fold higher the first peak plasma concentration (Cmax,1) at 15 min] and entero-hepatic circulation of FBX [i.e., 1.68-fold higher the second peak plasma concentration (Cmax,2) at 600 min] in FBX-PG-treated rats compared to the FBX-treated rats. The 1.59-fold greater AUC0-inf of FBX was due to a 1.65-fold higher Cmax,1 at 5 min, and a 1.15-fold higher Cmax,2 at 720 min of FBX in FBX-PG-treated mice compared to those in FBX-treated mice. FBX was highly distributed in the liver, stomach, small intestine, and lungs in both groups of mice, and the FBX distributions to the liver and lungs were increased in FBX-PG-treated mice compared to FBX-treated mice. The results suggest the FBX-PG has a suitable pharmacokinetic profile of FBX for improving its oral F value.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice

Yu,

You,

Bae

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…It is eliminated by the renal and hepatic systems. However, FBX is a BCS class II drug, 3 which is poorly soluble in water and has low solubility and wettability, leading to poor bioavailability. 4 To overcome this restriction, an emulsion-based topically applied formulation is developed, which incorporate hydrophobic therapeutic moieties and improve patient compliance.…”

Section: Introductionmentioning

confidence: 99%