Bioequivalence of crisaborole ointment in Chinese healthy subjects under topical conditions
SUI Xin
WANG Hua-wei
LI Xiao-bin
WU Xiu-jun
LI Mei-ye
WANG Ning
WANG Wen-ping
Abstract：Objective:To study the pharmacokinetics of crisaborole ointment in healthy subjects in China,and to evaluate the bioequivalence between the domestic test preparation and the original reference preparation.Methods:A single dose,randomized,open,two-period,crossover drug trial design was adopted.A total of 36 healthy subjects were randomly divided into two groups,and administered test preparation T or the reference preparation R(crisaborole ointment,4.0g)each period,respectively.The concentrations of crisaborole in plasma at different time points were determined by LC-MS/MS.The pharmacokinetic parameters were calculated and the bioequivalence was compared by SAS9.4 program.Results:The pharmacokinetic parameters of crisaborole for test and reference preparations in fasting condition were as follows:Cmax are 29.39 and 29.25 ng·mL-1;AUC0-t are 288.32 and 294.07 ng·h·mL-1;AUC0-∞ are 291.07 and 296.54 ng·h·mL-1,respectively.The ratios of crisaborole test preparation and reference preparation Cmax,AUC0-t,AUC0-∞ were 98.55%,97.28%,and 97.35%,respectively.The 90%confidence intervals were 91.26%～106.41%,90.20%～104.93%,and 90.37%～104.88%,respectively.Conclusion:The test and reference preparations of crisaborole ointment were bioequivalent in healthy Chinese subjects.
Keywords：crisaborolepharmacokineticsbioequivalenceliquid chromatography-tandem mass spec-trometryointment
Publication Date：2025-10-15
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：5( 2094-2098 )