Objective To compare the bioequivalence of the test formulation and the reference formulation of Crisaborole Ointments in healthy subjects after single topical dosage.Methods A randomized,open-label,two-treatment,single-dose,and two-way crossover design was adopted.Subjects were locally applied with 4 g(5 mg/cm2)Crisaborole Ointments test or reference preparation under fasting condition in each period,and the washout period was 4 d.The concentrations of crisaborole in human plasma were determined by HPLC-MS/MS method,and the pharmacokinetic parameters of crisaborole were calculated using noncompartmental analysis model(NCA)in Phoenix WinNonlin software(version 8.3).Results After a single fasting administration,the 90%confidence intervals of the geometric mean ratios(the test formulation/reference formulation)of Cmax,AUC0-t,and AUC0-∞ of crisaborole fell within the bioequivalent range of 80.00%to 125.00%.Conclusion The test and reference preparations of Crisaborole Ointments are bioequivalent in healthy subjects after single topical dosage of 4 g(5 mg/cm2)under fasting condition.
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