目的 比較克立硼羅軟膏受試制劑與參比制劑在健康受試者中單次局部外用后的生物等效性。方法 采用隨機(jī)、開(kāi)放、兩制劑、單次給藥、雙交叉設(shè)計(jì)。受試者于每周期在空腹?fàn)顟B(tài)下單次局部外用克立硼羅軟膏受試制劑或參比制劑4 g（約5 mg/cm²），清洗期為4 d。采用高效液相色譜-串聯(lián)質(zhì)譜法（HPLC-MS/MS）測(cè)定人血漿中克立硼羅的血藥濃度，使用Phoenix WinNonlin軟件（8.3版本）中的非房室模型（NCA）模塊計(jì)算克立硼羅的藥動(dòng)學(xué)參數(shù)。結(jié)果 單次給藥后，克立硼羅的C_max、AUC_0-t和AUC_0-∞的幾何均值比（受試制劑/參比制劑）的90%置信區(qū)間均在80.00%～125.00%。結(jié)論 克立硼羅軟膏受試制劑與參比制劑在健康受試者空腹條件下單次局部外用4 g（約5 mg/cm²）后具有生物等效性。

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 C_max, AUC_0-t, and AUC_{0- ∞} 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.

R986