Abstract：
OBJECTIVE: This study assessed effect of food on pharmacokinetics (PK) and safety of fuzuloparib capsules.
METHODS: A randomized, open-label, two-cycle, two-sequence, crossover clinical trial was conducted. 20 subjects were randomly assigned to 2 groups at a 1:1 ratio. The first group subjects were orally administered 150 mg fuzuloparib capsules under fasting condition in first dosing cycle. The same dose of fuzuloparib capsules were taken under postprandial state after a 7-day washout period. The second group was reversed. 3 ml whole blood was collected at each blood collection point until 72 h post dose. PK parameters were calculated. Furthermore, safety assessment was performed.
RESULTS: The time to maximum concentration (Tmax) was prolonged to 3 h and maximum concentration (Cmax) decreased by 18.6% on high-fat diets. 90% confidence intervals (CIs) of geometric mean ratios (GMRs) for Cmax, area under the concentration-time curve from time zero to time t (AUC0-t), and area under the concentration-time curve extrapolated to infinity (AUC0-∞) after high-fat meal were 71.6-92.6%, 81.7-102.7% and 81.6-102.5%, respectively. All treatment-emergent adverse events (TEAEs) were grade 1; No serious adverse events (SAEs), serious unexpected suspected adverse reaction (SUSAR) or deaths were reported.
CONCLUSIONS: Food decreased the absorption rate and slowed time to peak exposure of fuzuloparib capsules, without impact on absorption extent. Dosing with food was found to be safe for fuzuloparib capsules in this study.
BACKGROUND: This study was registered with chinadrugtrials.org.cn (identifier: CTR20221498).
METHODS: A randomized, open-label, two-cycle, two-sequence, crossover clinical trial was conducted. 20 subjects were randomly assigned to 2 groups at a 1:1 ratio. The first group subjects were orally administered 150 mg fuzuloparib capsules under fasting condition in first dosing cycle. The same dose of fuzuloparib capsules were taken under postprandial state after a 7-day washout period. The second group was reversed. 3 ml whole blood was collected at each blood collection point until 72 h post dose. PK parameters were calculated. Furthermore, safety assessment was performed.
RESULTS: The time to maximum concentration (Tmax) was prolonged to 3 h and maximum concentration (Cmax) decreased by 18.6% on high-fat diets. 90% confidence intervals (CIs) of geometric mean ratios (GMRs) for Cmax, area under the concentration-time curve from time zero to time t (AUC0-t), and area under the concentration-time curve extrapolated to infinity (AUC0-∞) after high-fat meal were 71.6-92.6%, 81.7-102.7% and 81.6-102.5%, respectively. All treatment-emergent adverse events (TEAEs) were grade 1; No serious adverse events (SAEs), serious unexpected suspected adverse reaction (SUSAR) or deaths were reported.
CONCLUSIONS: Food decreased the absorption rate and slowed time to peak exposure of fuzuloparib capsules, without impact on absorption extent. Dosing with food was found to be safe for fuzuloparib capsules in this study.
BACKGROUND: This study was registered with chinadrugtrials.org.cn (identifier: CTR20221498).
摘要：
目的：本研究评估了食品对夫祖洛尼胶囊的药代动力学（PK）和安全性的影响。
方法：随机，开放标签，两个周期，两个序列，进行交叉临床试验.20名受试者以1:1的比例随机分配到2组。第一组受试者在第一给药周期中在禁食条件下口服150mg夫祖洛尼胶囊。在7天的冲洗期后，在餐后状态下服用相同剂量的fuzuloparib胶囊。第二组被逆转。在每个血液收集点收集3ml全血直到给药后72小时。计算PK参数。此外，进行安全性评估.
结果：在高脂饮食中，达到最大浓度（Tmax）的时间延长至3h，最大浓度（Cmax）降低了18.6％。Cmax的几何平均比(GMR)的90%置信区间(CI)，从时间零到时间t的浓度-时间曲线下面积（AUC0-t），高脂餐后外推到无穷大的浓度-时间曲线下面积（AUC0-∞）为71.6-92.6％，81.7-102.7%和81.6-102.5%，分别。所有因治疗引起的不良事件（TEAE）均为1级；无严重不良事件（SAE），报告了严重的意外可疑不良反应（SUSAR）或死亡。
结论：食物降低了夫祖洛尼胶囊的吸收速率并减慢了达到峰值暴露的时间，不影响吸收程度。在这项研究中，发现食物给药对fuzuloparib胶囊是安全的。
背景：本研究已在chinadrugtrials.org注册。cn(标识符:CTR20221498)。
方法：随机，开放标签，两个周期，两个序列，进行交叉临床试验.20名受试者以1:1的比例随机分配到2组。第一组受试者在第一给药周期中在禁食条件下口服150mg夫祖洛尼胶囊。在7天的冲洗期后，在餐后状态下服用相同剂量的fuzuloparib胶囊。第二组被逆转。在每个血液收集点收集3ml全血直到给药后72小时。计算PK参数。此外，进行安全性评估.
结果：在高脂饮食中，达到最大浓度（Tmax）的时间延长至3h，最大浓度（Cmax）降低了18.6％。Cmax的几何平均比(GMR)的90%置信区间(CI)，从时间零到时间t的浓度-时间曲线下面积（AUC0-t），高脂餐后外推到无穷大的浓度-时间曲线下面积（AUC0-∞）为71.6-92.6％，81.7-102.7%和81.6-102.5%，分别。所有因治疗引起的不良事件（TEAE）均为1级；无严重不良事件（SAE），报告了严重的意外可疑不良反应（SUSAR）或死亡。
结论：食物降低了夫祖洛尼胶囊的吸收速率并减慢了达到峰值暴露的时间，不影响吸收程度。在这项研究中，发现食物给药对fuzuloparib胶囊是安全的。
背景：本研究已在chinadrugtrials.org注册。cn(标识符:CTR20221498)。
