枸橼酸托法替尼片两种制剂在中国健康志愿者空腹和进食条件下的生物等效性和安全性:随机、开放标签、两阶段、单剂量、交叉试验

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Yanping Liu, Yuping Ning, Yan Shi, Man Xu, Juanmin Tao, Yafen Dong, Jun Ma, Yan Qiu
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引用次数: 0

摘要

目的评价枸橼酸托法替尼片两种不同制剂在中国健康受试者空腹和进食条件下的生物等效性,并观察试验制剂和参比制剂在健康受试者中的安全性。研究方法这项随机、开放标签、两阶段、交叉、生物等效性研究纳入了64名中国健康受试者(空腹:32人,进食:32人)。受试者被分配接受单次5毫克剂量的枸橼酸托法替尼试验药片或参比药片。在用药前和用药后 24 小时内采集血样。生物等效性评估采用了从零到最后可测量浓度的血浆浓度时间曲线下面积(AUC0-t)、从零时到无限时的面积(AUC0-∞)和最大血浆浓度(Cmax)。在研究期间,从受试者接受试验药物到最后一次访问结束,通过生命体征、体格检查、实验室检查和 12 导联心电图进行安全性评估。研究结果在进食条件下,枸橼酸托法替尼片的AUC0-t、Cmax和AUC0-∞的试验/参考几何平均比值的90%CI分别为98.40%-104.16%、89.96%-116.70%和98.50%-104.15%。在空腹条件下,枸橼酸托法替尼片的AUC0-t、Cmax和AUC0-∞的试验/参考几何平均比值的90%CI分别为93.65-101.60%、90.06-109.15%和93.88-101.51%。没有发生严重事件。结论Cmax、AUC0-t和AUC0-∞的几何平均比值(试验/参比)的90% CI在80.00%-125.00%范围内,表明在空腹和进食条件下,中国健康受试者的试验制剂与参比制剂具有等效性。就安全性而言,两者相似。该试验的注册号为 CTR20190366。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Bioequivalence and Safety of Two Formulations of Tofacitinib Citrate Tablets in Healthy Chinese Volunteers under Fasting and Fed Conditions: Randomized, Open-Label, 2-Period, Single-Dose, Crossover Trials

Bioequivalence and Safety of Two Formulations of Tofacitinib Citrate Tablets in Healthy Chinese Volunteers under Fasting and Fed Conditions: Randomized, Open-Label, 2-Period, Single-Dose, Crossover Trials

Purpose. To evaluate the bioequivalence of two different tofacitinib citrate tablets formulations among healthy Chinese subjects under fasting and fed conditions and to observe the safety of test preparation and reference preparation in healthy subjects. Method. This randomized, open-label, 2-period, crossover, bioequivalence study included 64 healthy Chinese subjects (fasting: n = 32, fed: n = 32). The subjects were assigned to receive a single 5-mg dose of the test or a reference tofacitinib citrate tablets. Blood samples were collected at predose and up to 24 hours after dosing. Area under the plasma concentration time curve from zero to the last measurable concentration (AUC0-t), the area from time zero to infinite (AUC0-∞), and maximum plasma concentration (Cmax) were used for bioequivalence assessment. Safety assessment was conducted by vital signs, physical examination, laboratory examination, and 12-lead electrocardiogram during the study, from the time the subject receiving the test drug to the end of the last visit. Results. Under fed condition, the 90% CIs of the geometric mean ratios of the test/reference for tofacitinib citrate tablets were 98.40–104.16% for AUC0-t, 89.96–116.70% for Cmax, and 98.50–104.15% for AUC0-∞. Under fasting condition, the 90% CIs of the geometric mean ratios of the test/reference for tofacitinib citrate tablets were 93.65–101.60% for AUC0-t, 90.06–109.15% for Cmax, and 93.88–101.51% for AUC0-∞. There were no serious events. Conclusion. The 90% CI for the geometric mean ratio (test/reference) of Cmax, AUC0-t, and AUC0-∞ were within the range of 80.00%–125.00%, indicating that the test formulation was equivalent to the reference formulation in healthy Chinese subjects under both fasting and fed conditions. They are similar in terms of safety. This trial is registered with CTR20190366.

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来源期刊
CiteScore
4.10
自引率
5.00%
发文量
226
审稿时长
6 months
期刊介绍: The Journal of Clinical Pharmacy and Therapeutics provides a forum for clinicians, pharmacists and pharmacologists to explore and report on issues of common interest. Reports and commentaries on current issues in medical and pharmaceutical practice are encouraged. Papers on evidence-based clinical practice and multidisciplinary collaborative work are particularly welcome. Regular sections in the journal include: editorials, commentaries, reviews (including systematic overviews and meta-analyses), original research and reports, and book reviews. Its scope embraces all aspects of clinical drug development and therapeutics, including: Rational therapeutics Evidence-based practice Safety, cost-effectiveness and clinical efficacy of drugs Drug interactions Clinical impact of drug formulations Pharmacogenetics Personalised, stratified and translational medicine Clinical pharmacokinetics.
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