Reckitt Benckiser Health Limited, Slough, United Kingdom.
Simbec Research Ltd, Merthyr Tydfil, United Kingdom.
Clin Ther. 2019 Aug;41(8):1486-1498. doi: 10.1016/j.clinthera.2019.04.040. Epub 2019 Jun 12.
This study aimed to assess the comparative bioavailability between ibuprofen acid orodispersible tablets (Test product) and ibuprofen acid oral tablets (Reference product).
This was a randomized, single-dose, 3-way crossover, open-label, pharmacokinetic study in 36 healthy male and female volunteers. Blood samples were taken periodically over a 12-h period after dosing to derive total plasma ibuprofen and S(+)/R(-) ibuprofen enantiomer pharmacokinetic parameters; safety profile and tolerability were evaluated throughout the study.
After a single-dose administration of ibuprofen acid oral tablets (2 × 200 mg), the total ibuprofen C and AUC (geometric least square [LS] mean) for the Test product was 29.4 μg/mL and 100.6 h/μg/mL, respectively, and for the Reference product it was 30.6 μg/mL and 98.7 h/μg/mL. The geometric LS mean Test/Reference ratio 90% CI for both total ibuprofen C (90.71-101.77) and AUC (98.72-105.23) was contained entirely within the predefined 80.00%-125.00% lower and upper limits; in addition, no statistically significant difference was found in T (P = 0.1819) after fasted administration of the Test and Reference products. There were 4 mild treatment emergent adverse events, considered unrelated to the study drug, reported by 2 volunteers during the study; no serious adverse events, no suspected unexpected serious adverse events. and no clinically significant changes in laboratory safety, vital signs, or 12-lead ECG measurements were reported. The enantiomer-specific analysis mirrored that of total ibuprofen, with the C and AUC LS mean Test/Reference ratio 90% CI for both ibuprofen S(+) and R(-) enantiomers contained entirely within the predetermined 80%-125.00% limits.
This study found that ibuprofen acid 200 mg orodispersible tablets and ibuprofen acid 200 mg tablets met the regulatory criteria for bioequivalence for AUC and C. Post hoc analysis of ibuprofen both S(+) and R(-) enantiomers mirrored the findings for total ibuprofen. All investigational products were found to be well tolerated. Clinicaltrials.gov identifier: NCT03180879.
本研究旨在评估布洛芬酸口崩片（试验品）与布洛芬酸口服片剂（参比品）之间的生物等效性。
这是一项在 36 名健康男性和女性志愿者中进行的随机、单剂量、3 期交叉、开放标签、药代动力学研究。给药后 12 小时内定期采集血样，以获得总血浆布洛芬和 S(+)/R(-)布洛芬对映体药代动力学参数；在整个研究过程中评估安全性概况和耐受性。
单次给予布洛芬酸口服片剂（2×200mg）后，试验品的总布洛芬 C 和 AUC（几何最小二乘[LS]均值）分别为 29.4μg/mL 和 100.6μg·h/μg，参比品分别为 30.6μg/mL 和 98.7μg·h/μg。总布洛芬 C（90.71-101.77）和 AUC（98.72-105.23）的试验/参比几何 LS 均值 90%CI 完全包含在预定的 80.00%-125.00%下限和上限内；此外，空腹给予试验品和参比品后，T 无统计学差异（P=0.1819）。在研究过程中，有 4 名志愿者报告了 4 起轻度治疗突发不良事件，认为与研究药物无关；无严重不良事件、疑似意外严重不良事件和临床意义显著的实验室安全性、生命体征或 12 导联心电图测量值变化。对映体特异性分析与总布洛芬相似，布洛芬 S(+)和 R(-)对映体的 C 和 AUC LS 均值试验/参比 90%CI 完全包含在预定的 80%-125.00%范围内。
本研究发现，布洛芬酸 200mg 口崩片和布洛芬酸 200mg 片剂在 AUC 和 C 方面均符合生物等效性的监管标准。对总布洛芬的 S(+)和 R(-)对映体的事后分析结果与总布洛芬一致。所有研究产品均被认为具有良好的耐受性。临床试验.gov 标识符：NCT03180879。
