Wang Menglin, Li Longwei, Xie Junxia, Sun Yinghua, Ling Guixia, He Zhonggui
School of Pharmacy, Shenyang Pharmaceutical University, No103, Wenhua Road, Shenyang, 110016, China.
Research and Development Department, Beijing Wan Sheng Pharmaceutical Co., Ltd., No8, Guangyuan East Street, Tongzhou District, Beijing, 101113, China.
AAPS PharmSciTech. 2017 Aug;18(6):2141-2148. doi: 10.1208/s12249-016-0695-8. Epub 2016 Dec 29.
Topical delivery has many benefits toward NSAIDs administration, and the best-selling transdermal preparation in 2015 was the NSAID patch MOHRUS®. Herein, we report a ketoprofen adhesive patch (KAP) and evaluate the penetration and absorption compared to MOHRUS®. Microdialysis sampling technique was applied to determine drug penetration in the dermis and subcutaneous tissue. Simultaneously, blood samples were withdrawn over time to obtain the drug absorption in plasma. The ketoprofen concentrations in the dermis, subcutaneous tissue, and plasma were compared with the commercially available patch (MOHRUS®). Based on the detection, pharmacokinetic parameters including C, T, and AUC were determined for both the formulations. No significant differences were found in the dermis, subcutaneous tissue, and plasma in rats according to the bioequivalence assessment. The KAP demonstrated multiple therapeutic advantages including the controlled drug release and the sustained drug concentration in the skin as well as in plasma. The pharmacokinetic study coupled with microdialysis sampling provided an effective strategy to evaluate transdermal delivery.
局部给药对于非甾体抗炎药（NSAIDs）的应用具有诸多益处，2015年最畅销的透皮制剂是NSAID贴片MOHRUS®。在此，我们报告一种酮洛芬贴剂（KAP），并与MOHRUS®相比评估其渗透和吸收情况。应用微透析采样技术来测定药物在真皮和皮下组织中的渗透。同时，随着时间推移采集血样以获取药物在血浆中的吸收情况。将真皮、皮下组织和血浆中的酮洛芬浓度与市售贴片（MOHRUS®）进行比较。基于检测结果，确定了两种制剂的药代动力学参数，包括Cmax、Tmax和AUC。根据生物等效性评估，在大鼠的真皮、皮下组织和血浆中未发现显著差异。KAP展现出多种治疗优势，包括药物的控释以及在皮肤和血浆中持续的药物浓度。药代动力学研究与微透析采样相结合提供了一种评估透皮给药的有效策略。
