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离子导入辅助布比卡因和利多卡因作为麻醉药物的经皮给药的比较研究。

Comparative study of iontophoresis-assisted transdermal delivery of bupivacaine and lidocaine as anesthetic drugs.

作者信息

Morarad Rawita, Uerpairojkit Ketchada, Chalermkitpanit Pornpan, Sirivat Anuvat

机构信息

Conductive and Electroactive Polymers Research Unit, The Petroleum and Petrochemical College, Chulalongkorn University, Bangkok, 10330, Thailand.

Department of Anesthesiology, Faculty of Medicine, King Chulalongkorn Memorial Hospital, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand.

出版信息

Drug Deliv Transl Res. 2025 Feb;15(2):688-699. doi: 10.1007/s13346-024-01627-5. Epub 2024 May 23.

Abstract

Postoperative pain management is an important aspect of the overall surgical care process. Effective pain management not only provides patient comfort but also promotes faster recovery and reduces the risk of complications. Bupivacaine (BUP) and Lidocaine (LID) transdermal drug deliveries via thermoplastic polyurethane matrix (TPU) and iontophoresis technique are proposed here as alternative routes for postoperative pain instead of the injection route. Under applied electric field, the amounts of BUP and LID released were 95% and 97% from the loaded amounts, which were higher than the passive patch of 40%. The time to equilibrium of BUP turned out to be faster than the time to equilibrium of LID by approximately 1.5 times. This was due to 2 factors namely the drug molecular weight and the drug pK value; they play an important role in the selection of a suitable drug for fast-acting or long-acting for the postoperative patients. By using this transdermal patch via iontophoresis system, BUP was deemed as the suitable drug for fast-acting due to the shorter time to equilibrium, whereas LID was the suitable drug for long-acting. The in-vitro drug release - permeation study through a porcine skin indicated the efficiency and potential of the system with the amounts of drug permeated up to 76% for BUP and 81% for LID. The TPU transdermal system was demonstrated here as potential to deliver BUP and LID for postoperative patients.

摘要

术后疼痛管理是整个外科护理过程的一个重要方面。有效的疼痛管理不仅能为患者提供舒适感,还能促进更快康复并降低并发症风险。本文提出通过热塑性聚氨酯基质(TPU)和离子电渗技术进行布比卡因(BUP)和利多卡因(LID)的经皮给药,作为术后疼痛管理的替代途径,以取代注射途径。在施加电场的情况下,BUP和LID的释放量分别为加载量的95%和97%,高于被动贴片的40%。结果表明,BUP达到平衡的时间比LID快约1.5倍。这是由于两个因素,即药物分子量和药物pK值;它们在为术后患者选择速效或长效的合适药物方面起着重要作用。通过使用这种离子电渗系统的透皮贴剂,由于达到平衡的时间较短,BUP被认为是速效的合适药物,而LID是长效的合适药物。通过猪皮进行的体外药物释放 - 渗透研究表明该系统的有效性和潜力,BUP的药物渗透量高达76%,LID为81%。本文证明了TPU透皮系统为术后患者递送BUP和LID的潜力。

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