以離子電透入法與電破法於體外與體內促進Meloxicam 鹽類經皮吸收之研究   全文下載

The Effects of Iontophoresis and Electroporation on Transdermal Delivery of Meloxicam Salts Evaluated In Vitro and In Vivo

本研究之目的為利用離子電透入法與電破法之物理促進法在體外與體內促進meloxicam 的兩個鹽類 – meloxicam sodium 與meloxicam potassium – 之經皮吸收。體外實驗以Wistar rat 背部完整皮膚與人類表皮（human epidermal membrane）為穿透障壁，而體內實驗則以Wistar rat 為動物模式進行研究。離子電透入法和其與電破法之合併法可顯著促進鈉鹽與鉀鹽於體外的經皮穿透量，且離子電透入法與合併法之效果相當，再者，以人類表皮為穿透障壁時，合併法對鉀鹽的促進效果優於鈉鹽。離子電透入法與合併法於體外實驗中引起物種間差異。單獨使用電破法可能抑制鈉鹽且促進鉀鹽的體外穿透。相對於對照組，離子電透入法、電破法與合併法三者可顯著增加兩個鹽類於體內實驗的血中濃度曲線下面積（AUC），並且，相較於鈉鹽，鉀鹽更能得到合併物理促進法的幫助而得到較高的血中最大濃度。

The aim of this study was to evaluate the transdermal delivery of two meloxicam salts, meloxicam sodium and meloxicam potassium, enhanced by iontophoresis and/or electroporation in vitro with Wistar rat dorsal skin and human epidermal membrane (HEM) as barriers and in vivo with Wistar rat as the animal model. Iontophoresis and its combination with electroporation could significantly enhance the in vitro permeation of both salts, and two protocols had the same enhancement to each salt. Furthermore, the combination protocol had more enhancement to potassium salt than sodium salt. Interspecies difference was found in some electrical protocols. Electroporation might depress the transdermal delivery of meloxicam sodium while it might enhance that of meloxicam potassium. Iontophoresis, electroporation and their combination could increase the delivery of the two salts and result in significantly higher AUC of drug concentration to time in vivo. It was concluded that the in vitro and in vivo transdermal delivery of meloxicam potassium was more facilitated by the combination protocol than meloxicam sodium.