El Maghraby Gamal M, Arafa Mona F, Osman Mohamed A
Department of Pharmaceutical Technology, College of Pharmacy, University of Tanta , Tanta , Egypt.
Drug Dev Ind Pharm. 2014 Dec;40(12):1637-44. doi: 10.3109/03639045.2013.841186. Epub 2013 Oct 4.
This study investigated simultaneous transdermal delivery of indomethacin and benzocaine from microemulsion. Eucalyptus oil based microemulsion was used with Tween 80 and ethanol being employed as surfactant and cosurfactant, respectively. A microemulsion formulation comprising eucalyptus oil, polyoxyethylene sorbitan momooleate (Tween 80), ethanol and water (20:30:30:20) was selected. Indomethacin (1% w/w) and benzocaine (20% w/w) were incorporated separately or combined into this formulation before in vitro and in vivo evaluation. Application of indomethacin microemulsion enhanced the transdermal flux and reduced the lag time compared to saturated aqueous control. The same trend was evident for benzocaine microemulsion. Simultaneous application of the two drugs in microemulsion provided similar enhancement pattern. The in vivo evaluation employed the pinprick method and revealed rapid anesthesia after application of benzocaine microemulsion with the onset being 10 min and the action lasting for 50 min. For indomethacin microemulsion, the analgesic effect was recorded after 34.5 min and lasted for 70.5 min. Simultaneous application of benzocaine and indomethacin provided synergistic effect. The onset of action was achieved after 10 min and lasted for 95 min. The study highlighted the potential of microemulsion formulation in simultaneous transdermal delivery of two drugs.
本研究考察了吲哚美辛和苯佐卡因在微乳中的同步透皮给药情况。使用了以桉叶油为基础的微乳，分别以吐温80和乙醇作为表面活性剂和助表面活性剂。选择了一种由桉叶油、聚氧乙烯山梨醇单油酸酯（吐温80）、乙醇和水（20:30:30:20）组成的微乳制剂。在进行体外和体内评价之前，将吲哚美辛（1% w/w）和苯佐卡因（20% w/w）分别或合并加入该制剂中。与饱和水溶液对照相比，吲哚美辛微乳的应用提高了透皮通量并缩短了滞后时间。苯佐卡因微乳也呈现出相同的趋势。两种药物在微乳中的同步应用提供了相似的增强模式。体内评价采用针刺法，结果显示，应用苯佐卡因微乳后迅速产生麻醉效果，起效时间为10分钟，作用持续50分钟。对于吲哚美辛微乳，镇痛效果在34.5分钟后出现，持续70.5分钟。苯佐卡因和吲哚美辛的同步应用产生了协同作用。起效时间为10分钟，作用持续95分钟。该研究突出了微乳制剂在两种药物同步透皮给药方面的潜力。
