Shams M S, Alam M I, Ali A, Sultana Y, Aqil M, Shakeel F
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.
Pharmazie. 2010 Sep;65(9):679-82.
Monolithic transdermal therapeutic systems (TTS) were developed for sustained antihypertensive effect of losartan potassium using the polymers Eudragit E 100 and polyvinyl pyrrolidone VA 64. The developed formulations (polymeric films) were evaluated for physical characteristics, ex vivo (histopathology) and in vivo (pharmacokinetic studies). Pharmacokinetic parameters, such as C(max), t(max), and AUC were estimated. The transdermal formulation in the present study was found to enhance the relative bioavailability of losartan potassium by 2.2 times with reference to an oral delivery. The increased bioavailability might be due to elimination of hepatic first pass metabolism. Thus, the transdermal formulation F3E with polymeric composition of Eudragit E 100 and polyvinyl pyrrolidone VA 64 (5:3) was found to provide prolonged steady state concentrations of losartan potassium with minimal fluctuations and improved bioavailability.
采用聚合物Eudragit E 100和聚乙烯吡咯烷酮VA 64，开发了用于氯沙坦钾持续降压作用的整体式透皮治疗系统（TTS）。对所开发的制剂（聚合物膜）进行了物理特性、体外（组织病理学）和体内（药代动力学研究）评估。估算了药代动力学参数，如C(max)、t(max)和AUC。本研究中的透皮制剂相对于口服给药，使氯沙坦钾的相对生物利用度提高了2.2倍。生物利用度的提高可能是由于消除了肝脏首过代谢。因此，发现聚合物组成为Eudragit E 100和聚乙烯吡咯烷酮VA 64（5:3）的透皮制剂F3E能提供氯沙坦钾的延长稳态浓度，波动最小且生物利用度提高。
