背景:一种非Ergot多巴胺激动剂(NEDA)罗替戈汀已被设计为一种新的透皮给药系统。
目的:为了保持药物含量的最佳均匀性,罗替戈汀透皮贴剂是利用溶剂流延技术开发的。
方法:透皮贴剂的特性,包括贴片重量,折叠耐力,补片厚度,表面形态,抗拉强度,溶胀率,表面pH值,体外释放研究,保水率,药物含量的均匀性,和离体渗透研究,决心。
结果:体外药物释放研究明确证明了药物释放控制聚合物相互作用。在药物释放速率开始下降之前没有明显的滞后期。开发的贴剂在24小时内显示出70±1.18%的药物释放延长。渗透研究的结果表明,在24小时内,61±2.52%的罗替戈汀通过表皮屏障渗透。
结论:开发的包含罗替戈汀的透皮贴剂明显置于真皮层上,并且基于上述因素将适当的剂量输送到循环中更长的时间。这项研究的结果说明了透皮贴剂治疗帕金森病的有效方法。
BACKGROUND: A Non-Ergot Dopamine Agonist (NEDA)
rotigotine has been designed as a new transdermal drug delivery system.
OBJECTIVE: To maintain optimum homogeneity in drug content, the
rotigotine transdermal patch was developed utilizing a solvent casting technique.
METHODS: The characteristics of a transdermal patch, including patch weight, folding endurance, patch thickness, surface morphology, tensile strength, swelling rate, surface pH, in vitro release studies, water retention rate, uniformity of drug content, and ex-vivo permeation studies, were determined.
RESULTS: In vitro drug release studies unequivocally demonstrated that drug release controlled polymer interactions. There was no apparent lag period before the drug release rate started to decline. The developed patch showed 70 ± 1.18 % of prolongation of drug release within 24 hours. The result of the penetration studies demonstrated that 61 ± 2.52% of
rotigotine permeated through the epidermal barrier within 24 h.
CONCLUSIONS: The developed transdermal patch comprising
rotigotine was evidently placed on the dermis layer, and an appropriate dose was delivered into circulation for a longer time based on the aforementioned factors. The findings of this study illustrate the effective approach of transdermal patches to treat Parkinson\'s disease.