Abstract：
Rivastigmine hydrogen tartrate (RHT), a reversible cholinesterase inhibitor, is considered as the first-line therapy for mild to moderate Alzheimer\'s disease. Asiaticoside (AS), a pentacyclic triterpenoid saponin, is well known as cognitive enhancer due to its antioxidant effect. Based on the hypothesis of their synergistic therapeutic potential, RHT and AS were co-encapsulated in niosomal formulation. A simple, precise, and accurate high-performance liquid chromatography method was developed for simultaneous quantitative analysis. The chromatographic parameters were optimized by Box-Behnken experimental design. The separation was performed on a reversed-phase Phenomenex C18 (150 mm × 4.6 mm, 5 μm) column at 30 °C under the UV detection of 210 nm. The optimized mobile phase consisted of a mixture of 20 mM potassium dihydrogen phosphate buffer (pH 2.6) and acetonitrile (72:28 % v/v) under the isocratic mode at the flow rate of 0.9 mL/min. The developed method was fully validated under the ICH guidelines and could be successfully applied for simultaneous quantitative analysis of RHT and AS in niosomal formulation.
摘要：
酒石酸氢利伐斯的明（RHT），一种可逆的胆碱酯酶抑制剂,被认为是轻度至中度阿尔茨海默病的一线治疗。Asiaticoside（AS），五环三萜皂苷，由于其抗氧化作用，被称为认知增强剂。基于它们协同治疗潜力的假设，将RHT和AS共包封在脂质体制剂中。一个简单的，精确，建立了准确的高效液相色谱同时定量分析方法。采用Box-Behnken实验设计对色谱参数进行优化。分离是在反相PhenomenexC18（150mm×4.6mm，5μm）在30°C下在210nm的UV检测下进行色谱柱。优化的流动相由20mM磷酸二氢钾缓冲液(pH2.6)和乙腈(72:28%v/v)的混合物在等度模式下以0.9mL/min的流速组成。所开发的方法在ICH指南下得到了充分验证，可成功应用于脂质体制剂中RHT和AS的同时定量分析。
