Abstract：
Amiloride is a U.S. Food and Drug Administration-approved diuretic agent used to treat hypertension and congestive heart failure. Recent human and animal studies have suggested that amiloride may also have a role in treating anxiety through its acid-sensing ion channel antagonism. Intranasal administration of amiloride nasal spray via an extemporaneously compounded preparation has the potential for rapid delivery to the site of action to achieve therapeutic outcomes in individual patients with anxiety disorders. However, these patient-specific preparations do not have the pre-formulation characterization, including chemical stability, that conventional manufactured dosage forms have. The objective of this study was to assess the estimated chemical stability of compounded amiloride nasal spray over 6 months and 12 months utilizing accelerated degradation with high heat and the Arrhenius equation. A stability-indicating highperformance liquid chromatography analytical method was employed at appropriate intervals over a 12-month period to reveal that amiloride remained chemically stable over the period tested and by extrapolation. Physical stability and compatibility with the preservative benzyl alcohol were also confirmed via visual inspection, pH monitoring, and measurement of turbidity.
摘要：
阿米洛利是美国食品和药物管理局批准的利尿剂，用于治疗高血压和充血性心力衰竭。最近的人类和动物研究表明，阿米洛利还可能通过其酸敏感离子通道拮抗作用在治疗焦虑症中发挥作用。通过临时复合制剂鼻内施用阿米洛利鼻喷雾剂具有快速递送至作用部位以在患有焦虑症的个体患者中实现治疗结果的潜力。然而,这些患者特异性制剂不具有制剂前的特征，包括化学稳定性，传统制造的剂型。这项研究的目的是评估复合阿米洛利鼻喷雾剂在6个月和12个月内利用高热加速降解和阿伦尼乌斯方程的估计化学稳定性。在12个月的时间内，以适当的间隔采用了指示稳定性的高效液相色谱分析方法，以揭示阿米洛利在测试期间和通过外推法保持化学稳定。物理稳定性和与防腐剂苯甲醇的相容性也通过目视检查证实。pH监测,和浊度的测量。
