Ragab Marwa A A, Galal Shereen M, Korany Mohamed A, Ahmed Aya R
Faculty of Pharmacy, Department of Pharmaceutical Analytical Chemistry, University of Alexandria, El-Messalah, Alexandria, Egypt.
Luminescence. 2017 Dec;32(8):1417-1425. doi: 10.1002/bio.3339. Epub 2017 Jun 1.
LCZ696 (sacubitril/valsartan, Entresto™) is a therapy lately approved by United States Food and Drug Administration (US FDA) as a heart failure therapy. It is claimed to decrease the mortality rate and hospitalization for patients with chronic heart failure. This study is considered as the first report to investigate the fluorimetric behavior of sacubitril in addition to pursuing all the different conditions that may affect its fluorescence. Various conditions were studied, for example studying the effects of organized media, solvents and pH, which may affect the fluorescence behavior of sacubitril. For the simultaneous determination of the newly approved supramolecular complex of valsartan (VAL) and sacubitril (SAC) in their tablets, a sensitive and simple first derivative spectrofluorimetric method was developed. The method involved the measurement of native fluorescence at 416 nm and 314 nm (λ 249 nm) for VAL and SAC, respectively. The first (D1) derivative technique was applied to the emission data to resolve a partial overlap that appeared in their emission spectra. The proposed method was successfully applied for the assay of the two drugs in their supramolecular complex LCZ696 with no interference from common pharmaceutical additives. International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH) guidelines were followed in order to validate the proposed method.
LCZ696（沙库巴曲缬沙坦，商品名Entresto™）是一种最近被美国食品药品监督管理局（US FDA）批准用于治疗心力衰竭的药物。据称它可以降低慢性心力衰竭患者的死亡率和住院率。本研究被认为是第一份除了探究可能影响沙库巴曲荧光的所有不同条件之外，还研究其荧光行为的报告。研究了各种条件，例如研究有序介质、溶剂和pH对沙库巴曲荧光行为的影响。为了同时测定缬沙坦（VAL）和沙库巴曲（SAC）新批准的超分子复合物片剂中的含量，开发了一种灵敏且简便的一阶导数荧光分光光度法。该方法分别通过测量VAL在416 nm和SAC在314 nm（λ 249 nm）处的天然荧光来进行。一阶（D1）导数技术应用于发射数据，以解决它们发射光谱中出现的部分重叠问题。所提出的方法成功应用于测定超分子复合物LCZ696中两种药物的含量，不受常见药用辅料的干扰。本研究遵循人用药品注册技术要求国际协调会议（ICH）指南对所提出的方法进行验证。
