Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut 71524, Egypt.
General Courses Unit, Faculty of Sciences and Arts, King Khalid University, Dhahran Aljanoub, Saudi Arabia.
Spectrochim Acta A Mol Biomol Spectrosc. 2021 Sep 5;258:119806. doi: 10.1016/j.saa.2021.119806. Epub 2021 Apr 8.
α-Difluoromethylornithine or Eflornithine is an FDA-approved drug used for the treatment of Sleeping Sickness (as vials dosage form) and also used for diminishing the unwanted excess facial hair in the hirsutism (as creams dosage form). The proposed work is based on the condensation interaction between the amino moiety of Eflornithine and O-phthalaldehyde/2-mercaptoethanol to form a highly fluorescent isoindole derivative. The fluorescence and the Resonance Rayleigh Scattering (RRS) intensities of the reaction product were greatly augmented upon the addition of hexadecyl-trimethyl ammonium bromide by 153% and 250%, respectively. After optimization of the reaction conditions, the formed isoindole derivative was measured fluorometrically at λ= 429 nm after λ= 337 nm. Moreover, the significant augmentation in the RRS intensity of the formed product was measured at λ= 422 nm. In regards to accuracy, sensitivity, robustness and precision, the proposed methods were validated according to ICH guidelines. Furthermore, the proposed methods were successfully applied for the assay of Eflornithine in various commercial brands of the pharmaceutical cream samples with good recovery. In addition to the current fluorometric method was confirmed to be effective in the assaying of Eflornithine in spiked plasma and urine specimens with good recovery.
α-二氟甲基鸟氨酸或依氟鸟氨酸是一种获得美国食品和药物管理局批准的药物，用于治疗昏睡病（作为小瓶剂型），也用于减少多毛症中不必要的过多面部毛发（作为乳膏剂型）。这项工作是基于依氟鸟氨酸的氨基部分与邻苯二醛/2-巯基乙醇之间的缩合相互作用，形成一种高荧光异吲哚衍生物。反应产物的荧光和共振瑞利散射（RRS）强度在加入十六烷基三甲基溴化铵后分别增加了 153%和 250%。在优化反应条件后，在 λ=337nm 后，通过 λ=429nm 对形成的异吲哚衍生物进行荧光测量。此外，在 λ=422nm 处测量到形成产物的 RRS 强度显著增加。关于准确性、灵敏度、稳健性和精密度，根据 ICH 指南对所提出的方法进行了验证。此外，所提出的方法成功地应用于各种商业品牌的药用乳膏样品中依氟鸟氨酸的测定，回收率良好。除了目前的荧光法被证实对添加血浆和尿液标本中的依氟鸟氨酸的测定有效，回收率良好。
