Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, 42511, Egypt.
Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University-Assiut Branch, Assiut, 71524, Egypt.
J Fluoresc. 2022 Sep;32(5):1725-1732. doi: 10.1007/s10895-022-02979-2. Epub 2022 Jun 7.
Vonoprazan (VON) has been approved recently via US-FDA in 2015 as the first in class of potassium competitive acid blocker group. VON is used for management of GIT ulcer, reflux esophagitis and for eradication of Helicobacter pylori. So, the first spectrofluorimetric method was developed for estimation of VON in real human plasma and content uniformity test. The fluorimetric methodology based on reaction of secondary amine group in VON with benzofurazan (0.05% w/v NBD-Cl) reagent as nucleophilic substitution reaction in alkaline medium (0.1 M borate buffer pH 8.2) to produce highly fluorescent product measure at 530 nm after excitation at 465 nm. The linear calibration range was found 15 to 200 ng mL with lower limit of quantitation (LOQ) equal to 8.57 ng mL. The method was successfully applied for estimation of VON in pharmacokinetic (PK) and content uniformity studies. The maximum plasma concentration was found to be (C) 71.03 ng mL after maximum time (t) equal to 1.5 ± 0.15 h. The presented strategy also applied to ensure concentration of drug in each tablet using content uniformity test with high percent of recovery 100.05 ± 0.66. The proposed method was established for clinical laboratories and therapeutic drug monitoring studies.
伏诺拉生（VON）于 2015 年经美国食品药品监督管理局（US-FDA）批准，为首个钾离子竞争性酸阻滞剂类药物。VON 用于治疗胃肠道溃疡、反流性食管炎和幽门螺杆菌的根除。因此，建立了首个用于测定人血浆中伏诺拉生浓度和含量均匀度的分光荧光法。该荧光法基于伏诺拉生仲胺基团与苯并呋咱（0.05% w/v NBD-Cl）试剂发生亲核取代反应，在碱性介质（0.1 M 硼酸盐缓冲液，pH 8.2）中生成强荧光产物，在 465nm 激发光下于 530nm 处测定荧光强度。线性校准范围为 15-200ng/mL，定量下限（LOQ）为 8.57ng/mL。该方法成功应用于伏诺拉生的药代动力学（PK）和含量均匀度研究。最大血浆浓度（C）在最大时间（t）为 1.5±0.15h 时达到 71.03ng/mL。该策略还用于通过含量均匀度试验确保每片药物的浓度，回收率高达 100.05±0.66%。该方法已建立用于临床实验室和治疗药物监测研究。
