Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Port Said University, Port Said, Egypt.
Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut, Egypt.
Luminescence. 2023 Sep;38(9):1632-1638. doi: 10.1002/bio.4550. Epub 2023 Jul 18.
Avapritinib (AVP) was the first precision drug to be approved by the US Food and Drug Administration (FDA) in 2020 for patients suffering from metastatic gastrointestinal stromal tumors (GISTs) and progressive systemic mastocytosis. The analysis of AVP in pharmaceutical tablets and human plasma was then carried out using a fast, efficient, sensitive, and simple fluorimetric method using a fluorescamine reagent. The procedure is based on the interaction between fluorescamine as a fluorogenic reagent and the primary aliphatic amine moiety in AVP using borate buffer solution at pH 8.8. The produced fluorescence was measured at 465 nm (Excitation at 395 nm). The calibration graph's linearity range was discovered to be 45.00-500.0 ng mL . Utilizing the International Council for Harmonization (ICH) and US-FDA recommendations, the research technique was validated and bioanalytically validated. The proposed approach was effectively employed for determining the stated pharmaceuticals in plasma with a high percentage of recovery ranging from 96.87 to 98.09 and pharmaceutical formulations with a percentage of recovery equal to 102.11% ± 1.05%. In addition, the study was extended to a pharmacokinetic study of AVP with 20 human volunteers as a step for AVP management in therapeutic cancer centers.
阿伐普利替尼（AVP）是 2020 年美国食品和药物管理局（FDA）批准的首款用于治疗转移性胃肠道间质瘤（GIST）和进行性系统性肥大细胞增多症的精准药物。然后，使用荧光胺试剂，采用快速、高效、灵敏和简单的荧光法对药物片剂和人血浆中的 AVP 进行了分析。该方法基于荧光胺作为荧光试剂与 AVP 中伯酸盐缓冲溶液在 pH 8.8 下的伯胺部分的相互作用。在 465nm（激发波长 395nm）处测量产生的荧光。发现校准曲线的线性范围为 45.00-500.0ng·mL 。利用国际协调会议（ICH）和美国 FDA 的建议，对研究技术进行了验证和生物分析验证。该方法可有效用于测定血浆中的规定药物，回收率高达 96.87%至 98.09%，药物制剂的回收率等于 102.11%±1.05%。此外，该研究还扩展到了 20 名人类志愿者的 AVP 药代动力学研究，作为治疗癌症中心 AVP 管理的一个步骤。
