Verma Saurabh, Goand Umesh K, Garg Richa, Husain Athar, Katekar Roshan A, Riyazuddin Mohammed, Dadge Shailesh, Gayen Jiaur R
Division of Pharmaceutics & Pharmacokinetics, Council of Scientific & Industrial Research - Central Drug Research Institute, Lucknow, 226031, India.
Academy of Scientific & Innovative Research (AcSIR), Ghaziabad, 201002, India.
Bioanalysis. 2023 Jan;15(2):83-98. doi: 10.4155/bio-2022-0239. Epub 2023 Mar 14.
Raspberry ketone (RK), derived from red raspberry fruit (, family Rosaceae), is a reported potent antiobesity agent. This study aims to investigate method development, validation, and and pharmacokinetics in rats. LC-MS/MS was used to conduct method development, validation, stability, and oral PK samples of RK in plasma analyses. RK was highly soluble in Tris buffer and stable in gastrointestinal fluids as well as plasma. Rat liver microsomal stability of RK in phase I and II studies was 84.96 ± 2.39 and 69.98 ± 8.69%, respectively, after 60 min. Intestinal permeability was 4.39 ± 1.37 × 10 cm/s. Maximal concentration was 1591.02 ± 64.76 ng/ml, which was achieved after 1 h (time to maximal concentration), and absolute oral bioavailability was 86.28%. Pharmacokinetic data serve as a keystone for preclinical and clinical adjuvant therapy.
覆盆子酮（RK）源自红树莓果实（蔷薇科），据报道是一种有效的抗肥胖剂。本研究旨在探讨大鼠体内的方法开发、验证以及药代动力学。采用液相色谱-串联质谱法（LC-MS/MS）进行RK在血浆分析中的方法开发、验证、稳定性和口服药代动力学样品分析。RK在Tris缓冲液中高度可溶，在胃肠液和血浆中稳定。在I期和II期研究中，RK在大鼠肝微粒体中的稳定性在60分钟后分别为84.96±2.39%和69.98±8.69%。肠道通透性为4.39±1.37×10 cm/s。最大浓度为1591.02±64.76 ng/ml，在1小时后达到（达峰时间），绝对口服生物利用度为86.28%。药代动力学数据是临床前和临床辅助治疗的关键。
