• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
PAN Shiyuan, ZOU Qiaogen, HAN Mo, GAO Qianqian. Determination of imidafenacin in human plasma by UPLC-MS/MS and its bioequivalence[J]. Journal of China Pharmaceutical University, 2019, 50(5): 579-584. DOI: 10.11665/j.issn.1000-5048.20190511
Citation: PAN Shiyuan, ZOU Qiaogen, HAN Mo, GAO Qianqian. Determination of imidafenacin in human plasma by UPLC-MS/MS and its bioequivalence[J]. Journal of China Pharmaceutical University, 2019, 50(5): 579-584. DOI: 10.11665/j.issn.1000-5048.20190511
shu

Determination of imidafenacin in human plasma by UPLC-MS/MS and its bioequivalence

More Information
    Graphical Abstract
    • Abstract
  • A sensitive and selective method for the determination of imidafenacin in human plasma using liquid chromatography combined with mass spectrometry was established, and was applied to the pharmacokinetic and bioequivalence studies of imidafenacin in healthy Chinese volunteers. After the liquid-liquid extraction pretreatment, samples were separated by UPLC on BEH C8(2. 1 mm×50 mm, 1. 7 μm)column with mobile phase 2 mmol/L ammonium acetate solution with 0. 2% acetic acid and acetonitrile using gradient elution. The mass instrument was operated in the positive ion mode, and the monitored transition was set at m/z 320. 2→238. 1 and m/z 330. 2→248. 2 for imidafenacin and IS(imidafenacin-d10), respectively. In the single-dose, double cycle, self-crossover clinical trial, 24 healthy Chinese volunteers received 0. 1 mg reference or test imidafenacin tablet orally under fasting condition. Drug concentration in plasma was determined by this method and the pharmacokinetic parameters were calculated by DAS 3. 2. 8 software. The linear range of the analysis method is 10. 0 pg/mL to 1 000 pg/mL. The extraction recoveries of the low medium and high concentration samples were 84. 0%, 88. 0% and 90. 0%, respectively. The matrix effects of low medium and high concentration samples were 105%, 100% and 101%, respectively. The pharmacokinetic parameters of imidafenacin for the reference and test tablets were as follows: cmax 524. 8 pg/mL vs 612. 6 pg/mL, tmax 1. 250 h vs 1. 063 h, AUC0-∞ 2 229 pg ·h/mL vs 2 466 pg ·h/mL. The reference and test tablets of imidafenacin were bioequivalent. This method proved to be rapid and accurate for the pharmacokinetic and bioequivalence studies of imidafenacin.
    • FullText(HTML)
    • References (16)
  • [1]
    Guo H,Zhang YQ.New drug for overactive bladder:imidafenacin[J].Qilu Pharm Aff(齐鲁药事),2008,27(5):317-318.
    [2]
    Zhang Y.Synthesis research progress of imidafenacin[J].J Chem Ind & Eng(化学工业与工程技术),2004,35(3):59-61.
    [3]
    Liu SH. Clinical characteristics of bladder overactivity and its advances in drug therapy[J].J Med Theory Pract(医学理论与实践),2018,31(5):653-654.
    [4]
    Zhang Y.Research progress of imidafenacin[J].Zhejiang Chem Ind(浙江化工),2015,46(2):14-17.
    [5]
    Lee KS,Park B,Kim JH,et al.A randomised,double-blind,parallel design,multi-institutional,non-inferiority phase IV trial of imidafenacin versus fesoterodine for overactive bladder[J].Int J Clin Pract,2013,67(12):1317-1326.
    [6]
    Sakakibara R,Hamano H,Yagi H.Cognitive safety and overall tolerability of imidafenacin in clinical use:a long-term,open-label,post-marketing surveillance study[J].Lower Urinary Tract Symptoms,2014,6(3):138-144.
    [7]
    Masumori N.Long-term safety,efficacy,and tolerability of imidafenacin in the treatment of overactive bladder:a review of the Japanese literature[J].Patient Prefer Adherence,2013,7:111-120.
    [8]
    Uchida H,Otsuka M.Quantitative analysis of pseudopolymorphic transformation of imidafenacin by application of a novel combination of near-infrared spectroscopy and a humidity-controlled 96-well plate[J].J Pharm Pharmacol,2011,63(7):911-917.
    [9]
    Ohmori S,Miura M,Toriumi C,et al.Absorption,metabolism,and excretion of [14C]imidafenacin,a new compound for treatment of overactive bladder,after oral administration to healthy male subjects[J].Drug Metab Dispos,2007,35(9):1624-1633.
    [10]
    Otsuka A,Kageyama S,Suzuki T,et al.Comparison of mirabegron and imidafenacin for efficacy and safety in Japanese female patients with overactive bladder:a randomized controlled trial(COMFORT study)[J].Int J Urol,2016,23(12):1016-1023.
    [11]
    Nakade S,Ohno T,Nakayama K,et al.No effect of imidafenacin,a novel antimuscarinic drug,on digoxin pharmacokinetics in healthy subjects[J].Drug Metab Pharmacokinet,2008,23(2):95-100.
    [12]
    Ohno T,Nakade S,Nakayama K,et al.Absolute bioavailability of imidafenacin after oral administration to healthy subjects[J].Br J Clin Pharmacol,2008,65(2):197-202.
    [13]
    Hu YY,Shen L,Wang LP,et al.A liquid chromatography-tandem mass spectrometry method for the quantitation of imidafenacin in human plasma:application to a clinical pharmacokinetic study[J].Anal Methods,2016,8(38):6903-6908.
    [14]
    Hasegawa C,Ohno T,Nakade S,et al.Population pharmacokinetics and exposure-response relationship of a muscarinic receptor antagonist,imidafenacin[J].Drug Metab Pharmacokinet,2013,28(3):203-212.
    [15]
    Xiao YY,Ma PC,Wang Y,et al.Determination of 8′-hydroxy-dihydroergocryptine in human plasma by LC-MS/MS and its application to a bioequivalence evaluation[J].J China Pharm Univ(中国药科大学学报),2012,43(2):177-181.
    [16]
    Liang F,Li D,Wang RB,et al.Pharmacokinetics and absolute bioavailability of isoschaftoside in rat by LC-MS/MS[J].J China Pharm Univ(中国药科大学学报),2019,50(1):75-80.
    • Related Articles

  • Related Articles

    [1]XU Yuantao, WANG Jundong, GUAN Li, ZHAO Ning, LI Weize. Synthesis and antidiabetic activity evaluation of benzopyrimidine derivatives[J]. Journal of China Pharmaceutical University, 2023, 54(5): 569-576. DOI: 10.11665/j.issn.1000-5048.2023041701
    [2]MEI Yinliu, WU Jie. Application of nanoparticles in wound healing of diabetes[J]. Journal of China Pharmaceutical University, 2022, 53(1): 25-31. DOI: 10.11665/j.issn.1000-5048.20220104
    [3]TAO Yingjun, WU Jie, LIU Chang. Application of proteomics in diabetes and its complications[J]. Journal of China Pharmaceutical University, 2020, 51(3): 368-373. DOI: 10.11665/j.issn.1000-5048.20200315
    [4]LI Yongrong, CHENG Tao, WANG Yongsheng, LI Qin, GAO Bo, HE Yun, BAI Yu. Effect of extract of selenium-enriched Astragalus membranaceus on insulin resistance in streptozotocin-induced diabetic rats[J]. Journal of China Pharmaceutical University, 2018, 49(6): 739-745. DOI: 10.11665/j.issn.1000-5048.20180616
    [5]XU Zhimeng, ZHU Jingjing, JIANG Zhenzhou, LOU Fengchang, WANG Tao. Hypoglycemic effects of terpenes from Fructus Corni on db/db diabetic mice[J]. Journal of China Pharmaceutical University, 2016, 47(3): 337-341. DOI: 10.11665/j.issn.1000-5048.20160315
    [6]HU Mengyue, LIU Can, ZHANG Mian, HU Nan, LIU Li, LIU Xiaodong. Alteration of cytochrome P450s activity under diabetic conditions and its impact on the development of diabetes mellitus[J]. Journal of China Pharmaceutical University, 2014, 45(2): 153-160. DOI: 10.11665/j.issn.1000-5048.20140204
    [7]WANG Xin-ting, ZHANG Mian, GUO Hai-fang, LIU Can, HU Nan, LIU Li, LIU Xiao-dong. Effect and mechanism of atorvastatin on blood glucose of mild diabetic rats[J]. Journal of China Pharmaceutical University, 2012, 43(5): 453-459.
    [8]Effects of Melatonin on the Immune Functions of Diabetic Rats Combined with Injury-induced Stress[J]. Journal of China Pharmaceutical University, 2004, (4): 71-74.
    [9]PREVENTION AND TREATMENT OF ALLOXAN-INDUCED DIABETES IN MICE BY POLYSACCHARIDES ISOLATED RESPECTIVELY FROM BOTH TREMELLA FUCIFORMIS AND AURICULARIA A URICULA[J]. Journal of China Pharmaceutical University, 1989, (3): 181-183.
    [10]PREVENTION AND TREATMENT OF ALLOXAN-INDUCED DIABETES IN MICE BY POLYSACCHARIDES FROM SPORE OF TREMELLA FUCIFORMIS BERK[J]. Journal of China Pharmaceutical University, 1988, (4): 303-304.

  • Cited by

    Periodical cited type(7)

    1. 刘艳，温田田，孙野，陈庆山，张丽莉，匡海学，杨炳友. 白鲜皮化学成分研究. 中成药. 2025(03): 812-821 .
    2. 陈禹竹，徐晓敏，刘树民，卢芳. 白鲜皮及其有效成分的药理作用研究进展. 药物评价研究. 2024(02): 409-418 .
    3. 刘新月，陈乐乐，孙鹏，展照双，王加锋. 白鲜皮化学成分、药理作用和毒性研究进展及质量标志物预测分析. 中国新药杂志. 2023(08): 799-805 .
    4. 牛晨冬，郭丽娜，张金玲，卢宜然，王琳琳，李宗锴. 白鲜属植物化学成分与药理作用研究进展. 中成药. 2022(04): 1231-1238 .
    5. 葛翎，路露，周谦，张秋生，蔡波，黄晓德，张峰伦，钱雪，李海涛，陈斌，曹鹏. 马齿苋醇提物体外生物学活性测定. 中国野生植物资源. 2021(04): 8-14+21 .
    6. 梁郭智，孙淑英. 白鲜研究进展. 时珍国医国药. 2020(02): 408-411 .
    7. 胡玉恒，孙捷，杨洁，王晓静. 3-(4′-苯甲酰基氨基-苯基)-香豆素衍生物的合成及体外降血糖活性. 中国药科大学学报. 2019(02): 168-174 . 本站查看

    Other cited types(4)

Catalog

    Get Citation
    PDF
    XML
    Article views (630) PDF downloads (1012) Cited by(11)
    Turn off MathJax
    Article Contents
    Abstract
    References
    Related Articles

    Copyright © Journal of China Pharmaceutical University苏ICP备12050101号-2

    Address：24 Tongjia Lane, Nanjing City, Jiangsu Province （210009）Tel: 025-83271566E-mail: xuebao@cpu.edu.cn

    Supported by: Beijing Renhe Information Technology Co., Ltd.  Baidu Analytics

    Total visits：365847

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return