Pharmacokinetic Study of Lidocaine Hydrochloride Colonoscopy Glue in New Zealand Rabbits by Liquid Chromatography Tandem-Mass Spectrometry
LIU Xiao-yu1, QU Qing-mei2, XU Ling-ling1, WANG Fang1, QI Min1, CHEN Kai1*
1. Key Laboratory of Biopharmaceuticals, Shandong Academy of Pharmaceutical Sciences, Jinan 250101, China; 2. Shandong Drug and Food Vocational College, Weihai 264200, China
Abstract：OBJECTIVE To develop an LC-MS/MS method for determination of lidocaine in rabbit plasma and apply it in the pharmacokinetic study of lidocaine colonoscopy glue in New Zealand rabbits. METHODS Rabbit plasma was precipitated with acetonitrile, and the analytes were chromatographed on a Thermo Accucore C18 column (2.1 mm×50 mm,2.6 μm). The mobile phase A was methanol, and mobile phase B was water with 0.1% formic acid and 5 mmol·L-1 ammonium acetate. The flow rate was 0.5 mL·min-1. The column temperature was set at 45 ℃ and the injection volume was 2 μL. Detection was carried out by electrospray positive ionization mass spectrometry in multiple reaction monitoring (MRM) mode with m/z of 235.1/86.1. Lidocaine hydrochloride colonoscopy glue was given to six New Zealand rabbits, and plasma was collected at different time points. RESULTS The method exhibited satisfactory selectivity and sensitivity, and lidocaine exhibited good linearity in the concentration range of 2.5-5 000 ng·mL-1. The extraction recoveries ranged from 96.0% to 102.3%. Intra-and inter-run accuracies (in terms of RE) and precisions (RSD) ranged from 1.1% to 3.8% and 4.4% to 10.6%, respectively. After rectal administration of lidocaine hydrochloride colonoscopy glue, the ρmax and AUC0-t in female and male rabbits were 2 806 ng·mL-1 and 6 350 ng·h·mL-1, 2 213 ng·mL-1 and 5 384 ng·h·mL-1, respectively. CONCLUSION The absorption of lidocaine hydrochloride colonoscopy glue in rabbits is rapid and the analgesic effect can maintain for a while without drug accumulation after rectal administration.
JOHN N, LYNDA A, MARK A E. A brief history of local anesthesia[J]. Int J Head Neck Surg, 2016, 7(1): 29-32.
[2]
HOLMDAHL M H. Xylocaine (lidocaine, lignocaine), its discovery and gordh′s contribution to its clinical use[J]. Acta Anaesthesiol Scand, 1998, 42(7): 747-885.
[3]
YAO S J. Application of lidocaine hydrochloride in colonoscopy[J]. Chin J Misdiagn (中国误诊学杂志), 2011, 11(5): 1053-1053.
[4]
ZHANG M. Application of dicaine glue in colonoscopy[J]. J Qilu Nur(齐鲁护理杂志), 2005, 11(8): 1034-1034.
[5]
ANNA T, ARNE O, THOMA R E. A systematic review of lidocaine-prilocaine cream (EMLA) in the treatment of acute pain in neonates[J]. J Pediatr, 1998, 101 (2):doi:10.1542/peds.101.2.e1.
[6]
ALQUADEIB B T, ELTAHIR E K, ALAGILI M F. The oral administration of lidocaine HCl biodegradable microspheres: formulation and optimization[J]. Int J Nanomed, 2020, 15: 857-869.
[7]
MATTEO C, DOVRTELOVA G, DI CLEMENTE A, et al. HPLC-MS/MS measurement of lidocaine in rat skin and plasma. Application to study the release from medicated plaster[J]. J Chromatogr B, 2020, 1138: 1219-1242.
[8]
LIU B, DING L, XU X, et al. Ocular and systemic pharmacokinetics of lidocaine hydrochloride ophthalmic gel in rabbits after topical ocular administration[J]. Eur J Drug Metab Pharmacokinet, 2015, 40(4): 409-415.
[9]
CHIK Z, LEE T D, HOLTZ D W. Validation of high-performance liquid chromatography-mass spectrometric method for the analysis of lidocaine in human plasma[J]. J Chromatogr Sci, 2006, 44 (5): 262-265.
[10]
SANTOSH V G, ASHWINI D I. Development and validation of RP-HPLC method for simultaneous estimation of benzoxonium chloride and lidocaine hydrochloride[J]. World J Pharm Life Sci, 2017, 3: 99-102.
[11]
NADA S A, NOURUDDIN W A, HAMED M, et al. Determination of thiomesral, lidocaine and phenylepherine in their ternary mixture[J]. J Chromatogr Sep Tech, 2013, 4(8):DOI: 10.4172/2157-7064.1000199
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