Single Dose Pharmacokinetics of Metoclopramide Oral Tablets Utilizing HPLC-UV Method

Author(s): Iram Kaukab, Syed Nisar Hussain Shah, Ghulam Murtaza*

Journal Name: Current Pharmaceutical Analysis

Volume 15 , Issue 7 , 2019

Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


Background: Metoclopramide is a potent dopaminergic antagonist utilized for treating gastrointestinal disorders. The aim of this study was to examine the pharmacokinetics of oral formulation of metoclopramide in the Pakistani volunteers.

Methods: This open label, single dose, pharmacokinetic study was executed in non-smoking, 12 Pakistani healthy males, treated with a single 20 mg oral tablet dose of metoclopramide on test day. Maximum plasma concentration (Cmax), time to achieve Cmax (Tmax), and area under curve (AUC0-t) of metoclopramide were determined analyzing the serial blood samples using a validated HPLC-UV method.

Results: The determined values of Cmax, Tmax, and AUC0-t of metoclopramide were 34.51 ± 4.91 ng/ml, 1.56 ± 0.18 and 273.88 ± 114.49 ng.h/ml, respectively.

Conclusion: The results reveal that the findings of Pakistani individuals are slightly different when compared with the published data of other ethnic origins.

Keywords: Metoclopramide hydrochloride, High Performance Liquid Chromatography (HPLC), pharmacokinetic study, method development, protein precipitation, validation.

Martindale’s Extra Pharmacopoeia. 30th Edn; Reynolds, J.R. (ed.);Pharmaceutical Press: London, 1993, pp. 892-894.
Hamilton, C.W.; Brogden, R.N.; Linkewich, J.A.; Romankiewicz, J.A.; Heel, R.C. Metoclopramide. An updated review of its pharmacological properties and clinical use. Drugs, 1983, 25(45), 491-494.
Rang, H.P.; Dale, M.M.; Ritter, J.M.; Moore, P.K. Pharmacology, 5th ed; Edinburgh: Churchill Livingstone, 2003.
Tonini, M.; Candura, S.M.; Messori, E.; Rizzi, C.A. Therapeutic potential of drugs with mixed 5-HT4 agonist/5-HT3 antagonist action in the control of emesis. Pharmacol. Res., 1995, 31(5), 257-260.
Fass, R.; Pieniaszek, H.J.; Thompson, J.R. Pharmacokinetic comparison of orally‐disintegrating metoclopramide with conventional metoclopramide tablet formulation in healthy volunteers. Aliment. Pharmacol. Ther., 2009, 30(3), 301-306.
Livezey, M.R.; Briggs, E.D.; Bolles, A.K.; Nagy, L.D.; Fujiwara, R.; Furge, L.L. Metoclopramide is metabolized by CYP2D6 and is a reversible inhibitor, but not inactivator, of CYP2D6. Xenobiotic, 2014, 44(4), 309-319.
Lin, J.; Ying, N.; Wu, Y.; Lin, G. Determination of imatinib and CGP74588 in rat plasma by HPLC and its application to a pharmacokinetic study. Curr. Pharm. Anal., 2018, 14(2), 133-138.
Leucuta, A.; Vlase, L.; Farcau, D.; Nanulescu, M. Pharmacokinetic interaction study between ranitidine and metoclopramide. Rom. J. Gastroenterol., 2004, 13(3), 211-214.
Fairhead, A.P.; Brooks, S.G.; Butterworth, K.R.; Mangham, B.A. An automated high-performance liquid chromatographic trace enrichment method for the determination of metoclopramide in serum and its application to a bioequivalence human volunteer study. Food Chem. Toxicol., 1989, 27(5), 341-345.
Alonso-Campero, R.; Bernardo-Escudero, R.; de Jesús Francisco-Doce, M.T.; Cortés-Fuentes, M.; Castañeda-Hernandez, G. Bioequivalence study of metoclopramide hydrochloride 10 mg tablets in healthy male volunteers. J. Bioequivalence Bioavailab., 2011, 3(10), 222-227.
Ahmed, S.; Khan, A.; Sheraz, M.A.; Bano, R.; Ahmad, I. Development and validation of a stability-indicating HPLC method for the assay of carvedilol in pure and tablet dosage forms. Curr. Pharm. Anal., 2018, 14(2), 139-152.
Razzaq, R.; Ranjha, N.M.; Rashid, R.; Rashid, Z.; Hanif, M. Determination of diltiazem HCL by reverse phase high performance liquid chromatography in rabbit plasma. Curr. Pharm. Anal., 2018, 14(2), 153-156.
Cossu, M.; Sanna, V.; Gavini, E.; Rassu, G.; Giunchedi, P. A new sensitive reversed‐phase high‐performance liquid chromatography method for the quantitative determination of metoclopramide in canine plasma. Anal. Lett., 2008, 41(5), 767-778.
Bernard, S.; Neville, K.A.; Nguyen, A.T.; Flockhart, D.A. Interethnic differences in genetic polymorphisms of CYP2D6 in the US population: clinical implications. The Oncologist, 2006, 11(2), 126-135.
Yan, M.; Chen, B.M.; Liu, X.L.; Zhu, Y.G. Determination of metoclopramide in human plasma by LC-ESI-MS and its application to bioequivalence studies. J. Chromatogr. B , 2010, 878(11), 883-887.
Lee, H.W.; Ji, H.Y.; Kim, H.Y.; Park, E.S.; Lee, K.C.; Lee, H.S. Determination of metoclopramide in human plasma using hydrophilic interaction chromatography with tandem mass spectrometry. J. Chromatogr. B ., 2009, 877(18), 1716-1720.
Wright, M.R.; Axelson, J.E.; Rurak, D.W.; McErlane, B.; McMorland, G.H.; Ongley, R.C.; Price, J.D. Linearity of metoclopramide kinetics at doses of 5‐20 mg. Br. J. Clin. Pharmacol., 1998, 26(4), 469-473.
Kalow, W. Interethnic differences in drug response. In: Kalow, W.; Meyer, U.A.; Tyndale, R.F. eds. Pharmacogenomics. Marcel Dekker, New York,. , 2001, pp. 109-134.
Burroughs, V.J.; Maxey, R.W.; Levy, R.A. Racial and ethnic differences in response to medicines: Towards individualized pharmaceutical treatment. J. Natl. Med. Assoc., 2002, 94(10)(Suppl.), 1-26.
Kim, K.; Johnson, J.A.; Derendorf, H. Differences in drug pharmacokinetics between east asians and caucasians and the role of genetic polymorphisms. J. Clin. Pharmacol., 2004, 44, 1083-1105.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2019
Published on: 14 October, 2019
Page: [703 - 709]
Pages: 7
DOI: 10.2174/1573412914666180425123202
Price: $65

Article Metrics

PDF: 43
PRC: 1