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Drug Res (Stuttg) 2014; 64(10): 537-540
DOI: 10.1055/s-0033-1363250
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Effect of Dimeticone and Pepsin on the Bioavailability of Metoclopramide in Healthy Volunteers

D. F. do Nascimento
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
,
A. L. A. e Silva Leite
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
,
R. A. de Moraes
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
,
G. C. Camarão
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
,
F. A. F. Bezerra
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
,
M. O. de Moraes
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
,
M. E. A. de Moraes
1   Clinical Pharmacology Unit – Department of Physiology and Pharmacology, Federal University of Ceará, Brazil
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Weitere Informationen

Publikationsverlauf

received 09. September 2013

accepted 27. November 2013

Publikationsdatum:
06. Februar 2014 (online)

Auch verfügbar auf
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Abstract

Objective:

To assess the effect of dimeticone and pepsin on the bioavailability of metoclopramide (CAS 7232-21-5) in healthy volunteers.

Methods:

The study was conducted using a randomized, open, 2-period crossover design. The volunteers received single administration of 7-mg conventional metoclopramide capsule and a formulation containing metoclopramide (7 mg) plus dimeticone (40 mg) and pepsin (50 mg), with a 7-day interval between treatments. Serial blood samples were collected before dosing and during 24 h post-treatment. Plasma metoclopramide concentrations were analyzed by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS). The pharmacokinetics parameters AUClast and Cmax were obtained from the metoclopramide plasma concentration vs. time curves.

Results:

Metoclopramide’s association was bioequivalent to conventional capsule; 90% CIs for geometric mean treatment ratios of Cmax [108.0% (90% CI, 100.4–116.3%)], AUClast [103.3% (90% CI, 99.5–107.4%)] were within the predefined range. The metoclopramide formulations were well tolerated at the administered doses and no significant adverse reactions were observed. Thus, these results confirm the good bioavailability of metoclopramide in the new formulation and rule out any impaired absorption when the drugs are formulated in combination.

Key words

metoclopramide - bioavailability - pharmacokinetic - LC-MS/MS - clinical trial
 

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