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Bioavailability of intranasal metoclopramide
M J Ward1, D C Buss, J Ellershaw
1Department of Clinical Pharmacology, University of Wales College of Medicine, Liandough Hospital, South Glamorgan.
British Journal of Clinical Pharmacology
|November 1, 1989
Summary
Intranasal metoclopramide (5 mg) showed a maximum plasma concentration of 13.5 ng/mL, but absorption was not rapid. This route did not offer greater bioavailability compared to oral administration.
Area of Science:
- Pharmacokinetics
- Drug Delivery Systems
Background:
- Metoclopramide is commonly administered orally for various gastrointestinal conditions.
- Intranasal drug delivery offers potential advantages like rapid absorption and bypassing first-pass metabolism.
Purpose of the Study:
- To evaluate the pharmacokinetic profile of metoclopramide following intranasal administration.
- To compare the bioavailability and absorption rate of intranasal metoclopramide with the oral route.
Main Methods:
- Healthy volunteers received a single intranasal dose of metoclopramide (5 mg in 0.5 ml sterile water).
- Plasma concentrations of metoclopramide were measured over time.
- Key pharmacokinetic parameters including maximum plasma concentration (Cmax) and absolute bioavailability were calculated.
Main Results:
- The maximum plasma concentration (Cmax) achieved was 13.5 +/- 7.3 ng/mL.
- Absolute bioavailability was 50.5 +/- 29.5%.
- The time to reach maximum plasma concentration was 110 +/- 41 minutes, indicating relatively slow absorption.
Conclusions:
- Intranasal administration of metoclopramide does not result in rapid systemic absorption.
- The bioavailability via the intranasal route is comparable to, but not greater than, the oral route.
- Intranasal metoclopramide is not a superior alternative to oral administration for achieving faster or higher drug exposure.