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Drug Delivery: Enteral Route

The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
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Updated: Jul 26, 2026

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals
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Grapefruit juice increases oral nimodipine bioavailability

U Fuhr1, A Maier-Brüggemann, H Blume

  • 1Institute for Pharmacology, Clinical Pharmacology, Universität zu Köln, Germany.

International Journal of Clinical Pharmacology and Therapeutics
|April 30, 1998
PubMed
Summary

Grapefruit juice significantly increased the bioavailability of nimodipine, a dihydropyridine calcium channel blocker. This interaction means nimodipine should not be taken with grapefruit juice to avoid potential adverse effects.

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Area of Science:

  • Pharmacology
  • Drug Interactions
  • Clinical Pharmacokinetics

Background:

  • Dihydropyridine calcium channel blockers' oral bioavailability is often increased by grapefruit juice.
  • Naringin in grapefruit juice is a known inhibitor of CYP3A4, a key enzyme in drug metabolism.

Purpose of the Study:

  • To investigate the pharmacokinetic interaction between grapefruit juice and nimodipine.
  • To determine the effect of grapefruit juice on nimodipine bioavailability and its metabolites.

Main Methods:

  • A randomized crossover study involving eight healthy young men.
  • Nimodipine was administered with water or grapefruit juice, with plasma concentrations measured up to 24 hours.
  • Pharmacokinetic parameters were estimated using model-independent analysis.

Main Results:

  • Grapefruit juice increased nimodipine's area under the curve (AUC) by 51% and Cmax by 24%.
  • The 90% confidence intervals for AUC (114%-200%) and Cmax (0.76-2.01) indicated a significant interaction.
  • Metabolite AUC to parent drug AUC ratios were reduced, suggesting altered metabolism.

Conclusions:

  • Grapefruit juice significantly alters nimodipine pharmacokinetics, increasing its exposure.
  • A relevant interaction between grapefruit juice and nimodipine was confirmed.
  • Nimodipine should not be co-administered with grapefruit juice due to increased bioavailability and potential for enhanced effects.