The effect of orlistat, an inhibitor of dietary fat absorption, on the pharmacokinetics of beta-carotene in healthy volunteers

J Clin Pharmacol. 1996 Feb;36(2):152-9. doi: 10.1002/j.1552-4604.1996.tb04180.x.


To assess the influence of orlistat, a lipase inhibitor, on the absorption of beta-carotene, an open-label, parallel, placebo-controlled, randomized, two-way crossover study was performed in 48 healthy volunteers between the ages of 19 and 58 years. Each subject received a single oral dose of 0, 30, 60, or 120 mg beta-carotene (12 subjects per dose level) on the fourth day of treatment with orlistat (120 mg) or placebo 3 times a day for 6 days. The treatments were separated by a washout period of at least 5 weeks. Serial blood samples were collected before and at appropriate intervals after administration of beta-carotene to determine plasma concentrations of unchanged beta-carotene. Short-term (3 to 6 days) treatment with orlistat did not alter endogenous profiles of beta-carotene in plasma. When beta-carotene was given during orlistat treatment, its absorption was reduced by approximately one-third. This reduction was consistent for all three dose levels of beta-carotene studied; however, the results for the 30-mg dose level were subject to greater variability, particularly for area under the concentration-time curve (AUC). It was concluded that two thirds of a supplemental dose of beta-carotene will be absorbed during orlistat treatment; this may be sufficient to achieve physiologic levels of beta-carotene with an appropriate dose of beta-carotene, should supplementation be needed in obese patients who have developed beta-carotene deficiency during therapy with orlistat.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Absorption / drug effects
  • Administration, Oral
  • Adult
  • Antioxidants / analysis
  • Antioxidants / pharmacokinetics*
  • Cross-Over Studies
  • Dietary Fats / pharmacokinetics
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Enzyme Inhibitors / pharmacokinetics*
  • Enzyme Inhibitors / pharmacology
  • Female
  • Humans
  • Lactones / pharmacokinetics
  • Lactones / pharmacology*
  • Lipase / antagonists & inhibitors
  • Male
  • Middle Aged
  • Orlistat
  • Placebos
  • Reference Values
  • Reproducibility of Results
  • beta Carotene / blood
  • beta Carotene / pharmacokinetics*


  • Antioxidants
  • Dietary Fats
  • Enzyme Inhibitors
  • Lactones
  • Placebos
  • beta Carotene
  • Orlistat
  • Lipase