Premium
The Influence of Orlistat on the Pharmacokinetics and Pharmacodynamics of Glyburide in Healthy Volunteers
Author(s) -
Zhi J.,
Melia A. T.,
KossTwardy S. G.,
Min B.,
Guerciolini R.,
Freundlich N. L.,
Milla G.,
Patel I. H.
Publication year - 1995
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1995.tb04098.x
Subject(s) - pharmacokinetics , orlistat , medicine , crossover study , placebo , pharmacodynamics , pharmacology , obesity , weight loss , alternative medicine , pathology
To assess the influence of orlistat on the pharmacokinetics and pharmacodynamics (the blood glucose‐lowering effect) of glyburide, an open‐label, placebo‐controlled, randomized, two‐way crossover study was done in 12 healthy male volunteers. Each subject received single 5‐mg oral doses of glyburide (Micronase; The Upjohn Company, Kalamazoo, MI) on the fifth day of treatment with placebo (treatment A) and 80‐mg orlistat (treatment B) three times a day for 4 1/3 days; the two treatments were separated by a five‐day washout period. Serial blood samples were collected before and at appropriate intervals after each glyburide dose to determine plasma concentrations and blood glucose levels. Values of C max and AUC of glyburide showed an equality of the two treatments by the analysis of variance. There was an apparent correlation between blood glucose level and the logarithm of plasma glyburide concentration; this relationship appeared to not be altered when glyburide was administered with orlistat. In conclusion, orlistat administered at doses of 80‐mg three times daily does not significantly alter the pharmacokinetics and blood glucose‐lowering effect of a single 5‐mg oral dose of glyburide in healthy volunteers.