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Assessment of effect of food, gender, and intra‐subject variability in the pharmacokinetics of avitriptan
Author(s) -
Marathe P. H.,
Greene D. S.,
Lee J. S.,
Barbhaiya R. H.
Publication year - 1998
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199804)19:3<153::aid-bdd90>3.0.co;2-t
Subject(s) - pharmacokinetics , cmax , dosing , area under the curve , zoology , medicine , biology
The objectives of this study were to assess the effect of food and gender on the pharmacokinetics of avitripan. A group of 12 healthy men and 12 healthy women was administered a single 50 mg dose of avitriptan capsule under fasting conditions and 5 min after a high‐fat breakfast. The two treatments were repeated in a replicate design to assess the intra‐subject variability in the pharmacokinetics of avitriptan under fasted and fed conditions. There was a 1 week washout between treatments. Serial blood samples were collected over 24 h after dosing and analyzed by a validated HPLC method for avitriptan. The mean (SD) peak concentrations ( C max ) were 168 (86.4) ng mL −1 in the fasted condition and 57.3 (34.8) ng mL −1 in the fed condition in males and females combined. The corresponding areas under the plasma concentration curve (AUC) were 335 (162) and 185 (64.5) ng h mL −1 , respectively. Both C max and AUC were significantly reduced in the fed condition. In addition, the time to peak concentration ( t max ) was significantly delayed from a median of 45 min to 2 h after the high‐fat breakfast. The clinical significance of this food effect is unclear at the present time. There were no gender differences nor a gender by food interaction in the pharmacokinetics of avitriptan. The intra‐ and inter‐subject variability (%CV) in the C max and AUC of avitriptan in the fasted and fed conditions ranged from 10 to 60% in male and female subjects. © 1998 John Wiley & Sons, Ltd.