Published in:
01-10-2014 | Short Communication
Pharmacokinetics of Zolpidem from Sublingual Zolpidem Tartrate Tablets In Healthy Elderly Versus Non-Elderly Subjects
Published in: Drugs & Aging | Issue 10/2014
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Background
Pharmacokinetic parameters of sedative–hypnotic medications can be influenced by age and gender.
Objective
This study analyzed pharmacokinetic parameters of zolpidem, formulated as a sublingual zolpidem tartrate tablet (ZST; Intermezzo®), in healthy elderly males and females (mean age 72 years) and in non-elderly males and females (34 years).
Methods
This was a randomized, single-dose, open-label, two-way crossover study evaluating pharmacokinetic parameters of 1.75 and 3.5 mg dosages of ZST in elderly subjects (n = 22), and 3.5 mg dosages of ZST in non-elderly subjects (n = 24). Main outcome measures were pharmacokinetic parameters, including area under the plasma concentration–time curve (AUC), maximum observed concentration (C
max), time to reach C
max (T
max), elimination half-life (T
½), and apparent oral clearance (CL/F).
Results
Dose proportionality in zolpidem exposure was maintained between 1.75 and 3.5 mg doses for both elderly females and males. With administration of the 3.5 mg dose of ZST to elderly and non-elderly subjects, significantly higher systemic exposure was seen in elderly females (C
max +44.6 %, P < 0.01; AUC +40.4 %) compared with non-elderly females. However, systemic exposure was only modestly higher in elderly males compared with non-elderly males. Greater exposure was seen in elderly females compared to males (C
max +46.8 %, P < 0.01; AUC +31.4 %). In this study, exposure between non-elderly females and males was equivalent. Changes in T
½ and T
max values were not observed, with no significant age effect on oral clearance. There were no apparent differences in tolerability among age and gender groups.
Conclusion
Elderly individuals were found to have higher C
max and AUC values compared with non-elderly subjects. C
max and AUC were greater in elderly women compared with elderly men.