Development of a sufficient
design for estimation
of fluconazole
pharmacokinetics in people
with HIV infection
Juliana F. Roos, Carl M. J. Kirkpatrick, Susan E. Tett,
Andrew J. McLachlan
1
& Stephen B. Duffull
2
School of Pharmacy, University of Queensland, Brisbane and
1
Faculty of Pharmacy, University of
Sydney, Sydney, Australia, and
2
School of Pharmacy, University of Otago, Dunedin, Otago, New
Zealand
Correspondence
Carl Kirkpatrick, School of Pharmacy,
University of Queensland, Brisbane, QLD
4072, Australia.
Tel: + 61 7 3365 3227
Fax: + 61 7 3365 1688
E-mail: c.kirkpatrick@pharmacy.uq.edu.au
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Keywords
fluconazole, population
pharmacokinetics, optimal design, HIV
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Received
20 October 2007
Accepted
10 June 2008
Published OnlineEarly
12 August 2008
WHAT IS ALREADY KNOWN ABOUT
THIS SUBJECT
• Optimal design is being employed more
frequently to help reduce the number of
samples taken per patient, the number of
patients and number of doses to be given
within a study.
• In doing this the economic and patient
resources required to conduct a population
pharmacokinetic or
pharmacokinetic–pharmacodynamic study
are reduced.
WHAT THIS STUDY ADDS
• This is the first time that healthy volunteer
data (e.g. from Phase I) have been used to
develop an optimal design that is to be
conducted in a population with different
characteristics due to disease (e.g. Phase II).
AIMS
To assess an optimal design that is sufficient to gain precise estimates
of the pharmacokinetic (PK) parameters for fluconazole in people with
HIV infection.
METHODS
Two studies were identified, the first in healthy volunteers and the
second in HIV patients.The investigators (J.F.R. and S.B.D.) were blinded
to the second study results. The healthy volunteer study was modelled
and a design was found to estimate the PK parameters. The design was
evaluated by comparison of the standard errors of the parameters and
the predictive performance of the optimal design. The predictive
performance was assessed by comparing model predictions against
observed concentrations for two models. The first model, termed
‘sufficient design’,was developed from data extracted from the HIV
study that corresponded to the optimal design. The second model,
termed‘HIV outcome model’, by modelling all the data from the HIV
study.
RESULTS
An optimal design HIV study was developed which had considerably
fewer blood samples and dosing arms compared with the actual HIV
study. The optimized design performed as well as the actual HIV study
in terms of parameter precision. The performance of the design,
described as the precision (mg l
-1
)
2
(95% confidence interval) of the
predicted concentrations to the actual concentrations for the ‘sufficient
design’ and ‘HIV outcome model’ models were: 0.63 (0.40, 0.87) and 0.56
(0.32, 0.79), respectively.
CONCLUSION
This study demonstrates how data from healthy volunteers can be
utilized via optimal design methodology to design a successful study
in the target population.
British Journal of Clinical
Pharmacology
DOI:10.1111/j.1365-2125.2008.03247.x
Br J Clin Pharmacol / 66:4 / 455–466 / 455 © 2008 The Authors
Journal compilation © 2008 Blackwell Publishing Ltd