I Curso de Pós-Graduação Lato Sensu Análises Clínicas e Toxicológicas
http://www.ufpe.br/posact/
Determination and pharmacokinetics research of ciprofloxacin in human
plasma
Rocha,
1
R.C. ;
Alves,
2
A.Q. ;
4
C.J. ;
3
A.J.S. ;
Alves,
Góes,
1
Neto, J.L.; Alves, A.J.
Aquino,
3
T.M. ;
Carvalho
1. Departamento de Ciências Farmacêuticas. Universidade Federal de Pernambuco (UFPE), Brazil, 2. Faculdade Pernambucana de
Saúde, Brazil, 3. Departamento de Antibióticos. UFPE, Brazil, 4. Maxiclínica Médica Ltda, 5. Hospital Memorial Guararapes
Background:
Ciprofloxacin, 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperamzinyl)-3-quinolone
carboxylic
acid,
is
a
fluoroquinolone carboxylic acid derivative with broad
antibacterial activity against Gram-positive and Gramnegative bacteria, including those resistant to amino
glycosides and β-lactam antibiotics.
The chemical structure is as follows:
Means of plasma ciprofloxacin concentrations at various time
intervals are:
Time (hr)
Conc. (µg/ml)
Objectives:
To determine the plasma ciprofloxacin concentrations
by high-performance liquid chromatography (HPLC) and
to compare the pharmacokinetics parameters (PKP)
calculated by two softwares.
Methodology:
Nine healthy and nonsmoking volunteers were selected
and the study was conducted according with the current
revision of the Declaration of Helsinki. Each volunteer
signed an informed consent document before entering the
study. Ethical permission was acquired, to approve the
protocol and consent form of this study from the Ethical
Review Committee of Hospital Memorial Guararapes.
Blood samples were drawn before dosing and at 0.50,
0.75, 1.0, 1.25, 1.5, 2.0, 3.0 4.0, 6.0, 8.0, 12.0, 24.0, and
36.0 h after ciprofloxacin 500 mg tablets administration.
Serum drug concentrations were determined by HPLC
assay using fluorescence detection using the internal
standard enoxacin.
PKP were determined by Pharmkit program and
BrOffice calc in Kurumin Linux software.
Results:
The Mean of plasma concentrations-time profile of
ciprofloxacin is showed as follows:
0
0
0.50 0.75
1.00
1.032 1.685 2.026
1.25
1.50
2
2.105 1.949 1.741
Time (hr)
3
4
6
8
12
24
Conc. (µg/ml) 1.062 0.780 0.458 0.3288 0.178 0.035
36
0
The pharmacokinetic parameters of each subject were
individually calculated by the Pharmkit program and BrOffice
calc in Kurumin Linux software. Mean (Ttest) of area under
the serum concentration-time curve (AUC0-36), area under the
serum concentration-time curve extrapolated to infinity
(AUC0-∞), serum elimination half-life (t1/2), and elimination rate
constant (kel), were :
AUC0-t
AUC0-∞
(hr.µg/mL) (hr. µg/mL)
Pharmkit
BrOffice calc
Ttest(%)
9.860
8.992
48.34
10.316
9.536
53.03
t½
(hr)
kel
(hr-1)
3.603 0.204
3.571 0.207
93.58 91.61
Conclusions :
There was no significant difference between the means of all
PKP (Ttest greater than 5%). Pharmacokinetic parameters
can be calculated by both softwares.
Reference:
Azad, M.A.K.; Ullah, A.; Latif, A.H.M.M.; Hasnat, Abu. Bioequivalence and
Pharmacokinetic Study of Two Oral Formulations ofCiprofloxacin Tablets in
Healthy. The Journal of Applied Research. 7(2): 150-157, 2007
E-mail: [email protected]
I LUSO-BRAZILIAN CONGRESS OF THE EXPERIMENTAL PATHOLOGY
(XI International Symposium on Experimental Techniques) - Recife, 10 à 12/11/2011