99mTc-labeled antibiotics have an important role in the development of new radiopharmaceuticals for infection imaging. [99mTc]Tc-kanamycin was one of the radiolabeled antibiotics that was used for diagnosis of bacterial deep site infection. The pharmacokinetics study of [99mTc]Tc-kanamycin may be altered by a variety of drugs, disease states, and medical procedures which can have a significant clinical impact on safety, scan interpretation, and diagnostic imaging accuracy. This study was conducted to identify an interaction between several antibiotics with [99mTc]Tc-kanamycin based on the pharmacokinetic parameters. In vivo studies were conducted on eighteen male BALB/c mice and divided into six groups. Each group of mice was treated with kanamycin, ciprofloxacin, amoxicillin, levofloxacin, and cefotaxime. Two hours post antibiotics administration, a single dose of 25µCi/mL [99mTc]Tc–kanamycin was administered intravenously. Blood samples was collected from the coccygeal vein in an interval of 5 minutes to 24 hours. Then the radioactivity in the blood samples was measured using the Automatic Gamma Counter. The pharmacokinetic parameters showed that administration of kanamycin, ciprofloxacin, and amoxicillin on blood clearance of 99mTc-kanamycin had no significant difference indicated by one way ANOVA analysis (p>0.05). The administration of levofloxacin caused pharmacokinetic interactions significantly different (p<0.05) with t1/2 β 20.11±0.92 h and increased Cmax 10.86±3.05 and AUC0-inf 20.04 ± 5.27. Administration of cefotaxime increased the Cmax and AUC0-inf values, which were respectively 11.47±1.98, and 23.90±2.85. Pharmacokinetics studies showed that antibiotics administrations before [99mTc]Tc-kanamycin influences the pharmacokinetic profile of [99mTc]Tc-kanamycin. The absorption rate was increased and t1/2β of [99mTc]Tc-kanamycin was prolonged for levofloxacin and cefotaxime groups. While administration of antibiotics kanamycin, ciprofloxacin, and amoxicillin did not change the pharmacokinetic parameters.

1.
F. Y.
Lambrecht
, “
Evaluation of Tc-labeled antibiotics for infection detection
,” pp.
1
6
,
2011
.
2.
A.
Lupetti
,
M. M.
Welling
,
E. K. J.
Pauwels
, and
P. H.
Nibbering
, “
Review Radiolabelled antimicrobial peptides for infection detection
,” vol.
3
, no. April, pp.
223
229
,
2003
.
3.
A. H. S.
Katamihardja
,
J.
Malamitsi
,
H. M.
Moustafa
,
V. E.
Soroa
,
F. X.
Sundram
, and
A. K.
Padhy
, “
Imaging bacterial infection with (Infecton
),” pp.
817
823
,
2002
.
4.
Ö.
Uyaro
,
H.
Demiro
,
G.
Topal
, and
Y.
Parlak
, “
CHEMISTRY Radiosynthesis and biodistribution of 99m Tc-Sulfamethoxazole : a novel molecule for in-vivo infection imaging
,” pp.
3149
3157
,
2017
.
5.
A. A.
Martı
, “
A Portable Database of Adverse Reactions and Drug
,” vol.
41
, no.
3
, pp.
212
216
,
2013
.
6.
R.
Santos-oliveira
, “
Pitfalls With Radiopharmaceuticals
,” vol.
342
, no.
1
, pp.
50
53
,
2011
.
7.
S.
Vallabhajosula
,
R. P.
Killeen
, and
J. R.
Osborne
, “
Altered Biodistribution of Radiopharmaceuticals : Role of Radiochemical / Pharmaceutical Purity, Physiological, and Pharmacologic Factors
,”
Semin. Nucl. Med.
, vol.
40
, no.
4
, pp.
220
241
,
2010
.
8.
J. W.
Park
 et al., “
biosynthesis allows antibiotic manipulation
,”
Nat. Chem. Biol.
, vol.
7
, no.
11
, pp.
843
852
,
2011
.
9.
S.
Roohi
,
A.
Mushtaq
,
M.
Jehangir
, and
S. A.
Malik
, “
Synthesis , quality control and biodistribution of 99m Tc-Kanamycin
,” vol.
267
, no.
3
, pp.
561
566
,
2006
.
10.
T. H. A.
Wibawa
,
A.
Kurniawan
, and
I.
Daruwati
, “
Pharmacokinetics interaction study of 99m Tc-glutathione radiopharmaceutical with doxorubicin in mice ( mus musculus ) Pharmacokinetics interaction study of 99m Tc-glutathione radiopharmaceutical with doxorubicin in mice ( mus musculus
),”
2020
.
11.
A.
Kurniawan
,
T.
Hafiz
,
A.
Wibawa
,
I.
Daruwati
, and
A.
Kurniawan
, “
Pharmacokinetics Interaction and Biodistribution of 5 Fluorouracil with Radiopharmaceuticals 99m Tc-Glutathione for Cancer Diagnostic in Mice Cancer Model
,” vol.
30
, no.
2
, pp.
91
97
,
2019
.
12.
E. M.
Widyasari
,
M. E.
Sriyani
,
T. H. A.
Wibawa
, and
W.
Nuraeni
, “
Preparation of 99m Tc-Kanamycin using a Direct Labeling Method
,” vol.
41
, no.
3
, pp.
131
137
,
2015
.
13.
Y.
Zhang
,
M.
Huo
,
J.
Zhou
, and
S.
Xie
, “
PKSolver: An add-in program for pharmacokinetic and pharmacodynamic data analysis in Microsoft Excel
,”
Comput. Methods Programs Biomed.
, vol.
99
, no.
3
, pp.
306
314
,
2010
.
14.
C.
Maioli
,
G.
Lucignani
,
A.
Strinchini
,
L.
Tagliabue
, and
A.
Del Sole
, “
Quality control on radiochemical purity in Technetium-99m radiopharmaceuticals labelling : three years of experience on 2280 procedures
,” vol.
88
, pp.
49
56
,
2017
.
15.
IAEA
, “
Quality Control in the Production of Radiopharmaceuticals (IAEA-TECDOC-1856
),”
IAEA
, vol.
1856
,
2018
.
16.
T.
Razaq
,
H.
Nisar
,
S.
Roohi
,
A.
Shehzad
, and
I.
Ahmad
, “
Administration of 99m Tc-DTPA in combination with doxorubicin alters the radiopharmaceutical biodistribution in rats
,”
Iran J Nucl Med
, vol.
25
, no.
2
, pp.
122
128
,
2017
.
17.
E. M.
Widyasari
,
I.
Halimah
,
R. J.
Sugiharti
, and
M.
Eka
, “
Biological Evaluation of 99m Tc-Kanamycin for Infection Imaging
,” vol.
2
, no.
1
, pp.
34
41
,
2017
.
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