TY - JOUR
T1 - Pharmacokinetics of ofloxacin in serum and vitreous humor of albino and pigmented rabbits
AU - Perkins, R. J.
AU - Liu, W.
AU - Drusano, G.
AU - Madu, A.
AU - Mayers, M.
AU - Madu, C.
AU - Miller, M. H.
PY - 1995
Y1 - 1995
N2 - The purpose of this study was to evaluate the pharmacokinetics of ofloxacin in serum and vitreous humor samples from albino and pigmented rabbits by using a recently described animal model which permits robust estimation of parameter values. The drug was administered to rabbits intravenously, multiple vitreous humor and serum samples were taken from each rabbit, and the vitreous humor and serum samples were assayed by high- pressure liquid chromatography. The pharmacokinetic parameters were determined with RSTRIP, an iterative, nonlinear, weighted, least-squares regression program. Eight New Zealand White rabbits and eight Dutch belted rabbits (split into single-dose and multiple-dose groups) were investigated in this study. The value of penetration into the vitreous humor of albino rabbits (n = 6) was 32.6% ± 2.12%, with terminal-elimination half-life values of 3.21 and 2.39 h, respectively, for vitreous humor and serum. In pigmented rabbits after a single dose (n = 3) and with a steady-state concentration of drug in serum (n = 4), penetration values were similar, at 30.4% ± 2.98% and 30.0% ± 4.12%, respectively (P > 0.10). Following a single dose of ofloxacin, pigmented animals had elimination half-life values from serum and vitreous humor of 2.64 and 4.32 h, respectively. After steady state was achieved, half-life values for serum and vitreous humor were 3.12 and 6.05 h, respectively. By comparing pigmentation, dose mode, and elimination from vitreous humor, the vitreous humor half-life value for singly dosed albino rabbits (3.21 h) was not more rapid than that for singly dosed pigmented rabbits (4.32 h [P > 0.10]) but was more rapid than that for multiply dosed pigmented rabbits (6.05 h [P < 0.05]). The excellent penetration of ofloxacin into uninflamed rabbit eyes in conjunction with the higher levels in blood found in humans and greater activity against coagulase-negative staphylococci suggest that ofloxacin may be preferable to other quinolones for evaluation in the prophylaxis and treatment of bacterial eudophthalmitis.
AB - The purpose of this study was to evaluate the pharmacokinetics of ofloxacin in serum and vitreous humor samples from albino and pigmented rabbits by using a recently described animal model which permits robust estimation of parameter values. The drug was administered to rabbits intravenously, multiple vitreous humor and serum samples were taken from each rabbit, and the vitreous humor and serum samples were assayed by high- pressure liquid chromatography. The pharmacokinetic parameters were determined with RSTRIP, an iterative, nonlinear, weighted, least-squares regression program. Eight New Zealand White rabbits and eight Dutch belted rabbits (split into single-dose and multiple-dose groups) were investigated in this study. The value of penetration into the vitreous humor of albino rabbits (n = 6) was 32.6% ± 2.12%, with terminal-elimination half-life values of 3.21 and 2.39 h, respectively, for vitreous humor and serum. In pigmented rabbits after a single dose (n = 3) and with a steady-state concentration of drug in serum (n = 4), penetration values were similar, at 30.4% ± 2.98% and 30.0% ± 4.12%, respectively (P > 0.10). Following a single dose of ofloxacin, pigmented animals had elimination half-life values from serum and vitreous humor of 2.64 and 4.32 h, respectively. After steady state was achieved, half-life values for serum and vitreous humor were 3.12 and 6.05 h, respectively. By comparing pigmentation, dose mode, and elimination from vitreous humor, the vitreous humor half-life value for singly dosed albino rabbits (3.21 h) was not more rapid than that for singly dosed pigmented rabbits (4.32 h [P > 0.10]) but was more rapid than that for multiply dosed pigmented rabbits (6.05 h [P < 0.05]). The excellent penetration of ofloxacin into uninflamed rabbit eyes in conjunction with the higher levels in blood found in humans and greater activity against coagulase-negative staphylococci suggest that ofloxacin may be preferable to other quinolones for evaluation in the prophylaxis and treatment of bacterial eudophthalmitis.
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U2 - 10.1128/AAC.39.7.1493
DO - 10.1128/AAC.39.7.1493
M3 - Article
C2 - 7492092
AN - SCOPUS:0029017412
SN - 0066-4804
VL - 39
SP - 1493
EP - 1498
JO - Antimicrobial agents and chemotherapy
JF - Antimicrobial agents and chemotherapy
IS - 7
ER -
