TY - JOUR
T1 - Exploratory bioavailability and pharmacokinetic studies of sulphadimethoxine and ormetoprim in the penaeid shrimp, Penaeus vannamei
AU - Park, Eric D.
AU - Lightner, Donald V.
AU - Milner, Nicholas
AU - Mayersohn, Michael
AU - Park, Douglas L.
AU - Gifford, James M.
AU - Bell, Thomas A.
PY - 1995/2/15
Y1 - 1995/2/15
N2 - The pharmacokinetics and bioavailability of sulphadimethoxine (SDM) and ormetoprim (OMP) were examined, following simultaneous administration in penaeid shrimp. The hemolymph concentration versus time data following intra-sinus injection for both SDM (42 mg/kg) and OMP (8.6 mg/kg) were well described by a multiexponential equation suggesting multicompartmental behavior. The SDM:OMP parameter estimates of systemic clearance, steady-state volume of distribution, and disposition half-life were 215:1765 ml/kg · h, 1319:34 382 ml/kg, and 9.0:17.8 h, respectively. Hemolymph protein binding of SDM and OMP was 5.2% and 12.1%, respectively. The bioavailabilities of SDM and OMP were 30% and 32%, respectively. Peak hemolymph concentration (Cmax) and time of occurrence of that value (Tmax) for SDM following a single oral dose (210 mg/kg) were 25.0 μg/ ml at 4 h, while the corresponding values for OMP were (dose, 42 mg/kg) 0.70 μg/ml at 4 h. The percent of the available oral dose 2 h post-administration for SDM:OMP in the hemolymph, muscle, and hepatopancreas were 5.0:0.6%, 7.8:3.4%, and 2.4:24.8%, respectively. Hemolymph and muscle tissue concentrations were below detectable limits after 48 h for SDM and 24 h for OMP. The SDM:OMP drug combination has good potential as a shrimp chemotherapeutant in that they were rapidly and moderately absorbed, have relatively short half-lives and low hemolymph protein binding which translates to the bulk of absorbed drugs being available for a therapeutic response.
AB - The pharmacokinetics and bioavailability of sulphadimethoxine (SDM) and ormetoprim (OMP) were examined, following simultaneous administration in penaeid shrimp. The hemolymph concentration versus time data following intra-sinus injection for both SDM (42 mg/kg) and OMP (8.6 mg/kg) were well described by a multiexponential equation suggesting multicompartmental behavior. The SDM:OMP parameter estimates of systemic clearance, steady-state volume of distribution, and disposition half-life were 215:1765 ml/kg · h, 1319:34 382 ml/kg, and 9.0:17.8 h, respectively. Hemolymph protein binding of SDM and OMP was 5.2% and 12.1%, respectively. The bioavailabilities of SDM and OMP were 30% and 32%, respectively. Peak hemolymph concentration (Cmax) and time of occurrence of that value (Tmax) for SDM following a single oral dose (210 mg/kg) were 25.0 μg/ ml at 4 h, while the corresponding values for OMP were (dose, 42 mg/kg) 0.70 μg/ml at 4 h. The percent of the available oral dose 2 h post-administration for SDM:OMP in the hemolymph, muscle, and hepatopancreas were 5.0:0.6%, 7.8:3.4%, and 2.4:24.8%, respectively. Hemolymph and muscle tissue concentrations were below detectable limits after 48 h for SDM and 24 h for OMP. The SDM:OMP drug combination has good potential as a shrimp chemotherapeutant in that they were rapidly and moderately absorbed, have relatively short half-lives and low hemolymph protein binding which translates to the bulk of absorbed drugs being available for a therapeutic response.
KW - Ormetoprim
KW - Penaeus vannamei
KW - Pharmacokinetics
KW - Sulphadimethoxine
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U2 - 10.1016/0044-8486(94)00217-C
DO - 10.1016/0044-8486(94)00217-C
M3 - Article
AN - SCOPUS:0009215081
VL - 130
SP - 113
EP - 128
JO - Aquaculture
JF - Aquaculture
SN - 0044-8486
IS - 2-3
ER -