TY  - JOUR
T1  - Pharmacokinetics and Lung Tissue Concentration of Valnemulin in Swine
AU - Zhu, L.X. AU - Zhang, C.Y. AU - Guo, J.P. AU - Zhang, Z. AU - Liu, Y.H. AU - Wang, R. AU - Luo, X.Y. 
JO  - Journal of Animal and Veterinary Advances
VL  - 10
IS  - 14
SP  - 1824
EP  - 1828
PY  - 2011
DA  - 2001/08/19
SN  - 1680-5593
DO  - javaa.2011.1824.1828
UR  - https://makhillpublications.co/view-article.php?doi=javaa.2011.1824.1828
KW  - pig
KW  -bioavailability
KW  -HPLC-MS/MS
KW  -Valnemulin
KW  -pharmacokinetic
KW  -China
AB  - The systemic bioavailability and lung tissue distribution of valnemulin were investigated in swine. About 65 pigs received 10 mg kg<SUP>-1</SUP> body weight of valnemulin by either intravenous (i.v.) or oral (p.o.) route in two studies: study A (10 pigs, i.v. or p.o.) and study B (55 pigs, p.o.). The plasma and lung tissue concentration of the drug were determined by a validated HPLC-MS/MS method. Plasma concentration-time data after i.v. administration (10 mg kg<SUP>-1</SUP> b.w.) were best described by a two-compartment open model. The pharmacokinetic parameters were elimination   rate (k<SUB>e</SUB>) 0.95&plusmn;0.17 h<SUP>-1</SUP>, the maximum concentrations 4.63&plusmn;0.66 &#956;g mL<SUP>-1</SUP>, area under the plasma concentration-time curve (AUC<SUB>inf</SUB>) 5.30&plusmn;0.37 (h*&#956;g) mL<SUP>-1</SUP>. On the other hand, A one-compartment model with a 1st order absorption rate was best fitted to the plasma concentration-time curve of valnemulin after oral administration (10 mg kg<SUP>-1</SUP> b.w.) and the absorption rate (k<SUB>a</SUB>) was 0.34&plusmn;0.03 h<SUP>-1</SUP>, the elimination rate (k<SUB>e</SUB>) was 1.05&plusmn;0.19 h<SUP>-1</SUP>, the maximum concentration was 0.59&plusmn;0.08 &#956;g mL<SUP>-1</SUP> at 1.98&plusmn;0.21 h (t<SUB>max</SUB>), the mean p.o. bioavailability (F) was 57.43%. Following p.o. administration, a mean valnemulin concentration of 0.14 &#956;g g<SUP>-1</SUP> was detected in lung tissue at 36 h postdosing. The lung AUC<SUB>inf</SUB> (410.16 h*&#956;g g<SUP>-1</SUP>) was 77.39 times higher than the corresponding plasma AUC<SUB>inf </SUB>(5.30 h*&#956;g g<SUP>-1</SUP>). The apparent elimination half-time for valnemulin in lung was 3.57 h. The advisable bioavailability and extensive distribution to lung tissue following a single dose of valnemulin may be desirable pharmacokinetic attributes for an antimicrobial drug used for the treatment and prevention of respiratory disease in swine.
ER  -