Pharmacokinetics assessment of moxidectin long-acting formulation in cattle.
The plasma kinetics disposition of moxidectin following a subcutaneous administration with a long-acting formulation (Cydectin) 10%, Fort Dodge Animal Health, France) at the recommended dose of 1 mg kg(-1) body weight was evaluated in Charolais cattle breed (five females weighing 425-450 kg) for 120 days. Furthermore, its concentration was measured in hair for the same period. After plasma extraction and derivatization, samples were analysed by HPLC with fluorescence detection. Moxidectin was first detected at 1 h after treatment for plasma (2.00+/-1.52 ng ml(-1)) and at 2 days for hair (446.44+/-193.26 ng g(-1)). The peak plasma concentration (C(max)) was 55.71+/-15.59 ng ml(-1) and 444.44+/-190.45 ng g(-1) for plasma and hair, respectively. The mean calculated time of peak occurrence (T(max)) was 3.40+/-3.36 and 2 days for plasma and hair, respectively. The mean residence time (MRT) was 28.93+/-2.87 and 13.32+/-2.48 days for plasma and hair cattle. The area under concentration-time curve (AUC) was 1278.95+/-228.92 ng day ml(-1) and 2663.82+/-1096.62 ng day g(-1) for plasma and hair, respectively. At the last sampling time (120 days), the concentration was 1.91+/-0.26 ng ml(-1) and 0.69+/-0.52 ng g(-1) for plasma and hair, respectively. The bioavailability of this long-acting formulation of moxidectin is similar to that registered after subcutaneous administration of moxidectin in cattle at 0.2 mg kg(-1) body weight. For the first time the moxidectin pharmacokinetics parameters in hair after a subcutaneous administration was described. The moxidectin profile concentrations in hair reflected that registered in plasma. The previous studies of efficacy have to be correlated to the extended period of absorption and distribution by the LA formulation due to the fivefold higher dose rate in comparison with the 1% injectable formulation (0.2 mg kg(-1) body weight).
Dupuy
J
J
INRA-UR66, Laboratoire de Pharmacologie-Toxicologie, 180 Chemin de Tournefeuille, B.P. 3, 31931 Toulouse Cedex 9, France. Jacques.Dupuy@toulouse.inra.fr
Sutra
J F
JF
Alvinerie
M
M
D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D002417:Cattle; D003692:Delayed-Action Preparations; D005260:Female; D006197:Hair / Q000737:chemistry; D007279:Injections, Subcutaneous; D018942:Macrolides / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics
D000871:Anthelmintics; D003692:Delayed-Action Preparations; D018942:Macrolides; C027837:moxidectin