Bioequivalence of ivermectin formulations in pigs and cattle
- Resource Type
- Authors
- Carlos Edmundo Lanusse; Luis Alvarez; Juan Manuel Sallovitz; A. Pis; R. Kujanek; Adrian Luis Lifschitz; S. Sanchez; Guillermo Leon Virkel
- Source
- Journal of Veterinary Pharmacology and Therapeutics. 22:27-34
- Subject
- Male
Veterinary medicine
Swine
Chemistry, Pharmaceutical
Glycerol formal
Bioequivalence
High-performance liquid chromatography
Excretion
Random Allocation
Subcutaneous injection
Ivermectin
Animal science
Blood plasma
medicine
Animals
Chromatography, High Pressure Liquid
Anthelmintics
Pharmacology
General Veterinary
Chemistry
Therapeutic Equivalency
Area Under Curve
Injections, Intravenous
Linear Models
Cattle
Dose rate
medicine.drug
- Language
- ISSN
- 1365-2885
0140-7783
The vehicle in which endectocide compounds are formulated plays a relevant role in their absorption kinetics and resultant systemic availability. The pharmaceutical bioequivalence and comparative plasma disposition kinetics of ivermectin (IVM), following the subcutaneous administration of two injectable formulations to pigs and cattle were investigated using parallel experimental designs. Sixteen parasite-free male Duroc Jersey-Yorkshire crossbred pigs (90-110 kg) (Expt 1) and 16 parasite-free male Holstein calves (100-120 kg) (Expt 2) were divided into two groups and treated subcutaneously at either 300 (pigs) or 200 (calves) microg/kg with two different propylene glycol/glycerol formal (60: 40) based IVM formulations; in both experiments pigs or calves in Group A received the test (IVM-TEST) formulation and those in Group B were treated with the reference formulation (IVM-CONTROL). Heparinized blood samples were taken from 0 h up to either 20 (pigs) or 30 (calves) days post-treatment and plasma was extracted, derivatized and analysed by high performance liquid chromatography (HPLC) using fluorescence detection. Early detection of IVM (12 h) with a peak plasma concentration (C(max)) between 33 and 39 ng/mL was observed in pigs. The drug was detected in plasma up to 20 days post-administration of either formulation, resulting in elimination half-lives between 3.47 and 3.80 days. There were no differences between the IVM-TEST and IVM-CONTROL formulations in the kinetic parameters (except t(max)) obtained in pigs. IVM was detected in plasma between 12 h and 30 days post-administration of both formulations under investigation in cattle. The plasma disposition kinetics of IVM in calves was similar following treatment with both formulations. C(max) values (between 40.5 and 46.4 ng/mL) were achieved at 2 days post-administration of both formulations. None of the estimated kinetic parameters were statistically different between drug formulations. The injectable IVM formulations investigated were bioequivalent after their subcutaneous administration to both pigs and calves at recommended dose rates.