INVESTIGADORES
LANUSSE Carlos Edmundo
artículos
Título:
Moxidectin and ivermectin metabolic stability in sheep ruminal and abomasal contents
Autor/es:
LIFSCHITZ, A., VIRKEL, G., BALLENT, M., SALLOVITZ, J., LANUSSE, C.
Revista:
JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
Editorial:
Blackwell Publishing
Referencias:
Año: 2005 vol. 28 p. 411 - 418
ISSN:
0140-7783
Resumen:
The oral administration of macrocyclic lactones to sheep leads to poorer efficacy
and shorter persistence of the antiparasitic activity compared to the subcutaneous
treatment. Gastrointestinal biotransformation occurring after oral
treatment to ruminant species has been considered as a possible cause of the
differences observed between routes of administration. The current work was
addressed to evaluate on a comparative basis the in vitro metabolism of
moxidectin (MXD) and ivermectin (IVM) in sheep ruminal and abomasal
contents. Both compounds were incubated under anaerobic conditions during
2, 6 and 24 h in ruminal and abomasal contents collected from untreated adult
sheep. Drug concentrations were measured by high-performance liquid
chromatography with fluorescence detection after sample clean up and solid
phase extraction. Neither MXD nor IVM suffered metabolic conversion and/or
chemical degradation after 24-h incubation in ruminal and abomasal contents
collected from adult sheep. Unchanged MXD and IVM parent compounds
represented between 95.5 and 100% of the total drug recovered in the ruminal
and abomasal incubation mixtures compared with those measured in inactive
control incubations. The partition of both molecules between the solid and fluid
phases of both sheep digestive contents was assessed. MXD and IVM were
extensively bound (>90%) to the solid material of both ruminal and abomasal
contents collected from sheep fed on lucerne hay. The results reported here
confirm the extensive degree of association to the solid digestive material and
demonstrates a high chemical stability without evident metabolism and/or
degradation for both MXD and IVM in ruminal and abomasal contents.
moxidectin (MXD) and ivermectin (IVM) in sheep ruminal and abomasal
contents. Both compounds were incubated under anaerobic conditions during
2, 6 and 24 h in ruminal and abomasal contents collected from untreated adult
sheep. Drug concentrations were measured by high-performance liquid
chromatography with fluorescence detection after sample clean up and solid
phase extraction. Neither MXD nor IVM suffered metabolic conversion and/or
chemical degradation after 24-h incubation in ruminal and abomasal contents
collected from adult sheep. Unchanged MXD and IVM parent compounds
represented between 95.5 and 100% of the total drug recovered in the ruminal
and abomasal incubation mixtures compared with those measured in inactive
control incubations. The partition of both molecules between the solid and fluid
phases of both sheep digestive contents was assessed. MXD and IVM were
extensively bound (>90%) to the solid material of both ruminal and abomasal
contents collected from sheep fed on lucerne hay. The results reported here
confirm the extensive degree of association to the solid digestive material and
demonstrates a high chemical stability without evident metabolism and/or
degradation for both MXD and IVM in ruminal and abomasal contents.
in vitro metabolism of moxidectin (MXD) and ivermectin (IVM) in sheep ruminal and abomasal
contents. Both compounds were incubated under anaerobic conditions during
2, 6 and 24 h in ruminal and abomasal contents collected from untreated adult
sheep. Drug concentrations were measured by high-performance liquid
chromatography with fluorescence detection after sample clean up and solid
phase extraction. Neither MXD nor IVM suffered metabolic conversion and/or
chemical degradation after 24-h incubation in ruminal and abomasal contents
collected from adult sheep. Unchanged MXD and IVM parent compounds
represented between 95.5 and 100% of the total drug recovered in the ruminal
and abomasal incubation mixtures compared with those measured in inactive
control incubations. The partition of both molecules between the solid and fluid
phases of both sheep digestive contents was assessed. MXD and IVM were
extensively bound (>90%) to the solid material of both ruminal and abomasal
contents collected from sheep fed on lucerne hay. The results reported here
confirm the extensive degree of association to the solid digestive material and
demonstrates a high chemical stability without evident metabolism and/or
degradation for both MXD and IVM in ruminal and abomasal contents.