3H-PSGAG concentration in the synovial fluid of the equine antebrachiocarpal, metacarpophalangeal, coronopedal and tibiotarsal joints following a 500 MG i

Abstract

Summary Eight mature horses were administered a single intramuscular injection of 500 mg polysulfated glycosaminoglycan (PSGAG) labeled with 2.044 mCi tritium. Synovial fluid samples were collected from the antebrachiocarpal (carpal), metacarpophalangeal (fetlock), tibiotarsal (hock) and coronopedal (coffin) joints prior to injection and at 2, 4, 8, 12, and 24 hours after injection. The samples were subjected to scintillation counting in decays per minute and were converted to μg PSGAG per ml. The levels achieved in the synovial fluid of the various joints were compared to levels of PSGAG described as adequate to inhibit enzymes which degrade articular cartilage matrix components and hyaluronic acid and adequate to stimulate production of new matrix components and hyaluronic acid in diseased joints. Mean synovial fluid 3H-PSGAG levels indicated that peak concentrations of 3H-PSGAG were achieved 2 hours post injection in all joints and that these concentrations were within the therapeutic range for PSGAG. The peak concentrations were not significantly different among the joints except between the antebrachiocarpal and the metacarpophalangeal joints. The areas under the concentration-time curves (AUC) for each joint were computed by the trapezoidal method from hour 0 through hour 24 and by empirical exponential decay beyond hour 24. These values were subjected to an analysis of variance (ANOVA). The overall multivariate test of AUC among all joints was not significant. The data from this study indicate that a single intramuscular 500 mg injection of PSGAG provided therapeutic levels of the drug in the equine antebrachiocarpal, metacarpophalangeal, tibiotarsal, and coronopedal joints within 2 hours of injection. While there were differences in levels between joints at certain time points, the AUC values suggest similar distribution of the drug in all joints tested.