The distribution of free and non-ionic vesicular sodium stibogluconate in the dog.
J Drug Target
; 1(2): 133-42, 1993.
Article
en En
| MEDLINE
| ID: mdl-8069551
The pharmacokinetics and tissue distribution of antimony after the administration of sodium stibogluconate in a free form or entrapped in vesicles prepared from non-ionic surfactant were studied in the dog. Animals were given either one or two intravenous bolus injection(s) equivalent to 45 mg Sb kg-1 as free drug or 0.625 or 0.685 mg Sb kg-1 as vesicular drug. Blood samples were taken at various times after dosing and antimony levels in various tissues were determined at 3 h, 48 h and 6 days after dosing. After free stibogluconate antimony clearance from the blood occurred in a rapid elimination phase with a blood half-life of 0.58 +/- 0.08 h. This rapid elimination phase did not occur after vesicular drug. Both drug preparations gave similar antimony levels in the spleen, liver and femur and humerus bone marrow at all time points assessed even though the vesicular dose was one-seventieth of the free drug dose. After the free drug there was marked urinary excretion of antimony and, as a result, increased kidney loading at the expense of other tissue. Vesicle-mediated drug delivery suppressed renal excretion and a much greater proportion of the antimony dose was recovered from tissue than was obtained after free drug. A hypothesis is presented to account for the differences in tissue antimony concentrations produced by the two formulations.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Gluconato de Sodio Antimonio
Límite:
Animals
Idioma:
En
Revista:
J Drug Target
Asunto de la revista:
FARMACOLOGIA
Año:
1993
Tipo del documento:
Article
Pais de publicación:
Reino Unido