Sustained release characteristics of rifampin-loaded microsphere formulations in nonhuman primates.
Controlled release rifampin-loaded microspheres were evaluated for the first time in nonhuman primates. Animals received either 2.0 g of a large formulation (10-150 microm, 23 wt% rifampin) injected subcutaneously at Day 0 (118-139 mg rifampin/kg), 4.0 g of a small formulation (1-10 microm, 5.8 wt% rifampin) administered intravenously in 2.0 g doses on Day 0 and 7 (62.7-72.5 mg rifampin/kg), or a combination of small and large microspheres (169-210 mg rifampin/kg). Extended rifampin release was observed up to 48 days. Average rifampin concentrations remaining in the liver, lung, and spleen at 30 days were 14.03, 4.09, and 1.98 microg/g tissue, respectively.
Quenelle
Debra
D
Department of Pediatrics, Division of Infectious Diseases, University of Alabama at Birmingham, Alabama, USA.
Winchester
Gary A
GA
Staas
Jay K
JK
Hoskins
Darrel E
DE
Barrow
Esther W
EW
Barrow
William W
WW
D000818:Animals; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005260:Female; D008252:Macaca fascicularis; D008297:Male; D008863:Microspheres; D012293:Rifampin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D012293:Rifampin