Manufacture and properties of erythromycin beads containing neutron-activated erbium-171.
To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activation into the short-lived gamma ray-emitting radionuclide, erbium-171. In vitro studies indicated that the dissolution profile, acid resistance, and enteric-coated surface of the pellets were minimally affected by the irradiation procedure. Antimicrobial potency was also unaffected, as determined by microbiological assay. Neutron activation thus appears to simplify the radiolabeling of complex pharmaceutical dosage forms for in vivo study by external gamma scintigraphy.
Parr
A F
AF
Division of Medicinal Chemistry and Pharmaceutics, College of Pharmacy, University of Kentucky, Lexington 40536-0082.
Digenis
G A
GA
Sandefer
E P
EP
Ghebre-Sellassie
I
I
Iyer
U
U
Nesbitt
R U
RU
Scheinthal
B M
BM
D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding; D004871:Erbium / Q000032:analysis*; D004917:Erythromycin / Q000008:administration & dosage* / Q000494:pharmacology / Q000528:radiation effects; D005720:Gamma Rays; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D009501:Neutron Activation Analysis; D011868:Radioisotopes; D012995:Solubility; D013608:Tablets, Enteric-Coated
D011868:Radioisotopes; D013608:Tablets, Enteric-Coated; D004917:Erythromycin; D004871:Erbium