M. Hildebrand et al., DEVELOPMENT AND VALIDATION OF A SENSITIVE AND SPECIFIC RADIOIMMUNOASSAY FOR THE DETERMINATION OF CICAPROST IN BIOLOGICAL SAMPLES, Journal of immunoassay, 15(2), 1994, pp. 171-190
Cicaprost is a potent, chemically and metabolically stable PGI(2)-mime
tic. Pharmacodynamic effects were observed after oral administration o
f approximate to 10 mu g in man when plasma levels were in the low pg-
range. The present report describes the development of a selective ant
iserum and a tracer with high specific activity and their use for the
RIA determination of Cicaprost in biological samples. Cicaprost-[H-3]-
methylester with a specific activity of 819 GBq/mmol was used as a tra
cer. RIA-analyses were carried out with 0.05 - 0.5 ml plasma adjusted
to pH 2 with 1 N HCl and extracted with 2.5 ml diethylether. Separatio
n of antiserum bound and unbound Cicaprost was achieved by the charcoa
l method. Extraction recovery of Cicaprost was approximate to 90 % at
pH approximate to 2. The detection limit of the assay was 10 - 20 pg/m
l plasma. Coefficients of variations were 6, 3 and 9 % (within-day, n
= 5) and 25, 12 and 10 % (day-to-day, n = 11) at 50, 100 and 200 pg/ml
. HPLC-chromatograms of plasma extracts did not reveal any peak apart
from Cicaprost, demonstrating the specificity of the method. The prese
nt RIA for Cicaprost exhibits high specificity and sensitivity and wil
l be used for further bioanalyses in pharmacokinetic study.