A sensitive radioimmunoassay for budesonide in plasma. 1982

G W Aherne, and P Littleton, and A Thalen, and V Marks

Budesonide is a highly potent non-halogenated glucocorticoid with local anti-inflammatory properties. A sensitive radioimmunoassay for the measurement of the drug in unextracted plasma has been developed. Budesonide 21-hemisuccinate and budesonide 3-(O-carboxymethyl)oxime were conjugated to ovalbumin using the mixed anhydride method and antibodies to the haptens produced in sheep. The specificity of the antisera towards cortisol, and possible budesonide metabolites reflected the different sites of the attachment of the haptens to the carrier protein. An antiserum raised against the 3-(O-carboxy methyl)oxime conjugate was more specific (0.001% cross reaction) with respect to cortisol than the antiserum raised against the 21-hemisuccinate conjugate (0.344% cross reaction). Endogenous steroids at concentrations normally encountered in clinical samples, would not interfere with the measurement of budesonide. The radioimmunoassay was developed using the budesonide 3-(O-carboxy methyl)oxime antiserum, [3H]-budesonide and dextran coated charcoal phase separation. The theoretical limit of detection of the assay was 50 pg/ml. Budesonide was quantitatively recovered from normal human drug/free plasma at concentrations above 1 ng/ml (2.32 nmol/l) with a between batch variation of 12-15%. Budesonide was measured in the unextracted plasma of volunteers who had inhaled the drug from a pressurised aerosol spray.

UI MeSH Term Description Entries
D011282 Pregnenediones Unsaturated pregnane derivatives containing two keto groups on side chains or ring structures. Diketopregnenes,Dioxopregnenes
D011863 Radioimmunoassay Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation. Radioimmunoassays
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012756 Sheep Any of the ruminant mammals with curved horns in the genus Ovis, family Bovidae. They possess lachrymal grooves and interdigital glands, which are absent in GOATS. Ovis,Sheep, Dall,Dall Sheep,Ovis dalli
D019819 Budesonide A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS. Tarpeyo,Budesonide, (R)-Isomer,Budesonide, (S)-Isomer,Horacort,Pulmicort,Rhinocort

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