Determination of nuvenzepine in human plasma by a sensitive sup 3 Hpirenzepine radioreceptor binding assay

Journal Article · Fri Feb 01 04:00:00 EST 1991 · Journal of Pharmaceutical Sciences; (United States)

DOI:https://doi.org/10.1002/jps.2600800219· OSTI ID:5557039

Caselli, G; Ferrari, M P; Tonon, G; Clavenna, G; Borsa, M ^[1]

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1. Research Development Laboratories, Dompe Farmaceutici S.p.A., Milano (Italy)

A sensitive method for the quantitation of small amounts of nuvenzepine, a new M1-selective antimuscarinic drug, in plasma is described. The analytical method involves the use of a radioreceptor binding assay based on {sup 3}Hpirenzepine displacement in rat cerebral cortex homogenates; no previous extraction is required. The method is reliable, with an interassay CV ranging from 5 to 10%, and allows the analysis of greater than 100 samples/experiment. The limit of detection is {approximately} 0.1 ng/assay. Using this method we have determined the plasma levels of nuvenzepine in eight healthy volunteers treated PO with 15 or 25 mg of nuvenzepine.HCl. The pharmacokinetic parameters obtained were (for 15 and 25 mg): Cmax, 64 and 131 ng/mL; AUC0-infinity, 851 and 1379 ng.h/mL; t1/2, 8.6 and 7.2 h. These values are in good agreement with those obtained using an HPLC method. Therefore, this radioreceptor binding assay proved to be simple, rapid, and specific for the determination of low levels of nuvenzepine in human plasma.

• OSTI ID: 5557039
• Journal Information: Journal of Pharmaceutical Sciences; (United States), Journal Name: Journal of Pharmaceutical Sciences; (United States) Vol. 80:2; ISSN JPMSA; ISSN 0022-3549
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY FLUIDS
DOSE-RESPONSE RELATIONSHIPS
DRUGS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
MAMMALS
MAN
MATERIALS
ORAL ADMINISTRATION
PARASYMPATHOLYTICS
PRIMATES
RADIORECEPTOR ASSAY
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES