Enzyme immunoassay discrimination of a new angiotensin-converting enzyme (ACE) inhibitor, cilazapril, and its active metabolite.

Abstract:

:Simple and sensitive enzyme immunoassays (EIAs), discriminating a new angiotensin-converting enzyme (ACE) inhibitor, cilazapril [9(s) - [1(s)-(ethoxycarbonyl)-3-phenylpropylamino]-octahydro-10-oxo-6H- pyridazo[1,2-a] [1,2]diazepine-1(s)carboxylic acid] and its active metabolite [9(s)-[1(s)-carboxy-3-phenylpropylamino]-octahydro-10-oxo-6H- pyridazo[1,2-a][1,2]diazepine-1(s)carboxylic acid] were developed for pharmacokinetic studies of this drug which is used as an antihypertensive agent. These assays can be performed directly on serum or plasma specimens without pretreatment. The EIA for cilazapril (prodrug) allowed the determination of as little as 30 pg/mL, while a 1000-times greater concentration of its active metabolite was required to achieve the same extent of inhibition. The EIA for the active metabolite exhibited a sensitivity and specificity similar to those of the prodrug. Plasma specimens from a human volunteer study and a marmoset subacute toxicity study were assayed by these two newly developed EIAs. The plasma levels of active metabolite determined by the EIA were compared with those assayed by radioenzymatic assay, and a good correlation was observed between them.

journal_name

J Pharm Sci

authors

Tanaka H,Yoneyama Y,Sugawara M,Umeda I,Ohta Y

doi

10.1002/jps.2600760308

subject

Has Abstract

pub_date

1987-03-01 00:00:00

pages

224-7

issue

3

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)47362-9

journal_volume

76

pub_type

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