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


: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.


J Pharm Sci


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




Has Abstract


1987-03-01 00:00:00














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    journal_title:Journal of pharmaceutical sciences

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    authors: Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

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    abstract::The single pass mean residence time in peripheral tissues, tp1, is a characteristic constant of linear pharmacokinetic systems and nonlinear systems with linear distribution kinetics. It is descriptive of distribution kinetics in such systems and is not dependent on elimination kinetics as are other related parameters...

    journal_title:Journal of pharmaceutical sciences

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    authors: Veng-Pedersen P,Gillespie WR

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    abstract::Though there is an advantage in using the higher solubility amorphous state in cases where low solubility limits absorption, physical instability poses a significant barrier limiting its use in solid oral dosage forms. Unlike chemical instability, where useful accelerated stability testing protocols are common, no met...

    journal_title:Journal of pharmaceutical sciences

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    authors: Bhugra C,Pikal MJ

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    journal_title:Journal of pharmaceutical sciences

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    authors: Hindmarsh KW,Hamon NW,LeGatt DF,Wallace SM

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    authors: Perevozchikova T,Nanda H,Nesta DP,Roberts CJ

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    authors: Sapio JP,Sethachutkul K,Moody JE

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  • Interactions of cephalosporins and penicillins with nonpolar macroporous styrenedivinylbenzene copolymers.

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    pub_type: 杂志文章


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    pub_type: 杂志文章


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