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

杂志文章
  • Correlation of log P with molecular connectivity in hydroxyureas: influence of conformational system on log P.

    abstract::The correlation of log P (in octanol--water) with the nonempirical, topologically dependent, calculated molecular connectivity index (1chiv) delineates substituted hydroxyureas into two families of linearly related groups of compounds. The first group, composed of the 3-substituted ethyl, n-propyl, and n-butyl analogs...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670419

    authors: Parker GR

    更新日期:1978-04-01 00:00:00

  • Preparation of inhalable salbutamol sulphate using reactive high gravity controlled precipitation.

    abstract::Reactive high gravity controlled precipitation (HGCP) was carried out to produce salbutamol sulphate (SS) particles suitable for inhalation. Aqueous solutions of free salbutamol base and sulphuric acid were mixed intensely inside a HGCP reactor to form the particles. Spray drying was employed to obtain dry powders. Ph...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21026

    authors: Hu T,Chiou H,Chan HK,Chen JF,Yun J

    更新日期:2008-02-01 00:00:00

  • Effect of symmetrical tetraalkylammonium salts on cloud point on nonionic surfactants.

    abstract::The salting in and salting out of the nonionic surfactant octoxynol NF by halides of ammonium and the four lowest symmetrical tetraalkylammonium cations were investigated by measuring their effect on the cloud point at various salt concentrations. The chloride anion tended to salt the surfactant out, lowering its clou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660208

    authors: Schott H,Han SK

    更新日期:1977-02-01 00:00:00

  • Antidermatitic perspective of hydrocortisone as chitosan nanocarriers: an ex vivo and in vivo assessment using an NC/Nga mouse model.

    abstract::The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23446

    authors: Hussain Z,Katas H,Amin MC,Kumulosasi E,Sahudin S

    更新日期:2013-03-01 00:00:00

  • Effects of Product Handling Parameters on Particle Levels in a Commercial Factor VIII Product: Impacts and Mitigation.

    abstract::To reduce the risk of immunogenicity that may be caused by therapeutic protein products, it is important to properly characterize subvisible particles and to develop strategies to reduce the levels of particles delivered to patients. In the present study, by using state-of-the-art methods to quantify particle levels, ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.08.022

    authors: Ueda T,Nakamura K,Abe Y,Carpenter JF

    更新日期:2019-01-01 00:00:00

  • Solubility and partitioning. VII: Solubility of barbiturates in water.

    abstract::The solubility equation of Yalkowsky was used to estimate the aqueous solubility of 33 barbiturates in the temperature range of 5 to 45 degrees C. The equation was extended by adding a term which accounts for the effect of pH on the solubility of the drug. The extended equation is successful in estimating the aqueous ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600760120

    authors: Pinal R,Yalkowsky SH

    更新日期:1987-01-01 00:00:00

  • Estimating the relative stability of polymorphs and hydrates from heats of solution and solubility data.

    abstract::The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1080

    authors: Gu CH,Grant DJ

    更新日期:2001-09-01 00:00:00

  • Enhancement of solubility of drug salts by hydrophilic counterions: properties of organic salts of an antimalarial drug.

    abstract::Judicious choice of the salt form of a drug can greatly affect the aqueous solubility and formulation of the compound. The objective of this work was to demonstrate the effect of various counteranions on the aqueous solubility of the antimalarial agent alpha-(2-piperidyl)-3, 6-bis(trifluoromethyl)-9-phenanthrenemethan...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650533

    authors: Agharkar S,Lindenbaum S,Higuchi T

    更新日期:1976-05-01 00:00:00

  • Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effects of FcRn Inhibitors in Mice, Rats, and Monkeys.

    abstract::There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.10.065

    authors: Li T,Balthasar JP

    更新日期:2019-01-01 00:00:00

  • Development and characterization of a novel, antimicrobial, sterile hydrogel dressing for burn wounds: single-step production with gamma irradiation creates silver nanoparticles and radical polymerization.

    abstract::Patients with burn wounds are susceptible to wound infection and sepsis. This research introduces a novel burn wound dressing that contains silver nanoparticles (SNPs) to treat infection in a 2-acrylamido-2-methylpropane sulfonic acid sodium salt (AMPS-Na(+) ) hydrogel. Silver nitrate was dissolved in AMPS-Na(+) solut...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24095

    authors: Boonkaew B,Barber PM,Rengpipat S,Supaphol P,Kempf M,He J,John VT,Cuttle L

    更新日期:2014-10-01 00:00:00

  • Kinetic analysis of relationship between partition coefficient and biological response.

    abstract::Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700110

    authors: Cooper ER,Berner B,Bruce RD

    更新日期:1981-01-01 00:00:00

  • Degradation of paclitaxel and related compounds in aqueous solutions I: epimerization.

    abstract::Paclitaxel and other taxanes have complex structures including the presence of numerous hydrolytically sensitive ester groups and a chiral center that readily undergoes epimerization thus making their kinetics complex. The present study attempts to understand the mechanism of epimerization at the 7-position of paclita...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21112

    authors: Tian J,Stella VJ

    更新日期:2008-03-01 00:00:00

  • Novel method of derivatization of an amidinourea (lidamidine) for GLC analysis.

    abstract::A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710327

    authors: Won CM,Zalipsky JJ,Patel DM,Grim WM

    更新日期:1982-03-01 00:00:00

  • Physicochemical properties of carbovir, a potential anti-HIV agent.

    abstract::(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790908

    authors: Anderson BD,Chiang CY

    更新日期:1990-09-01 00:00:00

  • Low-density microparticles with petaloid surface structure for pulmonary drug delivery.

    abstract::The morphology of spray-dried particles composed of psicose and hydroxypropyl methylcellulose was modified by adding ammonium bicarbonate (ABC) to the solution. The surface structure of the particles was altered by immediate transformation of ABC to gaseous components during the spray drying. As a result, low-density ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23899

    authors: Kawakami K,Hasegawa Y,Zhang S,Yoshihashi Y,Yonemochi E,Terada K

    更新日期:2014-04-01 00:00:00

  • Drug release from hydrophilic matrices. 2. A mathematical model based on the polymer disentanglement concentration and the diffusion layer.

    abstract::A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer ch...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600841214

    authors: Ju RT,Nixon PR,Patel MV,Tong DM

    更新日期:1995-12-01 00:00:00

  • Differences in pharmacokinetics and ex vivo antioxidant activity following intravenous and oral administrations of emodin to rats.

    abstract::Emodin, a natural anthraquinone polyphenol, has been reported to possess promising in vitro antioxidation, anticancer and anti-inflammatory activities. Whether the in vitro bioactivities can predict in vivo effects remained an unanswered question without understanding emodin pharmacokinetics in animals. To fill this b...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21978

    authors: Shia CS,Hou YC,Tsai SY,Huieh PH,Leu YL,Chao PD

    更新日期:2010-04-01 00:00:00

  • Effect of micellization on rate of cupric-ion-promoted hydrolysis of dicarboxylic acid hemiesters.

    abstract::The effect of micellar sodium lauryl sulfate on the rate of cupric-ion-promoted hydrolysis of some dicarboxylic acid hemiesters was investigated at pH 5, ionic strength 0.1 M, and 40, 45, and 50 degrees. The rate of cupric-ion-promoted hydrolysis of sodium n-decyloxalate in the micellar phase is about 50 times as fast...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600651206

    authors: Ong JT,Kostenbauder HB

    更新日期:1976-12-01 00:00:00

  • Time-dependent changes in the activation of RhoA/ROCK and ERM/p-ERM in the increased expression of intestinal P-glycoprotein by repeated oral treatment with etoposide.

    abstract::Previously, we reported that repeated oral treatment with etoposide (ETP) increased ileal membrane localization of P-glycoprotein (P-gp) and that this was possibly mediated by increased expression of the ezrin/radixin/moesin (ERM)/phosphorylated ERM (p-ERM) via activation of RhoA/ROCK. These changes caused decreases i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23503

    authors: Kobori T,Harada S,Nakamoto K,Tokuyama S

    更新日期:2013-05-01 00:00:00

  • Interactions of acetylcholine mustard with acetylcholinesterase.

    abstract::The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600640839

    authors: Hudgins PM,Stubbins JF

    更新日期:1975-08-01 00:00:00

  • Zinc(II) in saliva: determination of concentrations produced by different formulations of zinc gluconate lozenges containing common excipients.

    abstract::A study of the pH of saliva produced by humans sucking hard candy lozenges containing zinc gluconate and citric acid demonstrated the probability that the formulation delivered an insignificant amount of the contained zinc as Zn2+. This could account for the negative results of several clinical studies of this lozenge...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810205

    authors: Zarembo JE,Godfrey JC,Godfrey NJ

    更新日期:1992-02-01 00:00:00

  • Topical oral cavity pharmacokinetic modeling of a stannous fluoride dentifrice: an unusual two compartment model.

    abstract::A pharmacokinetic model was developed describing the pharmacokinetics of stannous fluoride in human subjects after oral topical application of a stannous fluoride dentifrice. Twenty subjects participated in an investigation of an experimental dentifrice. Subjects rinsed their mouths with the experimental dentifrice sl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21691

    authors: Scott DC,Coggan JW,Cruze CA,He T,Johnson RD

    更新日期:2009-10-01 00:00:00

  • Micro and macro GLC determination of ethambutol in biological fluids.

    abstract::Previously available GLC methods for ethambutol may only be used to measure quantities of drugs much greater than those found in biological fluids such as plasma and dialysate. A previously published GLC method for plasma samples is extended to measure ethambutol in dialysate. A second GLC method, involving derivatiza...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670407

    authors: Lee CS,Benet LZ

    更新日期:1978-04-01 00:00:00

  • Preparation and characterization of quercetin nanocrystals.

    abstract::This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22446

    authors: Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

    更新日期:2011-06-01 00:00:00

  • Stereoselective pharmacokinetics and inversion of suprofen enantiomers in humans.

    abstract::The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600801116

    authors: Shinohara Y,Magara H,Baba S

    更新日期:1991-11-01 00:00:00

  • Chemical modifications of therapeutic proteins induced by residual ethylene oxide.

    abstract::Ethylene oxide (EtO) is widely used in sterilization of drug product primary containers and medical devices. The impact of residual EtO on protein therapeutics is of significant interest in the biopharmaceutical industry. The potential for EtO to modify individual amino acids in proteins has been previously reported. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24257

    authors: Chen L,Sloey C,Zhang Z,Bondarenko PV,Kim H,Ren D,Kanapuram S

    更新日期:2015-02-01 00:00:00

  • The Effect of Genetic Polymorphism on the Inhibition of Azole Antifungal Agents Against CYP2C9-Mediated Metabolism.

    abstract::We investigated the effect of cytochrome P450 (CYP) 2C9 polymorphism on the inhibition of methylhydroxylation activity of tolbutamide, a typical CYP2C9 substrate, by triazole antifungal agents, fluconazole and voriconazole. Although the Michaelis constants (Km), maximal velocities (Vmax), and Vmax/Km values for CYP2C9...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.01.007

    authors: Niwa T,Hata T

    更新日期:2016-03-01 00:00:00

  • Physiologically Based Pharmacokinetic Modeling to Supplement Nilotinib Pharmacokinetics and Confirm Dose Selection in Pediatric Patients.

    abstract::In adult patients, nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.01.028

    authors: Heimbach T,Lin W,Hourcade-Potelleret F,Tian X,Combes FP,Horvath N,He H

    更新日期:2019-06-01 00:00:00

  • Enhancing the Dissolution Stability of Hard Gelatin Capsules Using Activated Carbon as a Packaging Component.

    abstract::Hard gelatin capsule (HGC) shells are widely used to encapsulate drugs for oral delivery but are vulnerable to gelatin cross-linking, which can lead to slower and more variable in vitro dissolution rates. Adding proteolytic enzymes to the dissolution medium can attenuate these problems, but this complicates dissolutio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.08.009

    authors: Likar MD,Carroll SC,Colgan ST,Yeoh T,MacDonald BC,Johnson GM,Space JS

    更新日期:2018-12-01 00:00:00

  • Kinetic analysis of enantiomers of threo-methylphenidate and its metabolite in two healthy subjects after oral administration as determined by a gas chromatographic-mass spectrometric method.

    abstract::A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790602

    authors: Aoyama T,Kotaki H,Honda Y,Nakagawa F

    更新日期:1990-06-01 00:00:00