Influence of Food on the Bioavailability of Enalapril

Swanson, Brian N.; Vlasses, Peter H.; Ferguson, Roger K.; Bergquist, Paul A.; Till, Alice E.; Irvin, John D.; Harris, Katherine E.

doi:10.1002/jps.2600731146

Cited by 54 publications

(14 citation statements)

References 9 publications

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“…2 The drug is official in the USP 24. 3 The methods of analysis of the bulk drug and its tablets are high-performance liquid chromatography (HPLC) methods.…”

Section: Enalapril [(S)-1-(n-[1-(ethoxycarbonyl)-3-phenylpropyl]-lalamentioning

confidence: 99%

Flow-Injection Chemiluminescence Determination of Enalapril Maleate in Pharmaceuticals and Biological Fluids Using Tris(2,2′-bipyridyl)ruthenium(II)

Alarfaj

2003

ANAL. SCI.

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Enalapril maleate is a relatively new oral angiotensinconverting enzyme (ACE) inhibitor. Enalapril maleate, like its first-generation relative, captopril, has been shown to be effective in the treatment of hypertension and congestive heart failure. Enalapril [(S)-1-(N-[1-(ethoxycarbonyl)-3-phenylpropyl]-Lalanyl)-L-proline] is a prodrug which is de-esterified in the hepatic system to an active diacid form. 2 The drug is official in the USP 24. 3 The methods of analysis of the bulk drug and its tablets are high-performance liquid chromatography (HPLC) methods. It is also official in the European Pharmacopoeia 4 by a potentiometric titration method using sodium hydroxide.Other than the published analytical profile, 5 several methods have been reported for the analysis of enalapril maleate either in pure form, in pharmaceutical preparations, in biological fluids, or in mixture with other drugs. These include spectrophotometric methods, 33 Reviewing the literature revealed that up to the present time nothing has been published concerning the CL determination of enalapril maleate.Ru(bipy) 3 2+ is an extremely versatile base reactant for a variety of CL processes, and has also recently become a useful CL reagent. The process involves the oxidation of Ru(bipy)3 2+to Ru(bipy) 3 3+ , which is then followed by reduction with an analyte species to produce the emission of light. 34 There have been a variety of methods employed to obtain the active oxidized reagent Ru(bipy) 3 3+ .These include chemical, photochemical, electrochemical oxidation and in situ electrochemiluminescence.An analytical evaluation of commercially significant pharmaceutical drugs using Ru(bipy) 3 3+-CL detection has attracted considerable attention. A comprehensive review of the analytical applications of Ru(bipy) 3 3+ as a chemiluminescent reagent from 1978 to mid 1998 has been represented by Gerardi et al. 34The present paper describes the development of a simple flow-injection chemiluminometric method for the determination of enalapril maleate based on the chemical generation of Ru(bipy) 3 3+ by mixing two streams containing solutions of Ru(bipy) 3 2+ and acidic KMnO4. The experimental conditions for the reaction were optimized, and the final procedure allowed the successful determination of the studied drug in pharmaceuticals and biological fluids. Experimental Apparatus and manifoldThe flow system used for the determination and CL detection of enalapril maleate is shown schematically in Fig. 1. It consisted of a Gilson Minipuls 3MP4 peristaltic pump (two channels, variable speed) which was used to drive the carrier and the reagent streams through the flow system. Each stream was pumped at a constant flow rate using PTFE tubing (0.8 mm i.d.). The drug solution (250 µl) was injected through the sample injection valve, which allowed mixing of the sample with an acidified 1 × 10 -3 mol/l KMnO4 solution, and then combination with a 1 × 10 -2 mol/l Ru(bipy) 3 2+ solution in a Tshaped piece before entering the flow cell. The flow cell was a coil made of ...

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“…2 The drug is official in the USP 24. 3 The methods of analysis of the bulk drug and its tablets are high-performance liquid chromatography (HPLC) methods.…”

Section: Enalapril [(S)-1-(n-[1-(ethoxycarbonyl)-3-phenylpropyl]-lalamentioning

confidence: 99%

Flow-Injection Chemiluminescence Determination of Enalapril Maleate in Pharmaceuticals and Biological Fluids Using Tris(2,2′-bipyridyl)ruthenium(II)

Alarfaj

2003

ANAL. SCI.

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“…Enalapril binds moderately (50%-60%) with plasma proteins [12]. It is metabolized in the liver to enalaprilat in the first 4 h following oral administration [4,8,11,12]; first-pass metabolism of enalapril to enalaprilat is approximately 18% [12]. It is excreted mainly (60%) in the urine, 18% in the form of parent drug and 43% as enalaprilat [4,11,13]; faecal elimination is 6% as enalapril and 27% as enalaprilat [11].…”

Section: Introductionmentioning

confidence: 99%

“…Enalapril maleate is well absorbed (53%-73%) from the gastrointestinal tract [4À6], while enalaprilat is poorly absorbed following oral administration [7]; food does not affect the oral absorption of enalapril [4,8]. Following oral doses of 5, 10, 20, and 40 mg of enalapril maleate, peak serum enalaprilat concentrations of 15, 37, 71 and 123 ng/ml, respectively, were observed between 3.2 and 4.8 h after administration.…”

Section: Introductionmentioning

confidence: 99%

Bioequivalence evaluation of two brands of enalapril 20mg tablets (narapril and renitec) in healthy human volunteers

Najib

Idkaidek

Adel

et al. 2003

Biopharm & Drug Disp

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The bioequivalence of two brands of enalapril 20 mg tablets was demonstrated in 24 healthy human volunteers after a single oral dose in a randomized cross-over study, conducted at IPRC, Amman, Jordan. Reference (Renitec, MSD, Netherlands) and test (Narapril, Julphar, UAE) products were administered to fasted male volunteers; blood samples were collected at specified time intervals, plasma separated and analysed for enalapril and its active metabolite (enalaprilat) using a validated LC-MS/MS method at Cartesius Analytical Unit, Institute of Biomedical Sciences, USP, Sao Paulo, Brazil. The pharmacokinetic parameters AUC(0-t), AUC(0-infinity), Cmax, Tmax, T(1/2) and elimination rate constant were determined from plasma concentration-time profile for both formulations and were compared statistically to evaluate bioequivalence between the two brands, using the statistical modules recommended by FDA. The analysis of variance (ANOVA) did not show any significant difference between the two formulations and 90% confidence intervals fell within the acceptable range for bioequivalence. Based on these statistical inferences it was concluded that the two brands exhibited comparable pharmacokinetic profiles and that Julphar's Narapril is bioequivalent to Renitec of MSD, Netherlands.

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“…The bioavailability of pentopril was unaffected when administered with food, although a delay in absorption was suggested by a delay in tmax of approximately 1.5 h (Rakhit et al, 1985). In contrast, the bioavailability of enalapril, lisinopril and quinapril was not affected by food in any manner (Swanson et al, 1984;Mojaverian et al, 1986;Ferry et al, 1987).…”

Section: Introductionmentioning

confidence: 89%

The influence of food on the pharmacokinetics and ACE inhibition of cilazapril.

Massarella

Defeo

Brown

et al. 1989

Brit J Clinical Pharma

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1 The influence of food on the pharmacokinetics and angiotensin-converting enzyme (ACE) inhibitory effects of oral 5 mg doses of cilazapril was investigated in a two-way crossover study in 16 volunteers. 2 Plasma and urine concentrations of cilazaprilat, the active diacid metabolite of cilazapril, and plasma ACE activity were determined by a radio-enzymatic method.3 Cmax decreased by 30% (P < 0.05) with a delay in tmax of 1 h (P < 0.05) and area under curve (AUC) was decreased by 14% (P < 0.05). The elimination rate was unaltered.4 Onset of ACE inhibition was delayed by 30 min but degree and duration were unaffected.5 The effect of food on the bioavailability of cilazapril at this dose would not be expected to be clinically significant.

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Influence of Food on the Bioavailability of Enalapril

Cited by 54 publications

References 9 publications

Flow-Injection Chemiluminescence Determination of Enalapril Maleate in Pharmaceuticals and Biological Fluids Using Tris(2,2′-bipyridyl)ruthenium(II)

Flow-Injection Chemiluminescence Determination of Enalapril Maleate in Pharmaceuticals and Biological Fluids Using Tris(2,2′-bipyridyl)ruthenium(II)

Bioequivalence evaluation of two brands of enalapril 20mg tablets (narapril and renitec) in healthy human volunteers

The influence of food on the pharmacokinetics and ACE inhibition of cilazapril.

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