Dilution of maropitant (Cerenia) in lactated Ringer solution prolongs subcutaneous drug absorption and reduces maximum plasma concentration

Deborah E. Yee Faculty of Veterinary Medicine, University of Calgary, Calgary, AB, Canada

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 BSc
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Grace Ochigbo Faculty of Veterinary Medicine, University of Calgary, Calgary, AB, Canada

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 DVM, MSc
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Julie Menard Faculty of Veterinary Medicine, University of Calgary, Calgary, AB, Canada

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Brielle V. Rosa Faculty of Veterinary Medicine, University of Calgary, Calgary, AB, Canada

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 DVM, PhD

Abstract

OBJECTIVE

The aim of this study was to determine whether the pharmacokinetics of maropitant, administered SC as a commercially available maropitant-containing injectable product (Cerenia Injectable), differ when combined with lactated Ringer solution prior to administration.

ANIMALS

We used 6 adult spayed female Beagle dogs between 3 and 6 years of age, with a mean weight of 9.58 kg.

PROCEDURES

In this randomized crossover study, the dogs underwent 2 treatment protocols separated by a 14-day washout period: (1) an SC injection of 1 mg/kg of Cerenia Injectable (maropitant citrate; 10 mg/mL) and (2) 1 mg/kg of Cerenia Injectable diluted in 10 mL/kg of lactated Ringer injectable solution (LRS) given SC. Plasma maropitant concentrations were assessed by mass spectrometry. Pharmacokinetic analysis was performed using pharmacokinetic and pharmacodynamic data-analysis software to determine maximum plasma concentration (Cmax), time to reach maximum concentration, half-life, total exposure to the drug, mean residence time, clearance rate per fraction absorbed, and absorption and elimination kinetic parameters.

RESULTS

Cmax was reduced by 26% (P = .002), the absorption rate constant decreased 80% (P = .031), and the absorption half-life increased when Cerenia was administered diluted in LRS.

CLINICAL RELEVANCE

Administration of maropitant (Cerenia) diluted in LRS had a pharmacokinetic impact, resulting in a significantly reduced Cmax and slower absorption. Clinical efficacy was not assessed in this study.

Abstract

OBJECTIVE

The aim of this study was to determine whether the pharmacokinetics of maropitant, administered SC as a commercially available maropitant-containing injectable product (Cerenia Injectable), differ when combined with lactated Ringer solution prior to administration.

ANIMALS

We used 6 adult spayed female Beagle dogs between 3 and 6 years of age, with a mean weight of 9.58 kg.

PROCEDURES

In this randomized crossover study, the dogs underwent 2 treatment protocols separated by a 14-day washout period: (1) an SC injection of 1 mg/kg of Cerenia Injectable (maropitant citrate; 10 mg/mL) and (2) 1 mg/kg of Cerenia Injectable diluted in 10 mL/kg of lactated Ringer injectable solution (LRS) given SC. Plasma maropitant concentrations were assessed by mass spectrometry. Pharmacokinetic analysis was performed using pharmacokinetic and pharmacodynamic data-analysis software to determine maximum plasma concentration (Cmax), time to reach maximum concentration, half-life, total exposure to the drug, mean residence time, clearance rate per fraction absorbed, and absorption and elimination kinetic parameters.

RESULTS

Cmax was reduced by 26% (P = .002), the absorption rate constant decreased 80% (P = .031), and the absorption half-life increased when Cerenia was administered diluted in LRS.

CLINICAL RELEVANCE

Administration of maropitant (Cerenia) diluted in LRS had a pharmacokinetic impact, resulting in a significantly reduced Cmax and slower absorption. Clinical efficacy was not assessed in this study.

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