Comparative study of perindopril and perindopril metabolite pharmacokinetics using the HPLC/MS method

Perindopril is a prodrug which is converted to an active metabolite perindoprilat in the human organism. The present study led to the development of a fast and easily reproducible procedure for simultaneous detection of perinoprilat and its metabolite in plasma using HPLC with mass-spectrometric det...

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Bibliographic Details
Published inVedomosti Naučnogo centra èkspertizy sredstv medicinskogo primeneniâ (Online) no. 1; pp. 21 - 25
Main Authors L. M. Krasnykh, V. V. Smirnov, E. A. Egorenkov, G. F. Vasilenko, S. P. Dementyev, G. V. Ramenskaya
Format Journal Article
LanguageRussian
Published NEICON ISP LLC 01.02.2018
Subjects
bioequivalence
hplc-ms
perindopril
perindoprilat
pharmacokinetics
биоэквивалентность
вэжх-мс
периндоприл
периндоприлат
фармакокинетика
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Summary:Perindopril is a prodrug which is converted to an active metabolite perindoprilat in the human organism. The present study led to the development of a fast and easily reproducible procedure for simultaneous detection of perinoprilat and its metabolite in plasma using HPLC with mass-spectrometric detector (LC-MS). Detection of the target substance was performed using atmospheric pressure electrospray ionization (API-ES) techniques in negative polarity in two modes: SIM1, ion, m/z=368,10 for perindopril and SIM2, ion, m/z=339,30 for perindoprilat. Retention time of perindopril was about 2,4 min, for perindoprilat - about 1,4 min. Sample processing was performed using solid-phase extraction. The method’s limit of quantification was equal to 1 ng/ml for perindopril and 1 ng/ml for perindoprilat. The developed procedure was used to analyse pharmacokinetics and bioequivalence of medicines containing 8 mg of perindopril. Values of all calculated pharmacokinetic parameters had no statistically meaningful differences. Confidence intervals obtained fall within bioequivalence criterion (80-125% for AUC and 75-133% for Сmax и Cmax/AUC). The medicines under analysis were found to be bioequivalent.
ISSN:1991-2919
2619-1172