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Acta Medica Medianae
Vol. 51, No 4, December, 2012

UDK 61
ISSN 0365-4478(Printed version)
ISSN 1821-2794(Online)

 

Correspondence to:

Jadranka Odović

University of Belgrade

Faculty of Pharmacy

Department of Analytical Chemistry Vojvode Stepe 450, 11221 Belgrade, Serbia

E-mail: jodovic@pharmacy.bg.ac.rs

Original article                                                                                         

UDC: 615.355

doi:10.5633/amm.2012.0402

 

 

CORRELATION BETWEEN ANGIOTENSIN-CONVERTING ENZYME INHIBITORS LIPOPHILICITY AND PROTEIN BINDING DATA

 

          Jadranka Odović1 and Jasna Trbojević-Stanković2

 

                       University of Belgrade, Faculty of Pharmacy, Department of Analytical Chemistry, Belgrade, Serbia1

                       Clinical Center "Dr Dragiša Mišović", Department of Hemodialysis, Clinic of Urology, Belgrade, Serbia2

 

Angiotensin-converting enzyme (ACE) inhibitors represent a significant group of drugs primarily used in the treatment of hypertension and congestive heart failure. In this research, seven ACE inhibitors (enalapril, quinapril, fosinopril, lisinopril, cilazapril, ramipril, benazepril) were studied to evaluate the relationship between their protein binding and calculated (logP values) or ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS) and reversed-phase thin-layer chromatography (RP-TLC) lipophilicity data (j0, CHI or C0 parameters, respectively). Their protein binding data varied from negligible (lisinopril) to 99% (fosinopril), while calculated logPKOWWIN values ranged from -0.94 (lisinopril) to 6.61 (fosinopril). The good correlations were established between protein binding values and logPKOWWIN data (R2=0.7520) as well as between protein binding and chromatographic hydrophobicity data, j0, CHI or C0 parameters (R2 were 0.6160, 0.6242 and 0.6547, respectively). The possible application of hydrophobicity data in drugs protein binding evaluation can be of great importance in drug bioavailability. Acta Medica Medianae 2012;51(4):13-18.

 

      Key words: angiotensin-converting enzyme inhibitors (ACE inhibitors), protein binding,

lipophilicity