Naslov
Lipophilicity Characterization of Statin Drugs by Reversed-Phase High Performance Liquid Chromatograhy

Autori
Mornar, Ana ; Nigović, Biljana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
New Achievements in Chromatography, Book of Abstracts / N. Šegudović - Zagreb : ITG d.o.o., za izdavačku i grafičku djelatnost, 2008, 121-121

ISBN
978-953-6894-36-9

Skup
14th International Symposium on Separation Science, New Achievements in Chromatography

Mjesto i datum
Primošten, Hrvatska, 30.09.2008. - 03.10.2008

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
Reversed-phase high performance liquid chromatograhy; statin drugs; lipophilicity characterization

Sažetak
Lipophilicity is one of the major factors that influences the transport, absorption, and distribution of drugs in biological systems, and it is an important parameter in evaluating the drugs´ pharmacodynamic, pharmacokinetic and toxic profiles. RP-HPLC has been long recognized as a potential method for lipophilicity determination, where mainly hydrophobic forces dominate the retention process. In our work we have investigated the lipophilicity of six statin drugs using RP-HPLC method: lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, and rosuvastatin. The HPLC measurements were performed using Agilent 1100 LC System. The columns used were: Zorbax SB-C18 (4.6 mm x 250 mm, particle size 5 μ m), and Hypersil (4.6 mm x 150 mm, particle size 5 μ m). The binary solvent system (acetonitrile – water) was used as a mobile phase with a varying content of organic modifier (80 - 20%, increment 5%). The solvents were filtered through cellulose nitrate filter (0.45 μ m). The flow-rate was 1 mL/min at constant temperature (25 &ordm ; C). The samples were prepared as solutions of 0.1 mg/mL and the injection volume was 5 μ L. The void volume was measured by injecting acetone together with the sample. The optimum wavelength was set for each compound, according to maximum absorption in the UV spectra. All experiments were performed in duplicate. The logarithm of capacity factors were calculated from experimentally determined retention data: log k = log [(tr – t0)/t0], where tr and t0 are the retention times of the solute and of an unretained compound, respectively. The linear and polynomial relationships between the logarithm of capacity factor (log k) and the organic modifier concentration (φ ) in the mobile phase were investigated in order to predict the logarithm of capacity factors of selected statin drugs in the pure water as mobile phase (log kw). The extrapolated values characterize the partition of the compound between the non-polar stationary phase and water as a mobile phase. Also, the volume fractions of the organic modifier in the mobile phase for which retention (log k) is zero were calculated using liner relationship (φ 0). Log kw values obtained using Zorbax column were in the range from 2.060 to 2.817, while values obtained using Hypersil column were in the range from 2.037 to 2.935. Our findings suggest the usefulness of the chromatographic method in the fast characterization of the lipophilicity of statin drugs.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

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