Naslov
Semi-preparative chromatographic purification of the enantiomers S-(−)-amlodipine and R-(+)-amlodipine

Autori
Lukša, J ; Josić, Dj ; Podobnik, B ; Furlan, B ; Kremser, M

Izvornik
Journal of Chromatography B: Biomedical Sciences and Applications (0378-4347) 693 (1997), 2; 367-375

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Enantiomer separation ; Amlodipine

Sažetak
Pharmacokinetic studies of optically pure compounds after single enantiomer administration are becoming increasingly important. The process of racemization in vivo can diminish all expected advantages of single enantiomer treatment. Amlodipine, one of the calcium channel blockers, currently used in therapy as a racemate, is one of such drugs under study. In order to administer single enantiomers of amlodipine to healthy volunteers both were chromatographically purified and characterised. The two optical isomers of amlodipine, active S-(−)- and non-active R-(+)-amlodipine, were purified using chromatographic procedure adopted from the analytical separation. Enantiomers were successfully converted to benzenesulphonic salt without any racemization. All semi-preparative purifications were monitored with complementary analytical methods, HPLC and CE, along with the determination of optical activity so that the final product was sufficiently defined for further in vivo studies. The analytical method developed for the determination of plasma concentrations of each enantiomer of amlodipine in these studies is also briefly described.

Izvorni jezik
Engleski

Znanstvena područja
Biotehnologija u biomedicini (prirodno područje, biomedicina i zdravstvo, biotehničko područje)

POVEZANOST RADA