Enantioselective determination of cetirizine in human urine by HPLC

Abstract

In order to study the simultaneous determination of (+)- and (-)-cetirizine in human urine we have developed a chiral separation method by HPLC. A chiral stationary phase of alpha1-acidglycoprotein, the AGP-CSP, was used to separate the enantiomers. The pH of the phosphate buffer, as well as the content of the organic modifier in the mobile phase, markedly affected the chromatographic separation of (+)- and (-)-cetirizine. A mobile phase of 10 mmol/l phosphate buffer (pH 7.0)-acetonitrile (95: 5, v/v) was used for the urine assays. Ultraviolet absorption was monitored at 230 nm and roxatidine was employed as the internal standard for quantification. (+)-Cetirizine, (-)-cetirizine and the internal standard were eluted at retention times of 12, 16, and 32 mins, respectively. The detection limit for cetirizine enantiomers was 400 ng/ml of urine. A pharmacokinetic study was conducted with the help of 5 healthy female volunteers who were administered with a single oral dose of racemic cetirizine (20 mg). The peak area ratios provided by the cetirizine enantiomers were linear (r>0.997) over a concentration range of 2.5-200 microg/ml. The peak of the excreted cetirizine enantiomers appeared in the urine sample during the period of 1-2 hrs following the administration of the oral dose. The excreted level of (+)-cetirizine was slightly higher than (-)-cetirizine but the difference was not statistically significant. However, this method appears to have applications for enantioselective pharmacokinetic studies of racemic drugs.

Comparison of HPLC and CE methods for the determination of cetirizine dihydrochloride in human plasma samples

“…Although the total separation times were 6 and 9 min for HPLC and CE, respectively, method development was faster with CE since it did not require extensive equilibration times compared with HPLC columns. Concerning analysis time, both methods offer substantial advantages in comparison with earlier investigations that analyzed cetirizine in plasma samples (Benedetti et al, 2001;Macek et al, 1999;Choi et al, 2000b;Basavaiah and Charan, 2002).…”

“…There are only a few reports on the cetirizine analysis in human (Macek et al, 1999;Kim et al, 2005;Nagaralli et al, 2003;de Jager et al, 2002;Song et al, 2005;Tan et al, 2006;Baltes et al, 1988;Pandya et al, 1996) or animal plasma samples (Choi et al, 2000a;Gupta et al, 2005), which have been based on HPLC following some form of liquid-liquid extraction (LLE) (Macek et al, 1999;Choi et al, 2000a;Kim et al, 2005;Nagaralli et al, 2003;Gupta et al, 2005;de Jager et al, 2002;Tan et al, 2006) or solidphase extraction (SPE) (Song et al, 2005). Some methods have been described for quantitation of cetirizine also in serum (Zaater et al, 2000;Moncrieff, 1992), blood (Gergov et al, 2001), urine (Choi et al, 2000b;Rosseel and Lefebvre, 1991) or brain tissues (Gupta et al, 2005). It is possible to find in the literature several articles on stereoselective investigation of cetirizine in biological material (Choi et al, 2000a, b;Gupta et al, 2005).…”

Enantioselective analysis of cetirizine in pharmaceuticals by cyclodextrin‐mediated capillary electrophoresis

“…Previously, CET enantiomers have been separated and determined by HPLC using a chiral stationary phase of alpha(1)-acid glycoprotein [25,26] and polysaccharidederived chiral stationary phases [27,28]. The pH of the buffer, as well as the content of the organic modifier in the mobile phase, markedly affected the chromatographic separation of CET enantiomers.…”

Liquid chromatographic determination of ceterizine hydrochloride and paracetamol in human plasma and pharmaceutical formulations

“…CTZH is official in European Pharmacopoeia [1], while PARA is official in United States Pharmacopoeia [2]. Many HPLC methods have been reported for the determination of CTZH [3][4][5][6][7][8][9][10][11][12] and PARA [13][14][15][16][17][18][19][20][21][22][23][24][25][26] in biological fluids or in pharmaceutical formulations. But, none of these methods demonstrate the simultaneous quantification of these two drugs in combination in human plasma and pharmaceutical preparations.…”

“…Moreover, the reported methods are not satisfactory for routine quality assurance for one or the other reason. Some of these methods have low sensitivity [3,7,9,[13][14][15][16][17][18][19][21][22][23] or works out only at higher concentrations of the drugs [7,10,14,[16][17][18][19][21][22][23] or need more time for analysis [11,17]. Hence, it was felt necessary to develop a simple and sensitive HPLC method, which does not suffer from the above limitations for the determination of binary combination of CTZH and PARA in human plasma and pharmaceutical formulations.…”