• Biomolecules & Therapeutics
• /
• v.9 no.4
• /
• pp.282-284
• /
• 2001

The antiallergic drug, cetirizine, inhibits the histamine release from a rat basophilic leukemia (RBL-2H3) cell line, which is frequently used as a mast cell model. By investigating inhibitory activities of (+)- and (-)-cetirizine in RBL-2H3 cells on the histamine release, we aimed to evaluate the effect of their structual characteristics on the antihistamine activity. The study on RBL-2H3 cell has clearly demonstrated that the (-)-cetirizine is significantly more potent than the (+)- or the racemic cetirizine, although there was no difference in pharmacokinetics between (+)- and (-)-cetirizine in rats.

• Archives of Pharmacal Research
• /
• v.23 no.2
• /
• pp.178-181
• /
• 2000

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 $\alpha$$_1$-acidglycoprotein, the AGP-CSP was used to separate the enantiomers. The pH of the phosphate buffer, as well as the content of the organic modifier in the mobile phase, markedly affected the chromatographic separation of (+)- and (-)-cetirizine. A mobile phase of 10 m㏖/1 phosphate buffer (pH 7.0)-acetonitrile (95 : 5, v/v) was used for the urine assays. Ultraviolet absorption was monitored at 230nm and roxatidine was employed as the internal standard for quantification. (+)-Cetirizine, (-)-cetirizine and the internal standard were eluted at retention times of 12, 16, and 32 mins, respectively. The detection limit for cetirizine enantiomers was 400 ng/$m\ell$ 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 ${\mu}g/ml$. 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.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.2
• /
• pp.595-598
• /
• 2011

Cetirizine hydrochloride reacted with $BiI_4^-$ in an acidic aqueous solution to form precipitate. After centrifugation, the atomic emission intensity of $Bi^{3+}$ contained in the supernatant solution was measured at the characteristic wavelength of 206.170 nm. The difference between the spectral signal intensity of the blank solution and that of the supernatant, ${\Delta}I$, was linearly related to the concentration of cetirizine hydrochloride. As a result, a new inductively coupled plasmaatomic emission spectrometric (ICP-AES) method was developed for the analysis of cetirizine hydrochloride. The linear range was from 27.7 to 184.8 $mg{\cdot}L^{-1}$, with a correlation coefficient (r) of 0.9961 and a detection limit of 9.6 $mg{\cdot}L^{-1}$. This method is simple and accurate, Without using toxic organic solvents, and is feasible for the quality control of cetirizine hydrochloride tablets and capsules.

• Journal of Veterinary Clinics
• /
• v.19 no.2
• /
• pp.186-190
• /
• 2002

This crossover study was performed in order to compare the effects of cetirizine, loratadine, and terfenadine in canine skin. Five healthy dogs were used. Cetirizine 0.5 mg/kg, loratadine 5 mg/kg and terfenadine 5 mg/kg were administered orally 4 hours before the experiment. Erythema indices and wheal size were assessed by Hexameter ($MX^{\circledR}$ 18, CK, Germany) and skin reaction guide, respectively. Cetirizine-induced erythema inhibition was generally higher than other drugs and was significantly different from placebo. Cetirizine was superior to placebo at 3, 4, 5, 6, 7, and 8 minutes (p< 0.01). Cetirizine also was superior to placebo at 9 minutes (p< 0.05). Loratadine and terfenadine erythema inhibition were better than after placebo treatment from 4 to 9 minutes, but erythema index of terfenadine at 7 minutes was not observed probability of 95% and 99%. At 10 minutes, intradermal injection of the histamine caused a mean wheal dimension for placebo, cetirizine, loratadine and terfenadine, which were 13.25$\pm$0.75 mm,7.5$\pm$ 1.02 mm (53% reduction, p<0.007),6.2$\pm$0.58 mm(43% reduction, p <0.01), and 8.4 $\pm$0.67 mm(37% reduction, p< 0.05), respectively, comparing with placebo. Loratadine and cetirizine were good antihistamines for clinical therapy for atopic dermatitis in dog.

• Microbiology and Biotechnology Letters
• /
• v.50 no.4
• /
• pp.512-521
• /
• 2022

Since the main symptoms of COVID-19 involve the respiratory system, the infection rate of this disease is predicted to be higher in patients with other respiratory conditions such as allergic rhinitis. In such a situation, it will be meaningful to conduct research on an allergy treatment that has fewer side effects and can effectively reduce allergy symptoms. Here, we prepared experimental samples under various fermentation conditions with mixed extracts of six medicinal plants. To examine the anti-allergic efficacy of these samples, an egg albumin-induced allergic rhinitis animal model experiment, a serum histamine and IgE experiment, and a COX and LO inhibitory activity experiment were conducted. As a result of animal experiments, OVA+SP-4 showed superior efficacy compared to OVA+SP-1 in nasal rubbing and sneezing experiments and had anti-allergic efficacy similar to that of OVA-cetirizine. The serum histamine concentration of OVA+SP-4 was also 1.3 times higher than that of the OVA+cetirizine group, showing a high histamine reduction ability, and IgE showed the same trend. An analysis of COX inhibitory efficacy also confirmed that COX-1 and COX-2 inhibitory efficacy is high, and the longer the fermentation time, the higher the antiallergic efficacy. The composition proposed by this study is expected to have a significant effect on sustainable allergy prevention and treatment in the future by applying it to human patients.