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

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

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

• The korean journal of orthodontics
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• v.50 no.1
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• pp.42-51
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• 2020

Objective: The objective of this study was to evaluate the effects of cetirizine, a histamine 1 receptor antagonist, on bone remodeling after calvarial suture expansion. Methods: Sixty male Sprague-Dawley rats were divided into 4 groups; the phosphate-buffered saline (PBS)-injected no expansion group, cetirizine-injected no expansion group, PBS-injected expansion group, and cetirizine-injected expansion group, and were observed at 7, 14, and 28 days. Five rats per group were examined at each observation day. Daily injections of cetirizine or PBS were administered to the relevant groups starting 2 weeks prior to expander insertion. A rapid expander was inserted in the calvarial bone to deliver 100 cN of force to the parietal suture. The specimens were prepared for hematoxylin and eosin and tartrate-resistant acid phosphatase (TRAP) staining. Suture opening and bone regeneration were evaluated using microcomputed tomography and bone histomorphometric analysis. Serum blood levels of osteocalcin and carboxy-terminal collagen crosslinks (CTX) were also evaluated. Results: TRAP-positive cell counts and CTX levels decreased while osteocalcin levels increased in the cetirizine-injected expansion group at observation day 28. In the expansion groups, the mineralized area gradually increased throughout the observation period. At day 28, the cetirizine-injected expansion group showed greater bone volume density, greater mineralized area, and narrower average suture width than did the PBS-injected expansion group. Conclusions: Cetirizine injection facilitated bone formation after suture expansion, mostly by suppressing osteoclastic activity. Histamine 1 receptor antagonists may aid in bone formation after calvarial suture expansion in the rat model.

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

• YAKHAK HOEJI
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• v.57 no.3
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• pp.194-198
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• 2013

In the present study we evaluated drug-drug interaction potential of ambroxol and cetirizine mediated by inhibition of CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 using pooled human liver microsomes (HLMs). As measured by liquid chromatography-electrospray ionization tandem mass spectrometry, cetirizine and ambroxol inhibited significantly CYP2E1 but the maximal inhibition was approximately 36% at 10 ${\mu}M$ cetirizine and 28% at 3 ${\mu}M$ ambroxol. In addition, CYP2D6 activity was decreased to approximately 83% of control activity in pooled HLM incubated with 3 ${\mu}M$ ambroxol. Activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, and CYP3A4 were not significantly inhibited by cetirizine and ambroxol. Considering their maximal plasma concentration in human ($C_{max}$ of cetirizine is approximately 0.67 ${\mu}M$ and $C_{max}$ of ambroxol is 0.044 ${\mu}M$), these two drugs have very low possibility in drug-drug interaction by CYP inhibition in clinical situations.

• Journal of Pharmaceutical Investigation
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• v.35 no.5
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• pp.355-360
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• 2005

The purpose of the present study was to evaluate the bioequivalence of two cetirizine HCl tablets, Zyrtec tablet (UCB Pharm. Co., Ltd. Korea, reference product) and Zyrix tablet (Kukje Pharm. Co., Ltd., Korea, test product), according to the guidelines of Korea Food and Drug Administration (KFDA). After adding an internal standard (diazepam), plasma samples were extracted using 1 mL of dichloromethane. Compounds extracted were analyzed by reverse-phase HPLC with ultra-violet detector. This method for determination cetirizine is proved accurate and reproducible with a limit of quantitation of 10 ng/mL in male plasma. Twenty-four healthy male Korean volunteers received each medicine at the cetirizine HCl dose of 10 mg in a $2{\times}2$ crossover study. There was a one-week wash out period between the doses. Plasma concentrations of cetirizine were monitored for over a period of 24 hr after the administration. AUC (the area under the plasma concentration-time curve) was calculated by the linear trapezoidal rule. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed AUC and $C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals for the log transformed data were acceptable range of log 0.8 to log 1.25 $(e.g.,\;log\;0.93-log\;1.08\;for\;AUC_{0-t},\;log\;0.91-log\;1.08\;for\;AUC_{0-{\infty}}\;and\;log\;1.01-log\;1.11\;for\;C_{max})$. The major parameters, AUC and $C_{max}$ met the criteria of KFDA for bioequivalence indicating that Zyrix tablet is bioequivalent to Zyrtec tablet.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.17 no.2
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• pp.72-80
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• 2004

Background and Objectives: Recently the incidence of allergic rhinitis has increased but treatment in most cases has only dealt with the symptoms. Medicine has been developed that shows fewer side effects. However, some side effects and the psychological stress over taking medicine have remained. There have been no studies so far performed on the effect of Lizhongtang plus Baidusan Extract. This study aimed to find out the therapeutic effects of its exclusive use in rats with Allergic Rhinitis. Materials and Methods : Thirty Sprague-Dawley rats were divided into three groups: the control group, the cetirizine HCI group and the sample group. To induce allergic rhinitis in the control group, the cetirizine HCI group and the sample group, rats were sensitized intraperitoneally with 0.1$\%$ ovalumin solution 3 times at an interval of I week. Then intranasal sensitization was performed by diffusing 0.1$\%$ ovalumin solution 3 times at an interval of 2 days. After that time, rats of the cetirizine HCI group were orally administered with cetirizine HCI. Rats of the sample group were treated with Lizhongtang plus Baidusan Ex. for 28 days. We observed changes in nasal mucosa and submucosa. Also we found changes in the segment of neutrophil and lympocyte in Leukocyte. We used the statistical methods of ANOVA test(p 〈0.05). Results: The loss of the cilium and the secretion of mucus in the treated group was rare when compared to control group. Effects of Lizhongtang plus Baidusan Ex. on the liver function were also studied in rats. Treatment of Lizhongtang plus Baidusan Ex. did not affect AST and ALT. The segment of neutrophil was significantly increased in the treated group when compared with the control group and the cetirizine HCI group(p 〈0.05). The segment of lympocyte was significantly decreased in the treated group when compared with the control group and the cetirizine HCI group(p 〈0.05). Conclusion: This study shows that Lizhongtang plus Baidusan Ex. decreases the inflammatory response in rats with Allergic Rhinitis.

• Korean Journal of Clinical Pharmacy
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• v.26 no.3
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• pp.187-194
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• 2016

Background: Alopecia areata (AA) is a very disturbing and expensive disorder in which the exact etiology is not known and it is yet to be treated completely well. Most alopecia patients exhibit some inflammation in the hair follicles regardless of the causes. The clinical symptoms of alopecia present very diversely while the prime symptom is local intermittent fever which are related to inflamed cells. Methods: This study aimed to evaluate how repetitive intermittent fever can damage the normal human dermal fibroblast (NHDF) cells and investigated the cytotoxic and proliferative effects after application of new candidate drugs (ibuprofen, menthol, cetirizine) for alopecia in comparison to minoxidil. Results: This study demonstrated that ibuprofen, menthol, or/and cetirizine can prevent or slow down the damage of NHDF cells from intermittent fever in early alopecia. Aggressive preventative intervention with those drugs before complete destruction of hair follicle by excessive repetitive fever, is a very important step for alopecia therapy and these drugs are recommended as candidate drugs for alopecia in the future. Conclusion: Aggressive preventative intervention with drugs before complete destruction of hair follicles (NHDF cells) by excessive repetitive fever is a very important step for alopecia therapy or progression.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.398.2-398.2
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• 2002

A column switching HPLC assay was developed to allow the separation and quantitation of cetirizine in human plasma by ultraviolet (UV) detection. Plasma samples were prepared by liquid-liquid extraction. After drying, the residue was reconstituted in 20 mM phosphate buffer (pH 2.8) containing 15% acetonitrile. The samples were initially injected onto a clean-up Capcell Pak MF C18 column. (50 mm $\times$ 4.6 mm I.D.), and the chromatographic region containing the peaks of interest was followed in an analytical C18 microcolumn (250 mm$\times$1.5 mm I. D.) via column switching device. (omitted)