• Biomolecules & Therapeutics
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• 제9권4호
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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.

• Archives of Pharmacal Research
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• 제23권2호
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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.

• Bulletin of the Korean Chemical Society
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• 제32권2호
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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.

• 한국임상수의학회지
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• 제19권2호
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• pp.186-190
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• 2002

아토피성 피부염은 면역계재성 피부질환으로 소양증이 주요 증상이며 이의 치료가 필수적이다. 따라서 개에서 제2세대 항히스타민제의 임상적용을 위해 피부에 히스타민에 의해 유발된 팽진과 발적에 대한 loratadine, cetirizine과 terfenadine의억제 효과를 비교하였다. 3종의 항히스타민제는 대조군에 비해 매우 유의하게 발적반응을 억제하였으며(p<0.01) cetirizine이 다른 제제에 비해 높은 억제효과를 보였다. 3종의 항히스타민제는 팽진 반응을 억제하는 효과를 보였으며 loratadine의 억제효과가 일정하며 지속적이었다. 따라서 제 2세대 항히스타민제인 loratadine과 cetirizine은 개에서 아토피성 피부염의 소양증 치료에 적용할 수 있는 항히스타민제로 사료된다. 특히 스테로이드제제를 대체할 수 있는 치료효과를 보일 것으로 판단된다.

• 한국미생물·생명공학회지
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• 제50권4호
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• pp.512-521
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• 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.