• 제목/요약/키워드: cetirizine

검색결과 16건 처리시간 0.024초

Enantioselective Determination of Cetirizine in Human Urine by HPLC

  • Choi, Sun-Ok;Lee, Seok-Ho;Kong, Hak-Soo;Kim, Eun-Jung;Parkchoo, Hae-Young
    • Archives of Pharmacal Research
    • /
    • 제23권2호
    • /
    • 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.

  • PDF

Comparison of the Antihistaminic Activity Between Cetirizine Enantiomers

  • Park-Choo, Hae-Young;Choi, Sun-Ok;Lee, Seok-Ho
    • Biomolecules & Therapeutics
    • /
    • 제9권4호
    • /
    • 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.

  • PDF

개 피부에서 Histamine에 의한 팽진과 발적에 대한 loratadine, cetirizine과 terfenadine의 억제효과 (Effects of Loratadine, Cetirizine, and Terfenadine on Histamine-Induced Wheal and Erythema Responses in Normal Canine Skin)

  • Jeong, A-Young;Jeong, Hyo-Hoon;Heo, Woo-Phil;Eom, Ki-Dong;Jang, Kawng-Ho;Oh, Tae-Ho
    • 한국임상수의학회지
    • /
    • 제19권2호
    • /
    • pp.186-190
    • /
    • 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.

The effect of cetirizine, a histamine 1 receptor antagonist, on bone remodeling after calvarial suture expansion

  • Hwang, Soonshin;Chung, Chooryung J.;Choi, Yoon Jeong;Kim, Taeyeon;Kim, Kyung-Ho
    • 대한치과교정학회지
    • /
    • 제50권1호
    • /
    • pp.42-51
    • /
    • 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.

Indirect Determination of Cetirizine Hydrochloride by ICP-AES

  • Wang, Li-Sheng;Wei, Xiao-Ling;Gong, Qi;Jiang, Zhi-Liang;Li, Dong-Mei;Liang, Qing
    • Bulletin of the Korean Chemical Society
    • /
    • 제32권2호
    • /
    • 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.

암브록솔과 세티리진의 Cytochrome P450 저해 활성 평가 (In Vitro Assessment of Cytochrome P450 Inhibition by Ambroxol and Cetirizine)

  • 김봉희;류창선;장힘찬;이상윤;이지윤;채정우;권광일;김상겸
    • 약학회지
    • /
    • 제57권3호
    • /
    • pp.194-198
    • /
    • 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.

Bioequivalence Evaluation of Two brands of Cetirizine HCl 10 mg Tablets (Zyrix and Zyrtec) in Healthy Male Volunteers

  • Im, Ho-Taek;Won, Jong-Hoen;Cho, Sung-Hee;Lee, Heon-Woo;Park, Wan-Su;Rew, Jae-Hwan;Lee, Kyung-Tae
    • Journal of Pharmaceutical Investigation
    • /
    • 제35권5호
    • /
    • pp.355-360
    • /
    • 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.

알레르기성 비염 흰쥐모델에서 理中湯合敗毒散이 비염치료에 미치는 영향 (Therapeutic Effects of Lizhongtang plus Baidusan Extract in Rats with Allergic Rhinitis)

  • 이상문;최인화
    • 한방안이비인후피부과학회지
    • /
    • 제17권2호
    • /
    • pp.72-80
    • /
    • 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.

  • PDF

간헐적 발열 반응에 의한 세포 손상과 이와 관련된 탈모 치료를 위한 신 후보물질 연구 (Effects of Early Cell Damage from Repetitive Intermittent Fever Exposure in Alopecia Progression and Evaluation of New Candidate Drugs: Ibuprofen, Menthol, and Cetirizine)

  • 임성실;문홍섭
    • 한국임상약학회지
    • /
    • 제26권3호
    • /
    • pp.187-194
    • /
    • 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.

Narrowbore high-performance liquid chromatographic method for the determination of cetirizine in plasma using column switching

  • Hyun, Myung-Ja;Ban, Eunmi;Woo, Jong-Soo;Kim, Chong-Kook
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
    • /
    • pp.398.2-398.2
    • /
    • 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)

  • PDF