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Dexchlorpheniramine (maleate)

(Synonyms: 马来酸右氯苯那敏; S-(+)-Chlorpheniramine maleate salt) 目录号 : GC43427

A histamine H1 receptor antagonist

Dexchlorpheniramine (maleate) Chemical Structure

Cas No.:2438-32-6

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产品描述

Dexchlorpheniramine is a histamine H1 receptor antagonist with a pA2 value of 9.36 in guinea pig ileal tissue in vitro. [1] It inhibits the proliferation of previously sensitized, allergen-challenged peripheral blood mononuclear cells by 92% at a concentration of 4.8 µM. [2] Dexchlorpheniramine reduces noradrenaline uptake in the rat vas deferens ex vivo in response to tyramine stimulation when used at a concentration of 10 µM.[3]  In vivo, dexchlorpheniramine increases the pain threshold of mice exposed to thermal and chemical stimulation tests when administered intraperitoneally at a dose of 30 mg/kg.[4] Formulations containing dexchlorpheniramine have been used for the treatment of allergic reactions.

Reference:
[1]. Shamsa, F., Ahmadiani, A., and Khosrokhavar, R. Antihistaminic and anticholinergic activity of barberry fruit (Berberis vulgaris) in the guinea-pig ileum. J. Ethnopharmacol. 64(2), 161-166 (1999).
[2]. Holen, E., Elsayed, S., and Nyfors, A. The effect of H1 receptor antagonists on peripheral blood mononuclear cells, adenoid cells and primary cell lines. APMIS 103(2), 98-106 (1995).
[3]. Barnett, A., Symchowicz, S., and Taber, R.I. The effects of drugs inhibiting catecholamine uptake on tyramine and noradrenaline-induced contractions of the isolated rat vas deferens. Br. J. Pharmacol. 34(3), 484-492 (1968).
[4]. Farzin, D., Asghari, L., and Nowrouzi, M. Rodent antinociception following acute treatment with different histamine receptor agonists and antagonists. Pharmacol. Biochem. Behav. 72(3), 751-760 (2002).

Chemical Properties

Cas No. 2438-32-6 SDF
别名 马来酸右氯苯那敏; S-(+)-Chlorpheniramine maleate salt
化学名 γS-(4-chlorophenyl)-N,N-dimethyl-2-pyridinepropanamine, 2Z-butenedioate
Canonical SMILES ClC(C=C1)=CC=C1[C@H](CCN(C)C)C2=CC=CC=N2.OC(/C=C\C(O)=O)=O
分子式 C16H19ClN2•C4H4O4 分子量 390.9
溶解度 Slightly Soluble in DMSO, DMF, Chloroform, Methanol 储存条件 Store at -20°C
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1 mM 2.5582 mL 12.791 mL 25.582 mL
5 mM 0.5116 mL 2.5582 mL 5.1164 mL
10 mM 0.2558 mL 1.2791 mL 2.5582 mL
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Research Update

Simultaneous Assay of Dexchlorpheniramine maleate, Betamethasone, and Sodium Benzoate in Syrup by a Reliable and Robust HPLC Method

J Anal Methods Chem 2019 Nov 29;2019:2952075.PMID:31871819DOI:10.1155/2019/2952075.

The simultaneous determination of betamethasone, Dexchlorpheniramine maleate, and sodium benzoate in pharmaceutical syrup was done by using a simple validated HPLC method. The chromatographic separation of the three analytes was done in a C18 column maintained at 25°C, using a mixture of acetonitrile and 0.02 M phosphate buffer solution pH 2.70 (35 : 65, v : v) as mobile phase. The isocratic elution was chosen with total flow rate of mobile phase maintained at 1.0 mL per minute. The analytes were detected by a UV-Vis detector set at 254 nm. Injection volume was set at 50 μl. The method was fully validated in terms of specificity, linearity, precision, accuracy, and robustness according to requirements of current guidelines and was proven to be suitable for the intended application.

Ultraviolet A photosensitivity profile of Dexchlorpheniramine maleate and promethazine-based creams: Anti-inflammatory, antihistaminic, and skin barrier protection properties

J Cosmet Dermatol 2017 Dec;16(4):e59-e67.PMID:28593645DOI:10.1111/jocd.12349.

Background: Unwanted side effects such as dryness, hypersensitivity, and cutaneous photosensitivity are challenge for adherence and therapeutical success for patients using treatments for inflammatory and allergic skin response. Aims: In this study, we compared the effects of two dermatological formulations, which are used in inflammatory and/or allergic skin conditions: Dexchlorpheniramine maleate (DCP; 10 mg/g) and promethazine (PTZ; 20 mg/g). Methods: We evaluated both formulations for phototoxicity potential, skin irritation, anti-inflammatory and antihistaminic abilities, and skin barrier repair in vitro and ex vivo using the standard OECD test guideline n° 432, the ECVAM protocol n° 78, and cultured skin explants from a healthy patient. Ultraviolet A was chosen as exogenous agent to induce allergic and inflammatory response. Results: Both PTZ and DCP promoted increases in interleukin-1 (IL-1) synthesis in response to ultraviolet A (UVA) radiation compared to control. However, the increase observed with PTZ was significantly greater than the DCP, indicating that the latter has a lower irritant potential. DCP also demonstrated a protective effect on UVA-induced leukotriene B4 and nuclear factor kappa B (NF-κB) synthesis. Conversely, PTZ demonstrates more robust UVA antihistaminic activity. Likewise, PTZ promoted a significantly greater increase in the production of involucrin and keratin 14, both associated with protective skin barrier property. Conclusion: In conclusion, these data suggest possible diverging UVA response mechanisms of DCP and PTZ, which gives greater insight into the contrasting photosensitizing potential between DCP and PTZ observed in the patients.

Development of a validated capillary electrophoresis method for enantiomeric purity testing of Dexchlorpheniramine maleate

J Chromatogr A 2002 Jun 7;958(1-2):291-7.PMID:12134827DOI:10.1016/s0021-9673(02)00314-x.

A capillary zone electrophoresis method has been developed for the detection of 0.1% of (R)-levochlorpheniramine maleate in samples of (S)-dexchlorpheniramine maleate. Using 1.5 mM carboxymethyl-beta-cyclodextrin in an acidic background electrolyte, resolution values of more than 10 were obtained. Under these conditions the R-enantiomer is migrating in front of the bulk S-enantiomer. The assay was validated for linearity (2-10 microg/ml; R2 = 0.9992), selectivity [(RS)-pheniramine maleate and (RS)-brompheniramine maleate], limit of detection (0.25 microg/ml), limit of quantification (0.75 microg/ml), analytical precision (intra- and inter-day variability), repeatability of the method (RSD = 5.0%) and accuracy. In samples of Dexchlorpheniramine maleate from two different manufacturers, concentrations of, respectively, 0.15% and 1.95% (m/m) of levochlorpheniramine maleate were detected. The method was compared to the HPLC method described in the European Pharmacopoeia III monograph.

A comparative study of Dexchlorpheniramine maleate sustained release tablets and budesonide nasal spray in seasonal allergic rhinitis

Allergy 1983 Oct;38(7):517-24.PMID:6139040DOI:10.1111/j.1398-9995.1983.tb02361.x.

It was the aim of the study to compare the efficacy and side effects of oral antihistamine and nasal glucocorticoid therapy in seasonal allergic, rhinitis. In a double blind, double-dummy, group-comparative study, 61 adult grass pollen allergic patients were either treated with Dexchlorpheniramine maleate sustained release tablets (6 mg b.d.), or with budesonide nasal spray (200 micrograms b.d.). After a 1-week run-in period, treatment was given for 3 weeks in the grass pollen season. Patients treated with budesonide showed significantly less nasal blockage than those who received Dexchlorpheniramine (P less than 0.05), but there was no difference in the number of sneezes and nose blowings. Patients treated with budesonide and a larger quantity of antihistamine-vasoconstrictor eye drops (P less than 0.01). Drowsiness occurred in the group that was treated with Dexchlorpheniramine, but mainly during the first week of treatment. The side effects caused by the budesonide spray were few and insignificant. The patients' overall assessment of the treatment favoured the glucocorticoid spray (P = 0.06).

Derivative ultraviolet spectrophotometric determination of Dexchlorpheniramine maleate in tablets in presence of coloring agents

Farmaco 2005 Nov-Dec;60(11-12):900-5.PMID:16226263DOI:10.1016/j.farmac.2005.08.009.

Formulation excipients can frequently affect the drug analysis in pharmaceuticals yielding background interference by ultraviolet spectrophotometry. Sample separation procedures to diminish such interferences are usually recommended as sample pre-treatment, however it can be difficult to eliminate them and they can still persist. In addition, these procedures can be time consuming and laborious to perform. Excipients, like dyeing agents can also be present in a formulation and yield color to drug solution. This work reports the successful development of a derivative ultraviolet spectrophotometry for Dexchlorpheniramine maleate (DPM) determination in solid dosage forms, in spite of the color imparted to tablets solution. Standard curves obtained by second order derivative ultraviolet spectrophotometry showed linearity with a correlation coefficient of 0.9999 in the concentration range of 9.75-32.5 microg ml(-1) DPM in 0.1 mol l(-1) sulfuric acid, using zero-peak (ZP) and peak-peak (PP) methods. The average relative standard deviation range was between 0.26% and 1.08% and 0.18% and 0.63% for ZP and PP methods, respectively. Application of the method in tablet samples resulted in coefficients of variation in the range of 0.83-1.40%, and 0.63-0.83% for ZP and PP methods, respectively. Recovery test percentage values obtained were between 96.95% and 105.61% for the tested tablet samples.