• The Korean Journal of Physiology and Pharmacology
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• v.13 no.3
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• pp.215-220
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• 2009

Chlorpheniramine is a potent first-generation histamine $H_1$ receptor antagonist that can increase action potential duration and induce QT prolongation in several animal models. Since block of cardiac human ether-a-go-go-related gene (hERG) channels is one of leading causes of acquired long QT syndrome, we investigated the acute effects of chlorpheniramine on hERG channels to determine the electrophysiological basis for its proarrhythmic potential. We examined the effects of chlorpheniramine on the hERG channels expressed in Xenopus oocytes using two-microelectrode voltage-clamp techniques. Chlorpheniramine induced a concentration-dependent decrease of the current amplitude at the end of the voltage steps and hERG tail currents. The $IC_{50}$ of chlorpheniramine-dependent hERG block in Xenopus oocytes decreased progressively relative to the degree of depolarization. Chlorpheniramine affected the channels in the activated and inactivated states but not in the closed states. The S6 domain mutations Y652A and F656A partially attenuated (Y652A) or abolished (F656A) the hERG current block. These results suggest that the $H_1$ antihistamine, chlorpheniramine is a blocker of the hERG channels, providing a molecular mechanism for the drug-induced arrhythmogenic side effects.

• Journal of Pharmaceutical Investigation
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• v.5 no.4
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• pp.32-37
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• 1975

The intentional test of the clinical test on the mouse, which are orally administered salicylamide combined with chlorpheniramine maleate were made by writhing syndrome method of 0.7% acetic acid-saline solution and following effects were found. 1) The cross-over test of writhing syndrome method have intention in case of three days rest after the first examination. 2) The most active rate of salicylamide by administration combined with chlorpheniramine maleate is salicylamide 20mg/kg: chlorpheniramine maleate 20mg/kg (1:1) 3) The most active range of chlorpheniramine maleate used for assistant action of salicylamide is $15mg/kg{\sim}20mg/kg$

• Journal of Pharmaceutical Investigation
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• v.6 no.2
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• pp.58-68
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• 1976

120 tablets of 25mg phenformin hydrochloride tablet and 4mg chlorpheniramine maleate tablet, respectively, were assayed and analyzed to obtain basic data on the content uniformity of domestic pharmaceuticals. All of the tablets of phenformin hydrochloride and that of chlorpheniramine maleate were met the requirements of the test for weight variation and content but no regularity was found in the content unformity specifications. In case of chlorpheniramine maleate tablets, standard deviation of active ingredient content of B maker was 4.1% and that of C maker 7.1%.

• Journal of Pharmaceutical Investigation
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• v.10 no.1
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• pp.4-12
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• 1980

The studies of the compounding analgestic antipyretics were examined by the converted Koster's method (mice) and the converted Mac Donald's method (mice) induced on the three assumption crossover test. And the following results were found. 1. The same effect of the writhing inhibition in this compounding antipyretic dosage by it's oral administration is as follows. Aminopyrine 100mg/kg. (standard), aminopyrine 50mg/kg compounding with chlorpheniramine maleate 2mg/kg., compounding with diphenhydramine hydrochloride 8mg/kg., compounding with atropine sulfate 0.2mg/kg., or compounding with scopolamine hydrobromide 0.2mg/kg. And aspirin80mg/kg., Salicylamide 90mg/kg., sulpyrine 60mg/kg., or phenacetin 70mg/kg. compounding with the same dosage of the adjutants above. 2. The elevation-rate of the reaction threshold in this compounding antipyretic dosage by it's oral administration calculate as follows. When the elevation-rate (ER) of aminopyrine (100mg./kg.) is 1.00 (Standard), ER of aminopyrine (50mg./kg.) compounding with chlorpheniramine maleate (2mg./kg.) calculated 1.42, aspirin (80.mg./kg.) compounding with diphenhydramine hydrochloride (80mg./kg.) calculated 1.18, salicylamide (90mg./kg.) compounding with chlorpheniramine maleate (2mg./kg.) calculated 1.15, sulpyrine (60mg./kg.) compounding with chlorpheniramine maleate(2mg./kg.) calculated 1.28, and ER phenacetin (70mg./kg.) compounding with chlorpheniramine maleate (2mg./kg.) calculated 1.19.

• Journal of Pharmaceutical Investigation
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• v.1 no.1
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• pp.58-61
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• 1971

Comparatives studies were made on stabilities of some hormons, used individually and combined with some stabilizers, and the following results were found. 1. The increasing order of antiallergic hormons (prednisolone, dexamethasone) to the stabilities as follows : Chlorpheniramine>Menadione>Inositol>Ascorbic acid. 2. The increasing order of sulfonylureas in as follows : Chlorpheniramine>Thiamine>Inositol>Ascorbic acid.

• Carbon letters
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• v.19
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• pp.12-22
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• 2016

Date palm leaflets were used as a precursor to prepare dehydrated carbon (DC) via phosphoric acid treatment at 150℃. DC, acidified with H₃PO₄, was converted to activated carbon (AC) at 500℃ under a nitrogen atmosphere. DC shows very low surface area (6.1 m²/g) while AC possesses very high surface area (829 m²/g). The removal of lisinopril (LIS) and chlorpheniramine (CP) from an aqueous solution was tested at different pH, contact time, concentration, and temperature on both carbons. The optimal initial pH for LIS removal was 4.0 and 5.0 for DC and AC, respectively. However, for CP, initial pH 9.0 showed maximum adsorption on both carbons. Adsorption kinetics showed faster removal on AC than DC with adsorption data closely following the pseudo second order kinetic model. Adsorption increases with temperature (25℃–45℃) and activation energy (E_a) is in a range of 19–25 kJ mol/L. Equilibrium studies show higher adsorption on AC than DC. Thermodynamic parameters show that drug removal is endothermic and spontaneous with physical adsorption dominating the adsorption process. Column adsorption data show good fitting to the Thomas model. Despite its very low surface area, DC shows ~70% of AC drug adsorption capacity in addition of being inexpensive and easily prepared.

• YAKHAK HOEJI
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• v.33 no.3
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• pp.141-148
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• 1989

The weak UV absorbing antihistaminics such as chlorpheniramine, triprolidine, tripelennamine and diphenhydramine were analyzed by charge-transfer spectrophotometric method. The results obtained are summarized as folows. It was possible to determine a weak UV absorbing antihistaminics using the intense charge-transfer UV bands in chloroform. Charge transfer complexes were formed in a 1:1 ratio between antihistaminics and iodine in chloroform. Linear relationship was found between absorbance and concentration in the range of $1.0\;{\times}\;10^{-5}M-5.0\;{\times}\;10^{-5}M$ for chlorpheniramine( ${\varepsilon}\;=\;2.082\;{\times}\;10^4$) and tripelennamine ( ${\varepsilon}\;=\;1.578\;{\times}\;10^4$), $1.0\;{\times}\;10^{-5}M-8.0\;{\times}\;10^{-5}M$ for triprolidine ( ${\varepsilon}\;=\;1.120\;{\times}\;10^4$) and $1.0\;{\times}\;10^{-5}M-1.0\;{\times}\;10^{-4}M$ for diphenhydramine ( ${\varepsilon}\;=\;9.900\;{\times}\;10^3$). Charge transfer complexes of chlorpheniramine, triprolidine and tripelennamine have absorption maxima at 293 nm and complex form of diphenhydramine has absorption maximum at 270 nm. By UV, IR spectra, it could be inferred that CT-complexes were formed by interaction between the basic nitrogen of antihistaminics as electron donor (non bonding electron) and iodine as electron acceptor (${\sigma}$ bonding electron).

• YAKHAK HOEJI
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• v.18 no.2
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• pp.133-144
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• 1974

The metal indicator, acidic azo dyes NN, EBT and Calcon are utilized to analyse quantitatively chlorpheniramine, tripelenamine and diphenhydramine forming insoluble ion pair in aqueous solution at proper pH values between the acidic azo dyes and the sample molecules, these compexes are extracted by organic polar solvents, and organic layer is determined spectrophotometrically. Generally, the absorption maxima of the complexes are shifted to longer wavelengths compare to the absorption maxima of the dyes themselves. The binding ratio of the ion pair forming complex molecules in chloroform soln, are as follows ; NN-antihistamines (chlorpheniramine, tripelennamine, diphenhydramine) are NN-1 to antihisamine-1, EBT-antihistamines are EBT-2 to antithistamines a and Calcon-antihistamines are Calcon-3 to antithistamines-1. These coomplexes in chloroform soln. are very stable, and show higher absorbance than the other organic polar solvents. The binding state of complexes were presumed intermolecular hydrogen bond by their infrared spectra. In the mixture solution of three samples, the aqueous phase is buffered at pH 1.0, and benzene is used to extract ion pair of diphenhydramine EBT complex selectively. At pH 1.0 of aqueous layer, Calon-diphenhydramine complex is also extracted selectively by benzene. However, in this case very small amount of chlorpheniramine-calcon calcon simultaneously. The binding state of diphenhydramine-EBT and diphenhydramine-calcon in benzene are smae as the complexes in chloroform. But the absorption maxima of the complexes in benzene are shifted to shorter wavelenlgths than the complexes in chloroform.

• Journal of Pharmaceutical Investigation
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• v.20 no.2
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• pp.89-95
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• 1990

Ethylcellulose-PEG 4000 film coated on core tablets was investigated as a potential drug delivery system for the controlled release of chlorpheniramine maleate (CPM). The kinetic analysis of the release data indicated that CPM release followed a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The effect of the film composition, CPM concentration, plasticizer concentration and CPM solubility on the release characteristics were examined. The release rate constant increased as CPM concentration increased. It also increased as the PEG 4000 content in the film increased above 10%(w/w), however, it decreased as the PEG 4000 content increased in the concentration range below 10%(w/w). The release rate constant was not affected by the coated weight on the core tablet. The film-coated tablets which contain CPM only in the coated film layer seemed to be a potential oral drug delivery system for the controlled release of CPM.

• 대한임상약리학회:학술대회논문집
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• 2006.11a
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• pp.31-32
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• 2006