Chlorpheniramine

There are several groups of compounds which are used as active and inactive ingredients in various over-the-counter drug compositions. These compounds are different in nature and can be organic and inorganic. Most of the active ingredients are either hydrophobic basic, hydrophilic basic or hydrophilic neutral compounds. Basic active ingredients of cough and cold remedies used as salts of organic and inorganic acids. The most commonly used hydrophobic active ingredients are doxylamine, pyrilamine, chlorpheniramine, brompheniramine, and dextromethorphan. Doxylamine is an antihistamine drug, used to relieve symptoms of allergy, hay fever, and the common cold. Doxylamine is used in combination with other active ingredients to provide effective nighttime relief from cough and cold symptoms. Pyrilamine is an antihistamine drug, which targetsH1 receptors as an inverse agonist. Brompheniramine is an antihistamine drug of propylamine nature. Chlorpheniramine is an antihistamine used to treat symptoms such as allergic rhinitis. Dextromethorphan is a medication mostly used as a cough suppressant. It is a morphine type of medication with sedative, dissociative, and stimulant properties. Succinic acid is a hydrophilic diacid that is used as a counterion. Maleic acid is hydrophilic diacid which is used as a counterion. Both compounds have very limited retention even in RP-AQ columns. Due to the strongly hydrophobic and basic properties of these compounds, they demonstrate a poor peak shape in traditional reversed-phase chromatography due to the overloading of residual silanol groups on the surface when these basic drugs are analyzed. In addition to this, hydrophilic counterions are not retained in RP because there is no mechanism of retention for these acidic hydrophilic compounds. Both problems were eliminated by using Heritage MA reversed-phase anion-exchange column. Column and method demonstrate high efficiency and good peak shape for acidic and basic analytes. It can be used to develop methods for various cough, cold, and congestion compositions without the use of ion-pairing reagents. Compounds are well retained by a combination of one or more mechanisms. The column is compatible with 100% ACN and 100% water as well as with most buffers with pH 1.5-7. Various additives to the mobile phase can be used based on the nature of samples and detection techniques.

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Conditions of Experiment

Column:	Heritage MA
Separation Modes:	reversed-phase, cation-exclusion, anion-exchange
Column Dimenstions:	4.6x150 mm, 3 um, 100A
Mobile Phase:	5% ACN with 30 mM AmFm pH 3
Detection:	UV 275
Sample:	various
Injection:	3 uL
Flow rate:	1 ml/min

Analytes

Class of compounds:	Amines, Aromatic base, Drug, Organic acid, Pyridine
Nature of compounds:	Acidic, Basic, Hydrophilic, Hydrophobic, Polar
Compounds:	Doxylamine, Pyrilamine, Succinic acid, Chlorpheniramine, Brompheniramine, Maleic acid, Dextromethorphan

Vick’s NyQuil Cold and Cough remedy temporarily relieves common cold/flu symptoms: cough due to minor throat & bronchial irritation, sore throat, headache, minor aches & pains - fever - runny nose & sneezing. The active ingredients include acetaminophen, chlorpheniramine, and dextromethorphan. Acetaminophen or paracetamol is a relatively hydrophilic drug, which is used to treat pain and fever. Dextromethorphan is a hydrophobic and basic compound, which serves as a cough suppressant in over-the-counter (OTC) medications. Chlorpheniramine hydrophobic and basic antihistamine drugs are used to treat symptoms of allergic conditions. All three active ingredients retain very differently, and usually, dextromethorphan and chlorpheniramine show a poor peak shape in RP chromatography due to residual silanol interactions. This problem does not exist on Coresep 100 mixed-mode column, where the polar ionizable group shields analytes from interacting with the residual silanols. Coresep 100 column demonstrates high efficiency and selectivity of separation. Methods for this drug composition are robust and reproducible and can be used in method development and validation. The column is compatible with 100% ACN and 100% water and can be used in a single or dual mode depending on the nature of the analyte and mobile phase composition. Very often order of elution can be changed by changing the amount of ACN, buffer pH, buffer concentration, and buffer nature.

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Conditions of Experiment

Column:	Coresep 100
Separation Modes:	reversed-phase, cation-exchange
Column Dimenstions:	4.6x150 mm, 2.7 um, 90A
Mobile Phase:	A: 10% ACN with 0.02% H2SO4 B: 70% ACN with 0.2% H2SO4 from 100% A to 100% B in 8 min, 4 min hold
Detection:	UV 275
Sample:	various
Injection:	3 uL
Flow rate:	1 ml/min

Analytes

Class of compounds:	Amines, Aromatic base, Aromatic compound, Drug
Nature of compounds:	Basic, Hydrophilic, Hydrophobic, Neutral
Compounds:	Acetaminophen, Chlorpheniramine, Dextromethorphan