GLC Determination of Chlorpheniramine in Human Plasma

Hanna, Suzan K.; Tang, Anbang

doi:10.1002/jps.2600631230

Cited by 20 publications

(3 citation statements)

References 11 publications

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“…However, its absorption has been reported to be sensitive to local gastrointestinal conditions and formulation employed [13][14][15]. The site of absorption for CPM is thought to be the small intestine due to its basicity [11,16]. DMH is an antitussive agent included commonly in cough and cold preparations [17].…”

Section: Introductionmentioning

confidence: 99%

Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Kim¹,

Jun²,

Lee

2020

Pharmaceutics

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Jellies for oral administration have been suggested as alternative dosage forms to conventional tablets for improved palatability and compliances for pediatric and geriatric patients. To evaluate the effect of jelly formulation on the bioavailability of cold medicines, two types of jellies were prepared for a fixed-dose combination of acetaminophen (AAP), chlorpheniramine maleate (CPM), dextromethorphan hydrobromide (DMH), and dl-methylephedrine hydrochloride (MEH). Jelly-S and Jelly-H were fabricated using carrageenan and locust bean gum in the absence and presence of xanthan gum, respectively. In vitro dissolution and in vivo absorption of the four drugs in the jellies were compared with other conventional formulations, a syrup and two types of immediate-release (IR) tablets with different hardness, Tablet-S (15 kPa) and Tablet-H (20 kPa). All the formulations exhibited more than 80% dissolution rate within 2 h even though the syrup, Jelly-S, and Tablet-S showed higher 30-min dissolution compared to Jelly-H and Tablet-H. The dissolution rates from the jellies decreased with increasing pH, which resulted in the slowest dissolution in pH 6.8 compared to the syrup and IR tablets. When administered orally to beagle dogs, all five formulations were determined not to be bioequivalent. However, Jelly-S and Jelly-H showed 0.82–1.05 of the geometric mean ratios (GMRs) of AUC0-t for all four drugs compared to the syrup suggesting comparable absorption. In two IR tablets, GMRs of AUC0-t were in a range of 0.55–0.95 indicating a tendency of lower absorption than the syrup and jellies. In conclusion, jelly can be a patient-centered formulation with comparable bioavailability to syrup.

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Section: Introductionmentioning

confidence: 99%

Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Kim¹,

Jun²,

Lee

2020

Pharmaceutics

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“…33. The site of absorption is thought to be the small intestine because of its large surface area and the basicity of chlorpheniramine.…”

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confidence: 99%

Clinical Pharmacokinetics of Chlorpheniramine

Rumore¹

1984

Drug Intelligence & Clinical Pharmacy

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The clinical pharmacokinetics of chlorpheniramine are reviewed. Recent studies have established that the half-life of chlorpheniramine is longer than previously reported. Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. The half-life is increased in the presence of renal dysfunction and decreased in children. The exact mechanism of the presystemic first-pass elimination and the effects of dose levels on the process presently are unclear. Biopharmaceutical and pharmacokinetic studies after single or multiple doses in humans reveal wide interindividual variations in pharmacokinetics. Age, dialysis, urinary pH and flow influence the elimination kinetics of chlorpheniramine. Attention is brought to major issues that need further clarification to optimize drug therapy with this antihistamine. The use of pharmacokinetic parameters of chlorpheniramine for clinical application is discussed.

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“…Authors such as Sondack ( 14) who states that "the extrapolation results passed through the origin" and King et al (5) who conclude "a standard graph rather than a one-point standard is required for maximum accuracy in the procedure" are examples of those who clearly understand the requirement. Unfortunately, too often authors simply state that the response curve was linear but fail to report whether a significant intercept was found (15)(16)(17)(18). In one case where the response curve itself was reported, there is no indication of how the calculation was made (19).…”

mentioning

confidence: 99%

Potential error in single-point-ratio calculations based on linear calibration curves with a significant intercept

Cardone¹,

Palermo²,

Sybrandt³

1980

Anal. Chem.

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Calculations based on a single-point standard linear calibration curve which has a finite intercept are a potential source of bias error. The error has been shown to be a function of magnitude of the slope and intercept, and the magnitude of the difference in the standard and sample responses. For maximum accuracy, the ratio of the difference in responses to the standard response should be the lowest possible. For any response curve, a reliable calculation of the percent error resulting from making a single-point-ratio calculation (SPRC) where a finite intercept exists is shown so that a decision as to its proper use or non-use may be made. In most cases, even when an analytically significant intercept is found in a linear calibration curve, the SPRC technique may stili be employed by calculating the sample signal to standard signal, S,/S, ratio range for an acceptable % error bias range. This calculation of the S,/S, ratio constitutes a trade-off between the use of a single standard and a shortened linear dynamic range with its possibility of more reanalyses against the use of the entire linear dynamic range with its mandatory requirement of more standards but the lesser possibility of reanalyses.

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GLC Determination of Chlorpheniramine in Human Plasma

Cited by 20 publications

References 11 publications

Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Clinical Pharmacokinetics of Chlorpheniramine

Potential error in single-point-ratio calculations based on linear calibration curves with a significant intercept

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