Bioequivalency and dose proportionality of three tableted promethazine products

Zaman, R.; Honigberg, I. L.; Francisco, G. E.; Kotzan, Jeffrey A.; Stewart, James T.; Brown, W. J.; Shah, Vinod P.; Pelsor, Francis R.

doi:10.1002/bdd.2510070309

Cited by 10 publications

(1 citation statement)

References 9 publications

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“…10). To take into account the decrease in the dosage for these subjects, as promethazine presents linear pharmacokinetics for doses ranging from 25 to 50 mg, 18 plasma concentrations were considered to be twice the actual ones.…”

Section: Resultsmentioning

confidence: 99%

Influence of Simulated Weightlessness on the Intramuscular and Oral Pharmacokinetics of Promethazine in 12 Human Volunteers

Gandia

Saivin

Traon

et al. 2006

The Journal of Clinical Pharma

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The National Aeronautics and Space Administration (NASA) recommends using promethazine to prevent and treat space motion sickness, but pharmacologic responses in space and on Earth are different. Twelve volunteers were given 50 mg promethazine orally or intramuscularly before and after 48 hours of bed rest to simulate weightlessness. The maximum measured plasma concentration (C(max)), time to C(max) (t(max)), and area under plasma concentration versus time curve from 0 to infinity (AUC(inf)) were determined, and the bioequivalence was tested between bed-rest and ambulatory status for the intramuscular and oral routes as well as between both routes for bed-rest and ambulatory position. Simulated weightlessness did not influence the ratio AUC(bed rest)/AUC(ambulatory) after intramuscular injection, whereas a significant increase (26%) in the ratio was seen after oral administration, probably because of a prolonged contact time between promethazine and the intestinal wall associated with an increase in the intestinal transit time. The AUC was 3-fold higher when the drug was administered by the intramuscular route during both positions. Thus, intramuscular administration could be a good alternative to the oral route.

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Section: Resultsmentioning

confidence: 99%

Influence of Simulated Weightlessness on the Intramuscular and Oral Pharmacokinetics of Promethazine in 12 Human Volunteers

Gandia

Saivin

Traon

et al. 2006

The Journal of Clinical Pharma

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Rotary pursuit, a measure of human performance, and plasma concentrations of promethazine

Kotzan

Honigberg

Francisco

et al. 1986

Biopharm & Drug Disp

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Promethazine in doses of 50 mg has demonstrated detrimental effects upon the performance of visual tasks. The purpose of the study was to examine the relationship between the blood concentration levels of promethazine and two human performance tasks. Fifteen paid healthy male volunteers completed a randomized five-way crossover design which included a 25 mg and 50 mg dose of the innovator dosage form, a 50 mg dose of a generic dosage form, a 50 mg solution dosage form, and a placebo. Serial blood samples were obtained in addition to performance measures of rotary pursuit and a simple force choice reaction time. Analysis of the forced choice reaction depicted a mild relationship with the blood concentration levels of promethazine. However, the measures of rotary pursuit, a more sensitive determinant of human motor performance, proved to be more related to both the promethazine blood concentration and the inherent learning which was confounded in the experiment. The degree of impaired pursuit performance and reaction time differences could be defined in terms of a linear relationship to the promethazine concentration.

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A validated stability‐indicating reversed‐phase‐UPLC method for simultaneous estimation of promethazine hydrochloride, methylparaben, propylparaben and sodium benzoate assay of cough suppressant and antihistamine liquid oral dosage forms

Pippalla,

Nekkalapudi,

Komreddy

2024

Biomedical Chromatography

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A quick, simple, sensitive, efficient and stability‐indicating reverse‐phase ultraperformance liquid chromatographic method for the estimation of propylparaben, methylparaben and sodium benzoate in a pharmaceutical liquid oral formulation was developed. A Waters Acquity UPLC BEH C18, 50 × 2.1 mm, 1.7 μm i.d. column was used to perform chromatographic separation with a 0.1% perchloric acid mobile phase used as solvent A and a mixture of 0.1 % perchloric acid and methanol in the ratio 20:80 (v/v), respectively, as solvent B. The experiments were carried out at a flow rate of 0.4 ml/min and the detection wavelength was 240 nm. The compartment temperature of the column was set at 40°C and the injection volume was set at 2 μl. The main aim of the research was to develop a single UPLC assay method for promethazine (active ingredient) and preservatives in the oral solution of promethazine HCl and dextromethorphan HBr that contains promethazine (active ingredient) and methylparaben, propylparaben and sodium benzoate (preservatives). An assay of dextromethorphan HBr was developed and validated by another HPLC method. The drug and preservatives were eluted at retention times of 19.3 min for promethazine HCl, 9.3 min for methylparaben, 18.9 min for propylparaben and 8.9 min for sodium benzoate. Validation of the developed method was carried out as stated by the International Conference on Harmonization guidelines ICH Q2B and under USP<1225>. The analytical parameters verified specificity/selectivity, linearity, accuracy, ruggedness and robustness. The linearity ranges of promethazine HCL, methylparaben, propylparaben and sodium benzoate were 10–100, 10–80, 1.0–8.0 and 10–80 μg/ml, respectively, with a correlation coefficient of active ingredients and preservatives of 1.00. Percentage recoveries of promethazine, propylparaben, methylparaben, and sodium benzoate were 100.0–100.2, 99.0–100.3, 99.5–98.0 and 99.0–100.0%. The validated analytical method proves that the method is specific, precise, linear, accurate, sensitive, rugged and stable, indicating the quantification of the active ingredient and all preservatives in liquid oral formulations.

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Bioequivalency and dose proportionality of three tableted promethazine products

Cited by 10 publications

References 9 publications

Influence of Simulated Weightlessness on the Intramuscular and Oral Pharmacokinetics of Promethazine in 12 Human Volunteers

Influence of Simulated Weightlessness on the Intramuscular and Oral Pharmacokinetics of Promethazine in 12 Human Volunteers

Rotary pursuit, a measure of human performance, and plasma concentrations of promethazine

A validated stability‐indicating reversed‐phase‐UPLC method for simultaneous estimation of promethazine hydrochloride, methylparaben, propylparaben and sodium benzoate assay of cough suppressant and antihistamine liquid oral dosage forms

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