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Influence of Food on the Oral Bioavailability of Loratadine and Pseudoephedrine from Extended‐Release Tablets in Healthy Volunteers
Author(s) -
Nomeir Amin A.,
Mojaverian Parviz,
Kosoglou Teddy,
Affrime Melton B.,
Nezamis Jim,
Radwanski Elaine,
Lin ChinChung,
Cayen Mitchell N.
Publication year - 1996
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1996.tb04759.x
Subject(s) - loratadine , pseudoephedrine , bioavailability , pharmacokinetics , crossover study , pharmacology , chemistry , nasal decongestant , absorption (acoustics) , bioequivalence , area under the curve , cmax , oral administration , chromatography , medicine , anesthesia , ephedrine , placebo , physics , alternative medicine , pathology , acoustics
The effect of a high‐fat breakfast on the bioavailability of the components of an extended‐release tablet containing 10 mg loratadine in the immediate‐release coating and 240 mg pseudoephedrine sulfate in the extended‐release core was studied in 24 healthy male volunteers in a single‐dose, two‐way crossover study. The drug was administered after a 10‐hour overnight fast or within 5 minutes of consuming a standardized high‐fat breakfast. Serial blood samples were collected over a 48‐hour period, and plasma was analyzed for loratadine and its active metabolite descarboethoxyloratadine (DCL), and pseudoephedrine. For pseudoephedrine, maximum concentration (C max ) and area under the concentration—time curve extrapolated to infinity (AUC 0‐∞ ) were similar after both treatments, indicating no relevant food effect on the bioavailability of pseudoephedrine. Also, the absorption profiles of pseudoephedrine (from Wagner‐Nelson analysis) were similar for the fed and fasted treatments, indicating no apparent differences in absorption. Plasma concentration—time profiles and values for C max and AUC 0‐∞ of DCL were similar for the two treatments, indicating no relevant food effect on the pharmacokinetics of DCL. In contrast, for loratadine, administration with food resulted in a significantly increased mean C max (53%) and AUC from time zero to the final quantifiable sample (AUC tf ) (76%). However, the resultant C max and AUC of loratadine under fed conditions were well below those previously obtained at steady‐state after multiple‐dose administration of loratadine (40 mg/day) that were shown to be safe and well‐tolerated in several clinical studies. The effect of food on the bioavailability and pharmacokinetic profiles of the components of a combination loratadine/pseudoephedrine extended‐release tablet is not likely to be clinically significant.