The Pharmacokinetics (PK), Safety and Tolerability of Fexofenadine HCl 6 mg/mL Suspension in Children with Allergic Rhinitis (AR): a Multicenter, Open-label, Single-dose Study

Grubbe, Robert; Nayak, Ashwini; Kittner, Barbara; Segall, Nathan

doi:10.1016/j.jaci.2006.11.688

Cited by 2 publications

(8 citation statements)

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“…39 Several other studies evaluating the pharmacokinetics of fexofenadine HCl in children also support similar exposures in children who received ageadjusted doses to those of adults receiving a 60 mg dose of fexofenadine HCl. 30,31,48,49 When drug formulations are changed, it is important to demonstrate bioequivalence between the formulations. 24,25 Typically, such studies are conducted in adults.…”

Section: Discussionmentioning

confidence: 99%

“…There were no signs of clinically meaningful sedation or changes in QTc interval compared with placebo. 14 Various formulations of fexofenadine HCl are approved: hard capsules (60 mg), film-coated tablets (30,60,120, and 180 mg), gelcap tablets (180 mg), oral dispersible integrating tablets (ODT, 30 mg in USA only, 60 mg in Japan only), oral suspension (6 mg/mL), and powder for syrup (5%, in Japan only). The approved doses of fexofenadine HCl are 60 mg bid, 120 mg once daily (qd), or 180 mg qd for SAR, and 60 mg bid or 180 mg qd for CIU in patients ≥12 years; 30 mg bid for children 2-11 years with SAR, and 30 mg bid for children 2-11 years or 15 mg bid for children 6 months to <2 years with CIU.…”

mentioning

confidence: 99%

“…25 Moreover, bioavailability and bioequivalence studies are generally conducted in adult populations. 26 The pharmacokinetics of fexofenadine HCl are well characterized in healthy adults [27][28][29] and in children with SAR 30,31 and CIU. 32 Fexofenadine is rapidly absorbed (T max 1.4-1.5 hours) and has an absolute bioavailability of 35% after oral administration.…”

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confidence: 99%

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Bioequivalence of 2 Pediatric Formulations of Fexofenadine Hydrochloride Oral Suspension

Rauch,

Lucio,

De Fer

et al. 2023

Clinical Pharm in Drug Dev

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Fexofenadine hydrochloride (HCl) is a second‐generation, nonsedating, histamine H1‐receptor antagonist used to manage seasonal allergic rhinitis and chronic idiopathic urticaria. A new oral pediatric suspension of fexofenadine HCl has been developed, with the preservative potassium sorbate replacing parabens. The objective of this phase 1 single‐center, open‐label, randomized, 2‐treatment, full‐replicated, 4‐period, 2‐sequence crossover study in healthy adult volunteers was to assess the bioequivalence of 30 mg of the new oral suspension of fexofenadine HCl (test) versus 30 mg of the marketed pediatric oral suspension of fexofenadine HCl (reference). The replicate design was based on the high intra‐individual variability of fexofenadine (>30% on Cmax). The study comprised 68 randomized and treated volunteers. Plasma concentrations of fexofenadine were similar following the administration of a single dose of each formulation. Cmax, AUClast, AUC, median tmax, and mean t1/2z were similar between administrations of the same fexofenadine formulation and between formulations. A high intra‐individual variability was confirmed with both formulations. Bioequivalence of the test and reference fexofenadine HCl formulations was demonstrated as the 90% confidence intervals of the geometric least squares mean ratio for Cmax, AUClast, and AUC of fexofenadine were all within the bioequivalence range of 0.80‐1.25. There were no serious adverse events (AEs) or study discontinuations due to treatment‐emergent AEs with either fexofenadine HCl formulation. The new paraben‐free fexofenadine HCl 30‐mg oral suspension and marketed fexofenadine HCl 30‐mg pediatric oral suspension are bioequivalent under fasting conditions, with no safety concerns and a safety profile consistent with the known profile of fexofenadine.

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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Bioequivalence of 2 Pediatric Formulations of Fexofenadine Hydrochloride Oral Suspension

Rauch,

Lucio,

De Fer

et al. 2023

Clinical Pharm in Drug Dev

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“…They found equivalent areas under the curves for the oral suspension and the tablet formulation, suggesting bioequivalence of fexofenadine oral suspension and fexofenadine capsules. In a study focusing on the oral formulations, Grubbe et al (2007) evaluated the pharmacokinetics of fexofenadine oral suspension in 50 children, aged 2 to 5 years, which demonstrated the mean maximum plasma concentration of 224 ng/mL, and the mean area under the plasma concentration curve of 898 ng-h/mL. In capsule formulations in a double-blind, two-way crossover study in children with allergic rhinitis (with a mean age of 9.8 years, a mean height of 134 cm and a mean weight of 32.1 kg), Simons et al (1996) administered 30 or 60 mg of fexofenadine as a capsule and demonstrated the mean maximum plasma concentrations after the 30 mg dose of 78 ng/mL, and the mean maximum concentrations after the 60 mg dose of 286 ng/mL.…”

Section: Bioequivalence Of Oral Suspension and Solid Formulations Of mentioning

confidence: 99%

“…There were no clinically relevant differences for laboratory measures, vital signs, and physical examinations ( Milgrom et al 2007 ). Grubbe et al (2007) evaluated effects of fexofenadine oral suspension in 50 children, aged 2 to 5 years. Seven of their subjects experienced 10 adverse events, which resolved without sequelae.…”

Section: Efficacy and Safetymentioning

confidence: 99%

Fexofenadine hydrochloride in the treatment of allergic disease: a review

Bielory¹

2008

JAA

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Fexofenadine is a selective, non-sedating H1 receptor antagonist, marketed in the United States since 2000. The FDA approved an oral suspension in 2006, for the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria in children. The tablet, capsule, and oral suspension are bioequivalent. Although fexofenadine does not use P450 CYP 3A4 it does interact with a number of drugs at P-glycoprotein and organic anion transporter polypeptides. The risk of toxicity from other drugs may increase with the administration of fexofenadine. Orange and grapefruit juices reduce the bioavailability of fexofenadine. Fexofenadine has been shown to have an impact on infl ammatory mediators, other than histamine, such as decreasing the production of LTC 4 , LTD 4 , LTE 4 , PGE 2 , and PGF 2α ; inhibiting cyclo-oxygenase 2, thromboxane; limiting iNOS generation of NO; decreasing cytokine levels (ICAM-1, ELAM-1, VCAM-1, RANTES, I-TAC, MDC, TARC, MMP-2, MMP-9, tryptase); and diminishing eosinophil adherence, chemotaxis, and opsonization of particles. These effects may provide benefi t to some of the infl ammatory responses of an acute allergic reaction and provide a basis for future development of H1 antagonists with stronger anti-infl ammatory effects. These studies also support the contention that fexofenadine is effective for the treatment of allergic rhinits and chronic idiopathic urticaria.

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The Pharmacokinetics (PK), Safety and Tolerability of Fexofenadine HCl 6 mg/mL Suspension in Children with Allergic Rhinitis (AR): a Multicenter, Open-label, Single-dose Study

Cited by 2 publications

References 0 publications

Bioequivalence of 2 Pediatric Formulations of Fexofenadine Hydrochloride Oral Suspension

Bioequivalence of 2 Pediatric Formulations of Fexofenadine Hydrochloride Oral Suspension

Fexofenadine hydrochloride in the treatment of allergic disease: a review

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