Effect of food on the bioavailability of fexofenadine hydrochloride (MDL 16 455A)

✍ Scribed by Maxine Stoltz; Thangam Arumugham; Christina Lippert; Dale Yu; Vijay Bhargava; Mark Eller; Scott Weir

• Publisher: John Wiley and Sons
• Year: 1997
• Tongue: English
• Weight: 77 KB
• Volume: 18
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/(sici)1099-081x(199710)18:7<645::aid-bdd50>3.0.co;2-3

✦ Synopsis

The hydrochloride salt of fexofenadine, the primary metabolite of terfenadine (Seldane 1 ), is being developed for the treatment of symptoms associated with seasonal allergic rhinitis without producing sedation. Clinical safety and ecacy studies of fexofenadine hydrochloride were conducted using an immediate-release capsule formulation of the drug. A tablet containing the same granulation plus magnesium stearate is being developed as a supplementary dosage form. Because co-ingestion of food has been shown to eect the bioavailability of many drugs, 1,2 the present studies were conducted to evaluate bioavailability of fexofenadine hydrochloride given as capsules or tablets when administered with a high-fat meal. Previous studies with fexofenadine hydrochloride have shown that under fasted conditions the relative bioavailability of the capsule is 89±93% when compared to an oral solution. The bioequivalence of the tablets relative to the capsules has also been established under fasting conditions (unpublished data).

Two separate open-label, randomized crossover design studies were conducted where each subject received either (i) a single oral dose of 80 mg fexofenadine hydrochloride production-scale capsules (2640 mg) following a 10 h fast and 30 min following a high-fat breakfast or (ii) a single oral dose of 120 mg fexofenadine hydrochloride production-scale immediate-release tablets (3640 mg) after a 10 h fast and after ingestion of a high-fat breakfast. The high-fat breakfast consisted of two eggs fried in butter, two strips of bacon, two pieces of buttered toast, 2 oz hash browns, and 8 oz whole milk (55 g fat, 33 g protein, 58 g carbohydrate). A 6 d washout was allowed between treatment periods.