EP1964566A1 — Preparation with improved bioabsorbability of sapropterin hydrochloride

USPTO Abstract

A method of significant improvement for the bioavailability of orally administered sapropterin hydrochloride, a therapeutic agent used to treat BH4-responsive hyperphenylalaninemia, is provided. Also provided is a preparation for oral administration or ingestion having an improved bioavailability of sapropterin hydrochloride. Specifically, the preparation having an improved bioavailability of sapropterin hydrochloride contains sapropterin hydrochloride and an absorption promoter including an organic carboxylic acid having more than one carboxyl group in its molecule. The organic carboxylic acid having more than one carboxyl group in its molecule is selected from tartaric acid, citric acid, malic acid and optically active substances thereof, racemic mixtures thereof, anhydrides thereof, hydrates thereof or mixtures thereof. The amount by weight of the organic carboxylic acid is 0.1 to 100 times that of sapropterin hydrochloride.