OPTIMIZED PHARMACEUTICAL FORMULATION FOR THE TREATMENT OF INFLAMMATORY CONDITIONS OF THE ESOPHAGUS

摘要

Disclosed is an optimized pharmaceutical formulation for the treatment of inflammatory conditions of the esophagus. A pharmaceutical formulation in the form of an orodispersible effervescent tablet is stable, easy to produce, and can be used without dissolving same in a liquid. It is not necessary to drink anything with the tablet as this would reduce the time that the budesonide solution remains in the affected regions of the esophagus. The effervescent tablet of the invention surprisingly resulted in an unexpectedly high rate of histological remission in patients with active eosinophilic esophagitis.

主权项

1. An orodispersible effervescent tablet containing:
(a) 0.25 mg to 5 mg of budesonide, (b) a salt of at least one pharmacologically acceptable acid that, in an aqueous environment, can release a gas with a further acid, wherein said salt is selected from the group consisting of NaHCO3, Na2CO3, KHCO3, K2CO2, CaCO3, and mixtures thereof; (c) a pharmaceutically acceptable weak acid or salt thereof that decreases the pH value in an aqueous solution, wherein said weak acid is selected from the group consisting of disodium citrate, monosodium citrate, and mixtures thereof, and (d) sucralose in an amount of 0.1 to 1.0% by weight, based on the weight of the finished tablet, wherein: the effervescent tablet has a mass of 100 mg to 200 mg.