Oral Viscous Gel of Budesonide: Optimised formulation improving productivity

Introduction

Eosinophilic oesophagitis is a chronic immune-mediated oesophageal inflammatory disease characterized by oeosinophilic infiltration of the oesophagus, causing dysphagia, vomiting and epigastric pain. Treatment options include food elimination diets and topical steroids.

Regarding the increasing number of patients concerned, a stable dosage form suitable for the treatment were made [1], consisting in an oral gel of budesonide (OVBG) with xanthan gum and 70 single vials. This OVBG formulation allows longer oesophageal mucosal contact time and increase compliance with children. The aim of this work is to optimise the process of preparation by using pharmaceutical Budesonide feedstock in order to rationalize the number of stages and decrease repetitive traumatic gestures for the operators.

Materials and method

Single vial composition was studied. The presence of a citrate buffer must be taken into account. Various concentrations of polysorbate 80 were tested to enhance the solubility of Budesonide, which is poorly soluble in water. The constituent addition order has also been optimized.

Operators were asked to fill a survey to realize a feasibility study as well as an assessment of the costs. Moreover, High Precision Liquid Chromatography dosing assays were made in three separate locations from the OVBG to evaluated content uniformity.

Results and discussion

The pH of the formulation is maintained around 5.2 with citrate buffer for better stability of budesonide. 1% m/m of polysorbate 80 is also selected to enhance solubility.

This new formulation allows cost saving of 17.5€ for 70 oral pouch product versus 7.71€ for 70mg of budesonide feedstock and permits 15 minutes to be saved on operator’s time. It also limits traumatic gesture and reduces the volume of waste. A scale-up may be considered.