Development and evaluation of budesonide-based modified-release liquid oral dosage forms

Abstract

Modified-release oral drug delivery dosage forms are widely used in the pharmaceutical field to overcome all the potential issues imposed by the physiological variabilities of the gastrointestinal tract as well as to maintain drug concentrations within the therapeutic window. In the market, they are available only as solid dosage forms such as capsules or tablets. The development of a liquid oral dosage form with modified-release properties has been keenly awaited. This form could increase the compliance of patients with a swallowing impairment (i.e. paediatric, older or critically ill patients) and, consequently, the efficacy of the therapeutic treatment. In this study, budesonide was used as a model drug to develop a modified-release liquid oral dosage form (i.e. colonic-release, sustained-release). For this purpose, multi-layered particles were obtained, starting from small microcrystalline cellulose neutral cores (Cellets® with a mean diameter lower than 500 μm), in a lab-scale fluid-bed coater. Poly(meth)acrylate polymers commonly available under the trade name of Eudragit®, such as S100, RS PO, RL100 and E100, were used to get defined drug release profiles. They were also used to guarantee the stability of the reconstituted liquid syrup during 2 weeks of storage at room temperature.