Production and investigation of sustained berberine pellet drug release system

Abstract

Recent studies show that berberine (BBR) is a highly promising drug candidate to treat various diseases such as diabetes, hyperlipidemia and cancer. However, the potential therapeutic application of BBR in clinic is very limited due to its undesired pharmacokinetic characteristic. In current study, BBR pellets of acceptable size and shape quality (for capsuling) are generated by extrusion-spheronisation. Compared to commercial BBR tablets, the BBR pellets show significant sustained drug release behaviour which is expected to improve the pharmacokinetic behaviour of BBR and thus enhance its oral bioavailability. Experimental results indicate that not only the pellet size but also the excipient permeability plays an important role in pellet drug release behaviour. Low field-nuclear magnetic resonance (LF-NMR) is used, for the first time, to investigate and compare water diffusion rate and water distribution in pellet-release medium systems. It is found that the water diffusion rate is dominated by pellet surface area, while the total amount of water diffusing into pellets is mainly related to excipient permeability. This study provides a guidance in optimisation of formulation and product morphology to generate BBR pellets with a desired release behaviour based on LF-NMR technique.