Hydro-alcoholic media effects on theophylline release from sesamum polysaccharide gum matrices

Abstract

Concomitant ingestion of alcohol and medications can greatly affect drug plasma concentrations as dose dumping or failure may occur as a result of the fact that formulation excipients may not always be resistant to alcohol. In this study, a natural polysaccharide (Sesamum radiatum gum) (SG) was extracted, characterized and used to formulate sustained release theophylline compacts to study the effect of varying alcohol concentrations (v/v) in dissolution media on drug release from these compacts. X-ray powder diffraction showed that the extracted gum was amorphous in nature with the powder having excellent compaction properties as observed with its compact being significantly harder than those prepared with pure hydroxypropyl methyl cellulose (HPMC) K4M. X-ray microtomography showed that the compacts produced were homogenous in nature, however, swelling studies showed failure of the compacts at the highest concentration of absolute ethanol used (40% v/v). Dissolution studies showed similarity at all levels of alcohol tested (f₂ = 57–91) in simulated gastric (0.1 N HCl, pH 1.2) and intestinal fluids (phosphate buffer, pH 6.8) for the HPMC compacts whereas dissimilarity only occurred for the SG compacts at the highest alcohol concentration in both media (f₂ = 35). The suitability of SG as a matrix former that can resist alcoholic effects therefore makes it suitable as an alternative polymer with wider applications for drug delivery.

Keywords:

• HPMC K4M
• native sesamum gum
• matrix tablets
• theophylline
• hydro-alcoholic
• rheology

Acknowledgements

The authors will like to thank Colorcon and Meggle for the kind gifts of HPMC K4M and FlowLac^® 100, respectively and acknowledge Chris Dawson for generating the X-ray microtomography images.

Disclosure statement

The authors report no declarations of interest

Additional information

Funding

This project was funded by the Royal Society through the award of the Newton International Fellowship scheme to Elijah I. Nep (grant number NF120704).