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 (f = 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 (f = 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.

The use of visible and UV dissolution imaging for the assessment of propranolol hydrochloride in liquisolid compacts of Sesamum radiatum gum

“…The other event on the sesamum DSC trace is attributed to the polysaccharide decomposition (Zohuriaan and Shokrolahi 2004;Varma et al, 1997) between 251 and 302.3 °C. This phenomenon was confirmed using TGA analysis as a final weight loss of ~ 54.6 % by Nep et al 2018 with the thermal scission of carboxylate or carboxylic acid groups resulting in the evolution of C02 from the corresponding carbohydrate backbone being a probable mechanism for the observations. Figure 3c highlights that the characteristic peaks of PPN was present in all formulations (conventional and liquisolid).…”

“…by Nep et al 2018. The authors observed minor weight loss of ~ 11.5 % between -140 °C using TGA analysis and DSC.…”

“…The sesamum gum was successfully extracted and characterised. The gums characterisation has been extensively reported elsewhere (Nep et al, 2016(Nep et al, , 2016a(Nep et al, , 2018. In brief, sesamum is an amorphous polymer (Figure 3a).…”

Imaging of the Effect of Alcohol-Containing Media on the Performance of Hypromellose Hydrophilic Matrix Tablets: Comparison of Direct Compression and Regular Grades of Polymer

“…Nep et al also explored starch-free grewia polysaccharide in comparison to the native grewia gum and found extraction of starch to improve the blending process and increase the resistance of the polysaccharides to alcohol damage [ 16 ]. The same authors also explored the effects of hydroalcoholic media on an extracted sesamum gum polysaccharide [ 17 ]. Ethanol has been reported to not have any dose dumping repercussions on the kinetics of drug release from hypromellose incorporated matrices [ 2 , 18 ].…”

Mechanical and release behaviour of theophylline from matrix tablets containing psyllium powder in combination with grewia polysaccharides

“…Transport across this layer is by diffusion, but erosion can also occur when the polymer chains begin to untangle, as this happens the drug begins to be released [3]. The natural polymers have been used as matrices for sustained release [4][5][6][7][8][9][10][11][12] stabilizers or suspending agents in liquid dosage forms [13] and in bioadhesive drug delivery systems [14,15]. Apart from the fact that the natural materials are biocompatible, they have the additional advantages of being low cost and relatively abundant [16][17][18] compared to their synthetic counterparts.…”