Enzymatic degradation of cross-linked excipient matrix of co-processed xanthan gum-amylose and dissolution profile of diclofenac sodium tablet

Abstract

Objectives: This study aims to determine the amount of excipient that is degraded by alpha-amylase and the influence of alpha-amylase to the dissolution profile of sustained-release tablets that use matrix CL-Co-A-XG. Methods: Excipient is cross-linked with two concentrations of sodium trimetaphospate, which are 6% (CL6-Co-A-XG) and 12% (CL12-Co-A-XG). Each excipient is made with the ratios 1:1, 1:2, and 2:1 amylose-xanthan gum. Enzymatic degradation tests are performed on excipient powders for 60 minutes. Sustained-release tablet with CL-Co-A-XG excipient as a matrix is formulated through direct compression method. Then, drug dissolution tests are performed in a phosphate buffer with a pH of 7.4 both using and without using alpha-amylase as a medium for 8 hrs. Results: The results of this study show that CL6-Co-A-XG and CL12-Co-A-XG degraded 20% at 10 and 30 minutes, respectively. In addition, the release profile of F1-F6 tablets show the sustained-release profile that follows zero-order and Korsmeyer–Peppas kinetics and is unaffected by the presence of alpha-amylase. Conclusions: From this study, it can be concluded that the CL-Ko-A-XG excipients are more resistant to enzymatic degradation than amylose. Therefore, this excipient shows potential as a single matrix sustained-release tablet.