An Investigation of the Dimensional Changes of Polymer Mixture Tablets Containing a Soluble Drug, Using an Image Analysis Method. Influence of These Characteristics on Drug Release and Its Mechanism

摘要

The properties and characteristics of the polymer used for the preparation of matrix drug delivery systems considerably influence their performance and the extent of drug release and its mechanism. The objective of this research was to examine the dimensional changes, and gel evolution of polymer matrices consisting of three different polymers Polyox, sodium alginate (hydrophilic) and Ethocel (hydrophobic), using an image analysis method. Furthermore to explore how these changes influence the release rate of a soluble drug namely, venlafaxine. All tablets displayed marked dimensional expansion and gel growth particularly those consisting of two hydrophilic polymers Polyox/sodium alginate (POL/SA/V) compared to those consisting of the hydrophilic/hydrophobic Polyox/Ethocel (POL/ET/V). Similarly the thickness of the gel layer in POL/SA/V matrices increased considerably with time up to 8 hours. In general our findings show that the POL/SA/V matrices, due to their thicker gel layer produced a more effective barrier which results in a more pronounced sustained release delivery. This accounts for the slower and smaller overall drug release observed with the POL/SA/V matrices compared to those containing POL/ET/V and indicates that the formation of a thick and durable gel barrier is a characteristic necessary for the preparation of sustained drug release systems. Moreover the solubility of venlafaxine in combination with the polymer’s properties appears to play an important role on the extent of drug release and the release mechanism. Overall the polymer mixtures examined comprise a useful and promising combination of materials for the development and manufacture of sustained release preparations based on these polymers.