Study of the Critical Points in Combined Matrix Tablets Containing Both Inert and Swelling Excipients

This work estimates for the first time critical points in combined matrices containing varying concentrations of the hydrophilic polymer Hydroxypropyl methylcellulose (HPMC) K100 M CR in presence of a constant percentage of the inert matrix forming polymer Eudragit RS-PO as well as varying concentra...

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Detalles Bibliográficos
Autores: Aguilar de Leyva, Mercedes Ángela, Campiñez, Maria Dolores, Jost, Flavia, Gavira, Miguel, Caraballo Rodríguez, Isidoro
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2019
País:España
Institución:Universidad de Sevilla (US)
Repositorio:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/162817
Acceso en línea:https://hdl.handle.net/11441/162817
https://doi.org/10.1016/j.jddst.2019.06.005
Access Level:acceso abierto
Palabra clave:Critical points
Percolation theory
Expert system SeDeM
Matrix controlled release formulations
Interaction of matrix polymers
Science based design
Descripción
Sumario:This work estimates for the first time critical points in combined matrices containing varying concentrations of the hydrophilic polymer Hydroxypropyl methylcellulose (HPMC) K100 M CR in presence of a constant percentage of the inert matrix forming polymer Eudragit RS-PO as well as varying concentrations of the inert polymer in presence of a constant percentage of the hydrophilic excipient. Drug release assays, water uptake studies and calculation of the Exicipient Efficiency (EE) have been carried out to study the interaction between the polymers. Surprisingly, an increase in the drug release rate occurs as the percentage of the hydrophobic polymer increases in the formulations. This fact is supported by the EE values which indicate a negative interaction between the two excipients. Moreover the HPMC percolation threshold estimated is higher than the one observed in pure HPMC matrices. It can be concluded that the HPMC creates pores in the inert skeleton, destabilizing the system. Moreover, the inert excipient destabilizes the gel layer formed by HPMC, changing its critical point. This information is essential for a rational estimation of the Design Space of a formulation and provides new knowledge on the behavior of the polymers in combined matrices, which contributes to the science based design.