Adeleke O.A., Choonara Y.E., Kumar P., Du Toit L.C., Tomar L.K., Tyagi C., Pillay V.
Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa
Adeleke, O.A., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa; Choonara, Y.E., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa; Kumar, P., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa; Du Toit, L.C., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa; Tomar, L.K., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa; Tyagi, C., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa; Pillay, V., Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa
Drug release from hydrophilic matrices is regulated mainly by polymeric erosion, disentanglement, dissolution, swelling front movement, drug dissolution and diffusion through the polymeric matrix. These processes depend upon the interaction between the dissolution media, polymeric matrix and drug molecules, which can be significantly influenced by formulation variables and excipients. This study utilized mathematical parameters to evaluate the impacts of selected formulation variables and various excipients on the release performance of hydrophilic polyamide 6,10 (PA 6,10) monolithic matrix. Amitriptyline HCl and theophylline were employed as the high and low solubility model drugs, respectively. The incorporation of different excipient concentrations and changes in formulation components influenced the drug release dynamics as evidenced by computed mathematical quantities (tx%,MDT x%,f1, f2, k1, k2, and kF). The effects of excipients on drug release from the PA 6,10 monolithic matrix was further elucidated using static lattice atomistic simulations wherein the component energy refinements corroborates the in vitro and in silico experimental data. Consequently, the feasibility of modulating release kinetics of drug molecules from the novel PA 6,10 monolithic matrix was well suggested. © 2013 American Association of Pharmaceutical Scientists.
aluminum sulfate; amitriptyline; electrolyte; excipient; magnesium sulfate; polyamide; potassium sulfate; theophylline; article; drug concentration; drug delivery system; drug diffusion; drug formulation; drug release; drug solubility; hydrogen bond; hydrophilicity; hydrophobicity; mathematical parameters; monolithic matrix; particle size; priority journal; static electricity; tablet matrix; Amitriptyline; Antidepressive Agents, Tricyclic; Chemistry, Pharmaceutical; Electrolytes; Excipients; Hydrophobic and Hydrophilic Interactions; Kinetics; Models, Molecular; Models, Statistical; Nylons; Particle Size; Phosphodiesterase Inhibitors; Solubility; Theophylline