title: A novel approach for predicting the dissolution profiles of pharmaceutical tablets.
abstract: In this paper, the intrinsic dissolution profiles of naproxen (NAP) at pH values of 1.5 and 3.0 and of trimethoprim (TMP) at pH values of 1.5, 3.0, 5.0, 6.5 and 7.2 were measured. Meanwhile, the dissolution profiles of NAP and TMP from cylindrical tablets were measured at different temperatures (298.15K, 305.15K, 301.15K and 310.15K) and stirring speeds (50rpm, 100rpm and 150rpm) as well as at different pH values (1.5, 3.0, 5.0, 6.5 and 7.2). Additionally the pH-dependent solubilities of both APIs were measured and modeled. The chemical-potential-gradient model combined with the perturbed-chain statistical associating fluid theory (PC-SAFT) was applied to predict the dissolution profiles of the cylindrical tablets of NAP and TMP under different conditions based on the analysis of their intrinsic dissolution profiles as well as on the determination of the surface-area reduction of the API tablets during dissolution. It was shown that the predicted dissolution profiles of the tablets under different conditions were in a good accordance with the experimental findings.
authors.affiliation: TU Dortmund, Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, Emil-Figge Str. 70, D-44227 Dortmund, Germany.
authors.forename: Raphael
authors.initials: R
authors.lastname: Paus
authors.affiliation: TU Dortmund, Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, Emil-Figge Str. 70, D-44227 Dortmund, Germany.
authors.forename: Elena
authors.initials: E
authors.lastname: Hart
authors.affiliation: TU Dortmund, Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, Emil-Figge Str. 70, D-44227 Dortmund, Germany. Electronic address: Yuanhui.Ji@bci.tu-dortmund.de.
authors.forename: Yuanhui
authors.initials: Y
authors.lastname: Ji
mesh_terms: D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008956:Models, Chemical; D015394:Molecular Structure; D009288:Naproxen / Q000737:chemistry*; D033362:Powder Diffraction; D012995:Solubility; D013499:Surface Properties; D013607:Tablets; D013696:Temperature; D014295:Trimethoprim / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D013607:Tablets; D009288:Naproxen; D014295:Trimethoprim
keywords: Chemical-potential-gradient model; Drug solubility; PC-SAFT; Poorly-soluble drug; Surface area reduction; Tablet dissolution