Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers
Wydanie: 4 / 2011
Kategorie: Medicine and veterinary
Among the methods applied to ensure optimal pharmaceutical availability of a drug is the incorporation of solid dispersions, i.e. combinations containing a therapeutic substance and a carrier deprived of its pharmacological activity. While manufacturing solid dispersions, special attention must be paid to carriers with a polymeric structure and hydrophilic properties, e.g. polyvinylpyrrolidone (PVP) and also phosphatidylcholine (PC). The aim of this study has been to evaluate the influence of the carriers PVP and PC 45 on pharmacokinetic parameters of Mg2+ absorption from Mg(Lev)2, Mg(LevGly), Mg(LevArg) as well as from solid dispersions containing these salts. The o/w partition coefficient was determined and the log P value calculated for pure salts and for solid dispersions containing the salts during this study. The process of Mg2+ absorption was examined m v tro on a model of the rat's small intestine. Our analysis of the results indicates that addition of PVP or PC 45 to solid dispersions (containing magnesium levulinate salts) significantly improves the degree of Mg2+ ion absorption. lt has been found that addition of PVP and PC 45 to solid dispersions with magnesium levulinate salts significantly influences the rate of Mg2+ absorption from the formulations. Moreover, the results indicate that additional ligand (glycine or arginine) in the structure of magnesium levulinate triggers the effect consisting in depressed lipophilicity for these compounds. Using the PVP or PC 45 carriers for making solid dispersions containing magnesium levulinate and derivatives with glycine or arginine ligands is quite a promising solution for attaining improved pharmaceutical availability of drugs.
Marcoin W., Szulc-Musioł B. 2011. Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers. J. Elem. 16/4: 603-612, DOI - 10.5601/jelem.2011.16.4.09