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Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers

100%

Marcoin W., Szulc-Musiol B.

Journal of Elementology

2011

tom 16

nr 4

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 in vitro 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. It 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.

Estimation of absorption of magnesium nicotinate and its derivatives with selected amino acids

84%

Marcoin W., Szulc-Musiol B.

Journal of Elementology

2009

tom 14

nr 2

313-321

Preparation of solid dispersions is a popular pharmaceutical technology designed to improve the solubility and absorption characteristics of drugs. Solubilizing and moisturizing of carriers show influence on therapeutic substances; although dissolution of molecular dispersion of particles of the therapeutic substance in a neutral carrier is of utmost importance. This paper present the results of the research on influence of modification the structure of magnesium nicotinate Mg(Nic) with ligands, glycine and arginine, on the absorption process of Mg2+ions in vitro. The absorption area was the small intestine of a rat. It was found that structural changes with an additional arginine or glycine ligand affect the absorption process of Mg2+ions. Moreover, the effect of hydrophilic carriers on the partition coefficient (log P) for the system of n-octanol and phosphate buffer was investigated for the solid dispersions containing the examined magnesium salts. Phosphatidylcholine (PC-45) and polyvinylpirrolidone (PVP K-30) were used as carriers for solid dispersions with of magnesium salts. It was confirmed that using auxiliary substances PC-45 and PVP changes significantly (p<0.05) P values, corresponding to increasing hydrophobic properties of solid dispersions of the examined salts. It was found that modification of the structure of magnesium nicotinate by amino acids such as arginine or glycine positively influences the absorption process Mg2+ ions. The research carried out on properties of the solid dispersions containing magnesium salts and phospatidylcholine (PC-45) or magnesium salts and polyvinylpirrolidone (PVP K30) showed positive influence of these auxiliary substances.

Ograniczanie wyników

2 Journal of Elementology

2 Marcoin W.

2 Szulc-Musiol B.

1 2011

1 2009

Wyniki wyszukiwania

Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers

Estimation of absorption of magnesium nicotinate and its derivatives with selected amino acids