Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers


Wydanie: 4 / 2011

Autorzy:

  • Marcoin W.,  Szulc-Musioł B.

Kategorie: Medicine and veterinary

DOI: 10.5601/jelem.2011.16.4.09

Abstrakt:

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.


Cytacja:

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

 

Słowa kluczowe:

magnesium levulinate, solid dispersion, log P, absorption, amino acids: glycine, arginine


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