Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives†
AbstractMixtures of ibandronate monosodium salt with eleven gluco- and/or galacto-pyranoside derivatives as counterions were designed to prepare co-crystals with improved intestinal absorption. In general, gastrointestinal absorption of bisphosphonates after oral administration is approximately 1%. Co-crystals were generated by means of thermodynamically and/or kinetically controlled crystallization processes. Seventy-seven prepared samples were analyzed by means of FT-NIR, FT-Raman spectrometry and solid state NMR spectroscopy. New entities of ibandronate monosodium salt with phenyl-β-d-galactopyranoside were found and characterized. The absorption of these potential new co-crystals was investigated by means of PAMPA experiments. In the present study the relationships between the chemical structures of the studied compounds required for co-crystal generation are discussed.
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Oktabec, Z.; Kos, J.; Mandelova, Z.; Havelkova, L.; Pekarek, T.; Rezacova, A.; Placek, L.; Tkadlecova, M.; Havlicek, J.; Dohnal, J.; Jampílek, J. Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives. Molecules 2010, 15, 8973-8987.
Oktabec Z, Kos J, Mandelova Z, Havelkova L, Pekarek T, Rezacova A, Placek L, Tkadlecova M, Havlicek J, Dohnal J, Jampílek J. Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives. Molecules. 2010; 15(12):8973-8987.Chicago/Turabian Style
Oktabec, Zbynek; Kos, Jiri; Mandelova, Zuzana; Havelkova, Lenka; Pekarek, Tomas; Rezacova, Anna; Placek, Lukas; Tkadlecova, Marcela; Havlicek, Jaroslav; Dohnal, Jiri; Jampílek, Josef. 2010. "Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives." Molecules 15, no. 12: 8973-8987.