title: Preparation and properties of new co-crystals of ibandronate with gluco- or galactopyranoside derivatives.
abstract: Mixtures 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.
authors.affiliation: Zentiva k.s., U Kabelovny 130, 102 37 Prague 10, Czech Republic.
authors.forename: Zbynek
authors.initials: Z
authors.lastname: Oktabec
authors.forename: Jiri
authors.initials: J
authors.lastname: Kos
authors.forename: Zuzana
authors.initials: Z
authors.lastname: Mandelova
authors.forename: Lenka
authors.initials: L
authors.lastname: Havelkova
authors.forename: Tomas
authors.initials: T
authors.lastname: Pekarek
authors.forename: Anna
authors.initials: A
authors.lastname: Rezacova
authors.forename: Lukas
authors.initials: L
authors.lastname: Placek
authors.forename: Marcela
authors.initials: M
authors.lastname: Tkadlecova
authors.forename: Jaroslav
authors.initials: J
authors.lastname: Havlicek
authors.forename: Jiri
authors.initials: J
authors.lastname: Dohnal
authors.forename: Josef
authors.initials: J
authors.lastname: Jampílek
mesh_terms: D003460:Crystallization; D004164:Diphosphonates / Q000737:chemistry*; D005697:Galactosides / Q000737:chemistry*; D005947:Glucose / Q000031:analogs & derivatives* / Q000737:chemistry*; D000077557:Ibandronic Acid; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013059:Spectrum Analysis, Raman / Q000379:methods
chemical_list: D004164:Diphosphonates; D005697:Galactosides; C046399:phenyl-D-galactopyranoside; D005947:Glucose; D000077557:Ibandronic Acid