Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives

Molecules

Zbynek Oktabec¹  Jiri Kos¹  Zuzana Mandelova¹  Lenka Havelkova¹  Tomas Pekarek¹  Anna Rezacova¹  Lukas Placek¹  Marcela Tkadlecova¹  Jaroslav Havlicek¹  Jiri Dohnal¹ 

[1] ¹Zentiva k.s., U Kabelovny 130, 102 37 Prague 10, Czech Republic

关键词: ibandronate;    d-glucopyranosides;    d-galactopyranosides;    co-crystals;    FT-NIR;    FT-Raman;    CP/MAS NMR;    PAMPA;   

DOI  :  10.3390/molecules15128973

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.