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Usage Statistics Cite this paper as: Jampilek, J.; Oktabec, Z.; Rezacova, A.; Placek, L.; Kos, J.; Havelkova, L.; Dohnal, J.; Kral, V. Preparation and Properties of New Co-crystals of Ibandronate. In Proceedings of the 13th Int. Electron. Conf. Synth. Org. Chem., 1-30 November 2009; Sciforum Electronic Conferences Series, 2009, c001:1-6.
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13th Int. Electron. Conf. Synth. Org. Chem. 2009, c001:1-6
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Preparation and Properties of New Co-crystals of Ibandronate
Josef Jampilek 1,2,* 
, Zbynek Oktabec 1, Anna Rezacova 1, Lukas Placek 1,2, Jiri Kos 2, Lenka Havelkova 2, Jiri Dohnal 1,2 and Vladimir Kral 1,3
, Zbynek Oktabec 1, Anna Rezacova 1, Lukas Placek 1,2, Jiri Kos 2, Lenka Havelkova 2, Jiri Dohnal 1,2 and Vladimir Kral 1,31 Zentiva a.s., U kabelovny 130, 102 37 Prague 10, Czech Republic; E-mail: josef.jampilek@zentiva.cz; Tel. +420-2-67243695; Fax: +420-2-72701331;
2 Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic;
3 Department of Analytical Chemistry, Faculty of Chemical Engineering, Institute of Chemical Technology, Technicka 5, 16628 Prague 6, Czech Republic;
* Author to whom correspondence should be addressed.
(This article belongs to the section C. Bioorganic Chemistry and Natural Products)
Abstract: Polymorphism of active pharmaceutical ingredients (APIs) gets increasing attention as an important physico-chemical parameter influencing bioavailability and stability of API and pharmaceuticals. Co-crystals of API with common pharmaceutical excipients become very important as a tool to tune up solubility and absorption. Bisphosphonates (e.g. alendronate, risedronate, ibandronate) are widely used in clinical practice. They are indicated for the treatment and prevention of osteoporosis. They are powerful inhibitors of bone resorption, but their gastrointestinal adsorption is only about 1(percent) due to their high hydrophilicity. Some experiments were designed to prepare co-crystals of ibandronate. In the present study various mixtures of ibandronate and excipients were prepared. All the prepared mixtures (solid compounds) and/or new entities were analyzed by means of FT-NIR spectroscopy. The absorption of potential new co-crystals was investigated by means of the PAMPA experiments.
Keywords: Bisphosphonates; Co-crystals; FT-NIR; PAMPA
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