preparation and properties of new co-crystals of ibandronate with gluco- or galactopyranoside derivatives制备和性能的新co-crystals ibandronate glucou2014u2014或galactopyranoside衍生品.pdfVIP

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preparation and properties of new co-crystals of ibandronate with gluco- or galactopyranoside derivatives制备和性能的新co-crystals ibandronate glucou2014u2014或galactopyranoside衍生品.pdf

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preparation and properties of new co-crystals of ibandronate with gluco- or galactopyranoside derivatives制备和性能的新co-crystals ibandronate glucou2014u2014或galactopyranoside衍生品

Molecules 2010, 15, 8973-8987; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives † Zbynek Oktabec 1,2, Jiri Kos 3, Zuzana Mandelova 1,3, Lenka Havelkova 3, Tomas Pekarek 1, Anna Rezacova 1, Lukas Placek 1, Marcela Tkadlecova 1, Jaroslav Havlicek 1, Jiri Dohnal 1,3 and Josef Jampílek 1,3,* 1 Zentiva k.s., U Kabelovny 130, 102 37 Prague 10, Czech Republic 2 Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic 3 Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 612 42 Brno, Czech Republic † Preliminary results were presented at the Thirteenth Electronic Conference on Synthetic Organic Chemistry (ECSOC-13, /presentation/201), 1-30 November 2009 * Author to whom correspondence should be addressed; E-Mail: josef.jampilek@zentiva.cz; Tel.: +420-2 Fax: +420-2 Received: 22 November 2010; in revised form: 3 December 2010 / Accepted: 7 December 2010 / Published: 8 December 2010 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-cry