Preparation and solid-state characterization of nonstoichiometric cocrystals of a phosphodiesterase-IV inhibitor and L-tartaric acid

Crystal Growth and Design

Volumn 6, Issue 3, 2006, Pages 690-700

  Variankaval, Narayan ^a   Wenslow, Robert ^a   Murry, Jerry ^a   Hartman, Robert ^a   Helmy, Roy ^a   Kwong, Elizabeth ^b   Clas, Sophie D ^b   Dalton, Chad ^b   Santos, Ivan ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 33645320255     PISSN: 15287483     EISSN: None     Source Type: Journal    
DOI: 10.1021/cg050462u     Document Type: Article

References (25)

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21. See the Supporting Information.
22. The equilibrium solubility was evaluated by stirring excess solid in water for ca. 16 h in the absence of light at 25 °C. The supernatant was analyzed using a HP8453 UV spectrophotometer.
23. http://www.petrik.com/PUBLIC/library/misc/acid_base_pk.htm, accessed 29 Dec 2003.
24. Routine SS-NMR could not clearly locate ethanol in the crystal because of peak overlap with the free base and the complicated nature of the spectrum.
25. It was not possible to describe the exact nature of the residual solvents-surface-bound versus incorporated in the crystal lattice-with the current data. However, analysis of TG-MS data indicates that ethanol and water are both released from the solids only at higher temperatures, with ethanol being somewhat more tightly bound than water. See the Supporting Information for details.