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Liquid-free milling to prepare a cocrystal of ibuprofen and nicotinamide

  • Journal of the Korean Crystal Growth and Crystal Technology
  • Abbr : J. Korean Cryst. Growth Cryst. Technol.
  • 2016, 26(6), pp.232-237
  • DOI : 10.6111/JKCGCT.2016.26.6.232
  • Publisher : The Korea Association Of Crystal Growth, Inc.
  • Research Area : Engineering > Materials Science and Engineering
  • Received : October 7, 2016
  • Accepted : October 21, 2016
  • Published : December 31, 2016

Jinok Ham 1 Jisun Jang 1 IL WON KIM 1

1숭실대학교

Accredited

ABSTRACT

Cocrystallization of active pharmaceutical ingredients has been widely recognized as a versatile tool to regulate the physical properties of pharmaceutical compounds through designed crystal structures. Grinding or milling has been especially useful to screen the feasibility of cocrystal formation, and the addition of a small amount of liquid is routinely necessary. In the present study, the effect of temperature was studied for the milling cocrystallization of ibuprofen and nicotinamide to establish a liquid-free method. The milling-induced cocrystallization was more effective with liquid nitrogen cooling than at room temperature, which was confirmed by XRD and DSC analyses. This behavior was attributed to the limited molecular mobility below the glass transition temperatures of the cocrystal components, which made it effective to destruct the crystals of raw materials and consequently form the ibuprofen/nicotinamide cocrystal. Further studies would be necessary to establish the utility of the current conclusion to the field of pharmaceutical crystallization.

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