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Issue 3, 2015
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Thermodynamics and preliminary pharmaceutical characterization of a melatonin–pimelic acid cocrystal prepared by a melt crystallization method

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Abstract

Pharmaceutical cocrystals have been extensively investigated as a promising approach to improve drugs' physicochemical properties. Cocrystals are usually prepared using solution-mediated methods and grinding methods. In this study, a cocrystal of pimelic acid with poorly soluble melatonin was produced using a melt crystallization method by controlling the crystallization within a specific temperature range. The cocrystal was characterized by infrared spectroscopy, powder and single crystal X-ray diffraction. The binary phase diagram and the formation enthalpy established by differential scanning calorimetry provided the rationale for this spontaneous cocrystallization system. The cocrystal exhibited higher apparent solubility, a faster dissolution rate and acceptable stability as compared to the original melatonin. The study has shown that the melt crystallization method can be considered as a competitive route for producing pharmaceutical cocrystals with improved properties and the thermodynamic investigation can provide in depth understanding and guidance on the melt crystallization of cocrystals.

Graphical abstract: Thermodynamics and preliminary pharmaceutical characterization of a melatonin–pimelic acid cocrystal prepared by a melt crystallization method

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Publication details

The article was received on 18 Sep 2014, accepted on 01 Nov 2014 and first published on 07 Nov 2014


Article type: Paper
DOI: 10.1039/C4CE01921K
Author version available: Download Author version (PDF)
Citation: CrystEngComm, 2015,17, 612-620
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    Thermodynamics and preliminary pharmaceutical characterization of a melatonin–pimelic acid cocrystal prepared by a melt crystallization method

    Y. Yan, J. Chen and T. Lu, CrystEngComm, 2015, 17, 612
    DOI: 10.1039/C4CE01921K

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