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Issue 88, 2016, Issue in Progress
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A new polymorphic form and polymorphic transformation of loratadine

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Abstract

In this work, a new form of loratadine (Form B) was prepared from a 20% methanol and 80% water mixture and characterized by polarizing microscopy (POM), scanning electron microscopy (SEM), powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The dissolution, solubility and interfacial energy of Form B in water were measured and compared with those of amorphous and Form A loratadine. In addition, the solid-state transformations of loratadine solid forms were investigated by hot-stage microscopy (HSM) and DSC while the non-isothermal crystallization of amorphous loratadine was studied by DSC. It was found that Form B has a unique acicular structure and PXRD pattern, which are different from Form A. Moreover, Form B has a higher equilibrium solubility compared with Form A. The results of the solid-state transformation investigation (DSC) shows that the amorphous form was changed to the new polymorph B at 106.7 °C and Form B converted exothermally to Form A at 93.9 °C during heating. In the non-isothermal crystallization of amorphous loratadine, the crystallization rate constant (Zt) increased with the increasing heating rate and the Avrami exponent (n) was found to be about 3. Hopefully, Form B will be considered to be a promising approach to improve the loratadine solubility/dissolution rate.

Graphical abstract: A new polymorphic form and polymorphic transformation of loratadine

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Publication details

The article was received on 30 May 2016, accepted on 24 Aug 2016 and first published on 02 Sep 2016


Article type: Paper
DOI: 10.1039/C6RA14021A
RSC Adv., 2016,6, 85063-85073

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    A new polymorphic form and polymorphic transformation of loratadine

    R. Chang, Q. Fu, P. Yu, L. Wang, Y. Li, W. Du, C. Chang and A. Zeng, RSC Adv., 2016, 6, 85063
    DOI: 10.1039/C6RA14021A

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