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Solid‐State and Solution‐Mediated Polymorphic Transformation of Rifampicin
Author(s) -
Jing Dingding,
Gu Yuan,
Xia Huiming
Publication year - 2018
Publication title -
chemical engineering and technology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.403
H-Index - 81
eISSN - 1521-4125
pISSN - 0930-7516
DOI - 10.1002/ceat.201700233
Subject(s) - transformation (genetics) , rifampicin , chemistry , solid state , chemical engineering , materials science , thermodynamics , physics , antibiotics , engineering , biochemistry , gene
Rifampicin, a semisynthetic broad‐spectrum antibiotic with antibacterial activity for a variety of pathogenic microorganisms, has three crystal forms, namely, I, II, and SV. Forms I and II are bioavailable. Solid‐state polymorphic transformation (SST) from Form II to I and solution‐mediated polymorphic transformation (SMT) from Form I to II were investigated by offline X‐ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR), respectively. Solubility and supersolubility of rifampicin Forms I and II in different solvents were obtained using the static method and turbidity meter method separately. The thermodynamic study of rifampicin proved that crystal Form I was more stable than Form II. These studies were necessary to optimize the crystallization process and crystal form controlling. The bulk density which influences significantly the drug loading capacity was clearly developed.