title: Evaluation of the crystalline and amorphous states of drug products by nanothermal analysis and Raman imaging.
abstract: In recent years, amorphous formulations and other special dosage forms of drug products have been investigated to achieve adequate solubility and disintegration. We have evaluated the distribution of crystalline and amorphous states of a drug product using Nanothermal analysis (Nano-TA) and Raman imaging methods. Compared to conventional differential scanning calorimetry, Nano-TA can be used to more rapidly characterize the crystalline and amorphous states of model formulations, including their ingredient distributions, without any sample preparation. In the current study, imaging maps obtained for specific model formulations were evaluated on the basis of their visual appearance and the physicochemical properties of the active pharmaceutical ingredient (API). In addition, the crystalline and amorphous states of the model formulations were distinguished by Raman mapping. Nano-TA was found to be useful for the characterization of crystalline and amorphous states of APIs and the distribution of other ingredients. This technology could be used to monitor the changes in crystalline forms of drug substances and dosage forms during processing. In addition, Nano-TA can be used to characterize amorphous states.
authors.affiliation: Drug Development Technology Center, Customer Joy Department, Eisai Co. Ltd., Honjo, Saitama 367-0048, Japan. k2-nakamoto@hhc.eisai.co.jp
authors.forename: Keizo
authors.initials: K
authors.lastname: Nakamoto
authors.forename: Tetsuhiko
authors.initials: T
authors.lastname: Urasaki
authors.forename: Satoko
authors.initials: S
authors.lastname: Hondo
authors.forename: Naokazu
authors.initials: N
authors.lastname: Murahashi
authors.forename: Etsuo
authors.initials: E
authors.lastname: Yonemochi
authors.forename: Katuhide
authors.initials: K
authors.lastname: Terada
mesh_terms: D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004055:Differential Thermal Analysis; D005079:Excipients / Q000737:chemistry; D007564:Japan; D008968:Molecular Conformation; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D033362:Powder Diffraction; D011786:Quality Control; D013059:Spectrum Analysis, Raman; D013607:Tablets
chemical_list: D005079:Excipients; D004364:Pharmaceutical Preparations; D013607:Tablets