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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Crystalline phase transition of ezetimibe in final product, after packing, promoted by the humidity of excipients: Monitoring and quantification by Raman spectroscopy

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dos Santos Farias, Marco Antonio [1] ; Felipe Soares, Frederico Luis [1] ; Carneiro, Renato Lajarim [1]
Total Authors: 3
[1] Univ Fed Sao Carlos, Dept Chem, Rodovia Washington Luiz Km 235, BR-13565905 Sao Carlos, SP - Brazil
Total Affiliations: 1
Document type: Journal article
Source: Journal of Pharmaceutical and Biomedical Analysis; v. 121, p. 209-214, MAR 20 2016.
Web of Science Citations: 5

Ezetimibe (EZT), in its anhydrous form, is a drug used for cholesterol and lipids reduction in blood plasma. The presence of Elf monohydrate in commercial tablets can change the solubility rate of the API, decreasing its activity. The objective of this work was to verify if the humidity present in the excipients could promote the phase transition from Elf anhydrous to hydrate. Initially the stability of the pure anhydrous form was monitored by Raman, at room temperature (23 degrees C) and relative humidity (75%). The MCR-ALS method showed that almost all Elf changed to hydrated form in 30 min. Then tablets of ezetimibe in the presence of its excipients were prepared and vacuum packed using a polyethylene film. Such tablet was monitored by Raman spectroscopy for 24 h in order to quantify the mixture of the crystalline forms. A multivariate calibration model using Raman spectroscopy and Partial Least Square (PLS) regression was built, with validation and cross validation errors around 0.6% (wt/wt), for both crystalline forms, and R-2 higher than 0.96. The PLS model was used to quantify the crystalline mixture of ezetimibe in the monitored tablet, after 24 h more than 70% of ezetimibe changed to the hydrated form. (C) 2016 Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 13/24941-9 - Chemometrics applied to the synthesis of pharmaceutical co-crystals using peptides and nutraceuticals as co-formers
Grantee:Renato Lajarim Carneiro
Support type: Scholarships abroad - Research
FAPESP's process: 10/16520-5 - Application of calibration chemometrics methods and multivariate curve resolution in Raman spectroscopy for qualitative, quantitative and polymorphism analyses in medicines
Grantee:Renato Lajarim Carneiro
Support type: Regular Research Grants