| Texto completo | |
| Autor(es): |
dos Santos Farias, Marco Antonio
[1]
;
Felipe Soares, Frederico Luis
[1]
;
Carneiro, Renato Lajarim
[1]
Número total de Autores: 3
|
| Afiliação do(s) autor(es): | [1] Univ Fed Sao Carlos, Dept Chem, Rodovia Washington Luiz Km 235, BR-13565905 Sao Carlos, SP - Brazil
Número total de Afiliações: 1
|
| Tipo de documento: | Artigo Científico |
| Fonte: | Journal of Pharmaceutical and Biomedical Analysis; v. 121, p. 209-214, MAR 20 2016. |
| Citações Web of Science: | 5 |
| Resumo | |
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) | |
| Processo FAPESP: | 13/24941-9 - Químiometria aplicada à síntese de co-cristais farmacêuticos utilizando peptídeos e nutracêuticos como co-formadores |
| Beneficiário: | Renato Lajarim Carneiro |
| Modalidade de apoio: | Bolsas no Exterior - Pesquisa |
| Processo FAPESP: | 10/16520-5 - Aplicação de métodos quimiométricos de calibração e resolução multivariada de curvas em espectroscopia Raman para análise qualitativa, quantitativa e de polimorfismo em fármacos |
| Beneficiário: | Renato Lajarim Carneiro |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |