Mebendazole crystal forms in tablet formulations. An ATR-FTIR/chemometrics approach to polymorph assignment
| Autor: | Natalia Lorena Calvo, Teodoro S. Kaufman, Rubén M. Maggio |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
Benzimidazole
Chemistry Pharmaceutical Clinical Biochemistry Mebendazole Analytical chemistry Pharmaceutical Science 030226 pharmacology & pharmacy 01 natural sciences Analytical Chemistry Chemometrics 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Anthelmintic drug Spectroscopy Fourier Transform Infrared Drug Discovery CRYSTAL POLYMORPHISM medicine ATR-FTIR/CHEMOMETRICS Fourier transform infrared spectroscopy MEBENDAZOLE Spectroscopy Active ingredient Principal Component Analysis Chromatography Otras Ciencias Químicas 010401 analytical chemistry Ciencias Químicas 0104 chemical sciences chemistry Polymorphism (materials science) FORM ASSIGNMENT Principal component analysis PRINCIPAL COMPONENT ANALYSIS Powders Crystallization CIENCIAS NATURALES Y EXACTAS Tablets medicine.drug |
| Zdroj: | RepHipUNR (UNR) Universidad Nacional de Rosario instacron:UNR |
| Popis: | Structural polymorphism of active pharmaceutical ingredients (API) is a relevant concern for the modern pharmaceutical industry, since different polymorphic forms may display dissimilar properties, critically affecting the performance of the corresponding drug products. Mebendazole (MEB) is a widely used broad spectrum anthelmintic drug of the benzimidazole class, which exhibits structural polymorphism (Forms A-C). Form C, which displays the best pharmaceutical profile, is the recommended one for clinical use. The polymorphs of MEB were prepared and characterized by spectroscopic, calorimetric and microscopic means. The polymorphs were employed to develop a suitable chemometrics-assisted sample display model based on the first two principal components of their ATR-FTIR spectra in the 4000-600 cm-1 region. The model was internally and externally validated employing the leave-one-out procedure and an external validation set, respectively. Its suitability for revealing the polymorphic identity of MEB in tablets was successfully assessed analyzing commercial tablets under different physical forms (whole, powdered, dried, sieved and aged). It was concluded that the ATR-FTIR/PCA (principal component analysis) association is a fast, efficient and non-destructive technique for assigning the solid-state forms of MEB in its drug products, with minimum sample pre-treatment. Fil: Calvo, Natalia Lorena. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina Fil: Kaufman, Teodoro Saul. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina Fil: Maggio, Ruben Mariano. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina |
| Databáze: | OpenAIRE |
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