Artículos de revistas
Compatibility of sildenafil citrate and pharmaceutical excipients by thermal analysis and LC-UV
Registro en:
Journal Of Thermal Analysis And Calorimetry. Springer, v. 111, n. 3, n. 2037, n. 2044, 2013.
1388-6150
WOS:000315298800050
10.1007/s10973-012-2292-8
Autor
Julio, TA
Zamara, IF
Garcia, JS
Trevisan, MG
Institución
Resumen
The evaluation of sildenafil citrate (SC), the best-selling drug for treatment of impotence, for compatibility with various excipients was investigated using thermal and isothermal stress testing. Differential scanning calorimetry (DSC), hot-stage microscopy (HSM) and liquid chromatography (LC) with ultraviolet detection were successfully employed to investigate the compatibility between SC and various excipients commonly used in solid form in the pharmaceutical industry. The studies were performed using 1:1 (m/m) drug/excipient physical mixtures and samples were stored under accelerated stability conditions (40 A degrees C at 75% relative humidity). All excipients tested (such as colloidal silicon dioxide, croscarmellose sodium, lactose, mannitol and sucrose) showed potential incompatibilities by DSC and LC analysis after accelerated stability testing. However, some incompatibilities were not detected by the DSC method and were observed only when LC analysis was performed. HSM was able to differentiate active pharmaceutical ingredient degradation from solubilisation, supporting the interpretation of DSC in excipients where thermal events either overlapped or disappeared. The combination of both the analytical techniques (DSC and LC) and use of a stability chamber is extremely helpful in detecting incompatibilities and providing more robust and accurate approaches for pre-formulation studies. 111 3 2037 2044 Fundação de Amparo à Pesquisa do Estado de Minas Gerais (FAPEMIG) Minas Gerais State Research Foundation (FAPEMIG) [APQ-00410-09, APQ-02805-10]