Abstract
Azathioprine is an immunosuppressive drug for several inflammatory disorders. Due to its clinical relevance, to explore the solid-state properties for excipient compatibility in the product quality review process is essential. Fourier transform infrared spectroscopy, powder X-ray diffraction and thermal analysis (thermogravimetry/derivative thermogravimetry (TG/DTG), differential thermal analysis (DTA), and differential scanning calorimetry (DSC)) were applied. The compatibility studies evidenced that starch pregelatinized, colloidal silicon dioxide, and talc are fully compatible with azathioprine. However, stearic acid, magnesium stearate, and mannitol are incompatible after heat supply at temperatures easily reached by industrial processing. The nonlinear Vyazovkin isoconversional treatment performed the kinetic study of the thermal degradation. The activation energies were determined to clarify the influence of each excipient on the thermal drug stability, an essential procedure in the pharmaceutical development, and all over the commercial live span, in Good Manufacturing Practices.
Highlights
Safety and efficiency are the primary concern of the Pharmaceutical industry.[1,2] To inspect the global production, the health supervision regulatory agencies publish guidelines[3,4] to ensure the quality of the final product, promoting public health, as a set of procedures in the Good Manufacturing Practices (GMP) on the Pharmaceutical Inspection Co-operation Scheme (PIC/S).For tablets, the excipients have to be carefully selected, since they cannot show pharmacological activity
Adequate tools for data treatment obtained by process analytical technology (PAT) inserted in the production is crucial for GMP.[7]
For the AZA + MS binary, differential scanning calorimetry (DSC) curve exhibits the same endotherm of MS and another peak at Tonset = 254 °C, attributed to the AZA melting, but with an enthalpy of 1.22 J g−1, about 2% of the expected value, indicating that this signal refers to the fusion of remaining AZA, which did not interact with MS with heat supply
Summary
Safety and efficiency are the primary concern of the Pharmaceutical industry.[1,2] To inspect the global production, the health supervision regulatory agencies publish guidelines[3,4] to ensure the quality of the final product, promoting public health, as a set of procedures in the Good Manufacturing Practices (GMP) on the Pharmaceutical Inspection Co-operation Scheme (PIC/S).For tablets, the excipients have to be carefully selected, since they cannot show pharmacological activity. For the heating rates of 6, 10, 20, and 50 °C min−1, it was observed one endothermic response corresponding to AZA fusion, followed by another phenomenon identified as their exothermal decomposition.
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