The use of MTDSC to assess the amorphous phase content of a micronised drug substance

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

“…8 During postmilling storage, these amorphous regions, not being at thermodynamic equilibrium, may transform back to the crystalline state and affect long-term stability in terms of powder properties such as particle size distribution, specific surface area, chemical and physical reactivity, dissolution, and finally the drug product performance. 9 Batch-to-batch reproducibility of the materials with different degrees of crystalline disorder is another major concern in the pharmaceutical industry. 8 In order to stabilize the unstable amorphous form, comilling or co-grinding with amorphous excipients such as polyvinyl pyrrolidone (PVP), magnesium aluminometasilicate (Neusilin US2), etc., has been employed.…”

Recent Approaches of Solid Dispersion: A New Concept Toward Oral Bioavailability Sabitri Bindhani* , Snehamayee Mohapatra

“…Guinot and Lavillar [49] had described that this method was successfully used to detect and quantify amorphous phase transition. It has significant benefits over conventional DSC.…”

Detection of a Minor Amorphous Phase in Crystalline Etoricoxib by Dynamic Mechanical Analysis: Comparison with Raman Spectroscopy and Modulated Differential Scanning Calorimetry

“…Unlike first-order transitions such as vaporization, fusion, and sublimation, easily detected by their associated latent heats, the glass transition is discerned solely by a finite step change in the heat capacity. 44,45 Weak or subtle glass transitions are, therefore, barely discernable by conventional DSC methods. MDSC is inherently more sensitive, permitting the separation of thermally reversible transitions such as glass transitions from nonreversible events.…”

“…The fraction of amorphous material within the sample is simply related linearly to the magnitude of the step change in reversible heat capacity. 45 The calibration curve is shown in Figure 4 with an LOD of approximately 5%. Similar LODs for amorphous Carvedilol was obtained by Venkatesh et al 24 using MDSC (5%).…”