Thermal Analysis as a Screening Technique in Preformulation Studies of Picotamide Solid Dosage Forms

Abstract

The potential compatibilities of several commonly used pharmaceutical excipients with picotamide were evaluated using differential scanning calorimetry (DSC). The effects of aging and of mechanical treatment (blending, grinding, or kneading) of samples were also evaluated. Hot-stage microscopy (HSM) and scanning electron microscopy (SEM) were used as complementary techniques to implement and assist in interpretation of the DSC results. DSC analysis evidenced a noticeable modification of drug thermal features in the mixtures with palmitic acid, stearic acid, stearyl alcohol, polyethylene glycol (PEG) 20,000, and sorbitol, but HSM analysis showed that the DSC behavior was mainly because of the drug dissolution in the melted excipient, which allowed the presence of important solid-solid interactions to be excluded. Compatibility with Mg stearate was also found, even if sample manipulation induced the partial conversion of Mg stearate in a pseudo-polymorphic modification. Mechanical stress displayed an increased hygroscopicity of mixtures with glucose and lactose, as well as some solid-solid interactions with lactose and mannitol.

Drug–excipient interactions in ketoprofen: A vibrational spectroscopy study

“…[17][18][19][20] Raman spectra of freshly prepared ketoprofen:PVP and ketoprofen:LAC PMs are represented in Figures 1(c) and 2(c), respectively. Both vibrational patterns can be interpreted as almost the direct sum of the pure ketoprofen and excipient spectra, allowing us to assume an absence of noteworthy intermolecular interactions in the newly prepared PMs.…”

Ketoprofen-poly(vinylpyrrolidone) physical interaction

“…Mura et al [8] described that ket-PVP K30 solid dispersion seems to form spontaneously from fresh physical mixture (PM) during differential scanning calorimetry DSC analysis. Abd-El-Bary et al [9] described that ket-PVP K30 mixtures were physically unstable on storage at temperature above 40 C, with subsequent alteration of IR-spectra and important decrease in dissolution rate of ketoprofen.…”

Characterization of Physico-Mechanical Properties of Indomethacin and Polymers to Assess their Suitability for Hot-Melt Extrusion Processs as a Means to Manufacture Solid Dispersion/Solution**Mailing address of the place where the work was carried out, Hoffmann-La Roche, Inc., 340 Kingsland Street, Nutley, NJ, 07110.

“…18,19 Based on Gordon-Taylor equation, 20 if drug and polymer are miscible then the mixture will show a single T g that ranges between the T g of pure components and would depend on the relative proportion of each component. The T g of the mixtures can be predicted using Gordon-Taylor equation (GT equation).…”