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

• Published in: Drug development and industrial pharmacy 1998-01, Vol.24 (8), p.747-756
• Main Authors: Mura, P., Faucci, M. T., Manderioli, A., Furlanetto, S., Pinzauti, S.
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Blood. Blood coagulation. Reticuloendothelial system; Calorimetry, Differential Scanning; Fibrinolytic Agents - administration & dosage; Hot Temperature; Medical sciences; Microscopy, Electron, Scanning; Pharmacology. Drug treatments; Phthalic Acids - administration & dosage; Platelet Aggregation Inhibitors - administration & dosage
• ISSN: 0363-9045; 1520-5762
• DOI: 10.3109/03639049809082722

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.