Thermal analysis as a screening technique in preformulation studies of picotamide solid dosage forms

Area of Science:

• Pharmaceutical Science
• Materials Science

Background:

• Understanding drug-excipient compatibility is crucial for stable pharmaceutical formulations.
• Picotamide is a pharmaceutical compound requiring compatibility assessment with common excipients.

Purpose of the Study:

• To evaluate the compatibility of picotamide with common pharmaceutical excipients.
• To investigate the impact of aging and mechanical stress on these compatibilities.

Main Methods:

• Differential Scanning Calorimetry (DSC) was the primary technique.
• Hot-Stage Microscopy (HSM) and Scanning Electron Microscopy (SEM) were used as complementary methods.
• Excipients included fatty acids, alcohols, polymers, and sugar alcohols.

Main Results:

• DSC indicated thermal changes with palmitic acid, stearic acid, stearyl alcohol, PEG 20,000, and sorbitol, primarily due to excipient melting and drug dissolution.
• Mg stearate showed compatibility, though mechanical stress caused pseudo-polymorphic changes.
• Mechanical stress increased hygroscopicity with glucose and lactose, and induced solid-solid interactions with lactose and mannitol.

Conclusions:

• Picotamide demonstrates good compatibility with most tested excipients, with observed changes attributed to physical processes like melting rather than chemical degradation.
• Mechanical stress can influence hygroscopicity and induce interactions with specific excipients like lactose and mannitol.
• HSM and SEM are valuable for interpreting DSC data in drug-excipient compatibility studies.