Mechano-chemical decomposition of drugs through galenic processes

Investigation of Solid Phase Composition on Tablet Surfaces by Grazing Incidence X-ray Diffraction

“…On the contrary, TP-MH powder kept under similar conditions was stable. During compaction, primary friction and fracture of the particles can bring an increase of both entropy and enthalpy and can thus stimulate such a physical change (10,44). The role of shear stress has been described in detail for the polymorphic transformation of chlorpropamide (19).…”

“…This compaction-mediated phenomenon could be further explained by the concept of "mechanical activation" (10,44). Hüttenrauch et al reported that the chemical decomposition of ergocalciferol was promoted after compaction, and this effect was also related to the applied compaction pressure during tablet preparation.…”

Spiers Memorial Lecture: Mechanochemistry, tribochemistry, mechanical alloying – retrospect, achievements and challenges

“…In the chemical and pharmaceutical industry, where mechanical treatment is a part of a technological process, any change to the crystal structure – disordering, loss of crystallinity, polymorphic transitions – can be either beneficial, or detrimental, and must therefore be carefully controlled. 72,81,82,94,100,103,163–175 Mechanical treatment is a wide-spread technique of improving dissolution kinetics of poorly soluble drugs – via preparing fine particles with a high surface area, amorphization, polymorphic transformations. Radicals, active states, metastable molecular forms, like zwitterions that are formed on mechanical treatment, can be long-lived, especially if stabilized at the interfaces in mechanocomposites.…”

“…Very often mechanical treatment gives solid dispersions and mechanocomposites. 103,165,166,177,207–213 “Dry extraction” of biologically active compounds from plants has proved to be an efficient alternative to traditional multi-stage extraction using organic solvents. 214–219…”