Amorphous forms

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Why obtaining a new drug amorphous form


The amorphous solid state possesses several advantages in comparison to the crystalline state which allow enhanced forms of drugs to be produced. Many drugs when generated as an amorphous form will exhibit one or more of the following:


Solubility

The amorphous state is thermodynamically the form with the highest solubility. Consequently, amorphous forms will exhibit a greater solubility in a solvent than any crystalline form. Solubility advantages of factors >1000 have been observed between crystalline and amorphous drugs. The increased solubility of amorphous actives can lead to dramatically increased intrinsic dissolution rates when compared to crystalline forms.
Activery offers the production of stable amorphous microparticles which show significantly enhanced solubility when compared to a crystalline reference.

 

Wettability

For a drug to dissolve, its surface has first to be wetted by the surrounding fluid. Amorphous forms possess a chemically randomized surface which expresses equal amounts of hydrophobic and hydrophilic interactions which can lead to improved wettability expressed by a lower contact angle a of the drug particle surface with a liquid. A lower contact angle represents a higher degree of hydrophily with consequently faster surface wetting and faster dissolution.
Activery offers the generation of amorphous powders which show enhanced wetting through lower contact angles when compared to a crystalline starting material.

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