What effect does converting a crystalline drug form into an amorphous solid have on solubility?
Answer
It significantly increases apparent solubility and dissolution rate.
A major strategy for formulating poorly soluble drugs involves modifying the physical state of the Active Pharmaceutical Ingredient (API). Crystalline solids possess a highly ordered, repeating internal structure that requires a significant input of energy to break apart before dissolution can occur. In contrast, converting this material into an amorphous solid removes this regular structure. The amorphous state is inherently less stable energetically, making it far more willing to dissolve in a solvent. This structural change results in a marked increase in both the apparent solubility (the maximum amount that dissolves) and the rate at which dissolution proceeds.
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