Amorphous Solid

A solid form of a drug substance lacking long-range molecular order, characterized by higher free energy compared to its crystalline counterparts. Amorphous solids typically exhibit enhanced apparent solubility and faster dissolution rates (2-10 fold) but are thermodynamically unstable and may recrystallize during storage. Stabilization strategies include solid dispersions, spray-dried dispersions, and mesoporous carriers.

Примеры

• Vemurafenib: marketed as amorphous solid dispersion (co-precipitated with HPMC-AS) due to poor crystalline solubility
• Itraconazole Sporanox: amorphous form in HPMC matrix for adequate oral bioavailability
• Nifedipine: amorphous form has ~10x higher apparent solubility than crystalline form