Here's what I found in answer to some of your questions.
whats so hard about making amorphous drugs?
"For most substances, the amorphous form is unstable, returning to
more stable crystalline form in a few minutes or hours."
why does one want them to be amorphous?
"The beauty of amorphous forms is that they have a higher
dissolution rate and solubility than crystalline forms. However, very
few drugs are naturally amorphous."
Unfortunately, the only top selling amorphous drugs I found are:
Accupril/Accuretic, which makes over $300 Million in revenues
Worldwide. is used to treat High Blood Pressure.
Intraconazole, an Acne medication seems to use amorphous substances
in order to improve bioavailability or absorption.
what are 3 situations where you want a drug to NOT be amorphous and
what are 3 top selling examples?
I think one situation that best sums up when a drug should NOT be amorphous
is when it does not dissolve easily in water.
"Improvement of solubility and oral bioavailability of a poorly
water-soluble drug, TAS-301, by its melt-adsorption on a porous
calcium silicate....The drug existed in an amorphous state in the
product and hardly recrystallized even after storing at a stressed
condition (60°C/80% RH for 3 days)."
"Drugs that dissolve in fat (fat-soluble drugs), such as the
anesthetic drug halothane, tend to concentrate in fatty tissues"
Please let me know if you have anymore questions.
amorphous (pfizer, glaxosmithkline..... and other pharmaceutical companies)