Wisconsin Alumni Research Foundation

Abbvie Inc.

Abbvie Deutschland Gmbh and Co Kg

Abbott Gmbh & Co Kg

Lian Yu

Tian Wu

Geoff G Zhang

Markus Maegerlein

Melgardt M De Villiers

Jing Tao

Ye Sun

Mark D Ediger

Stephen Swallen

Ken Kearns

G Z Geoff

The present invention provides surface-stabilized amorphous pharmaceuticals comprising an amorphous pharmaceutical substrate coated with a biocompatible immobilizing material. Amorphous pharmaceutical substrates that are prone to surface enhanced crystallization benefit from the present coatings. The coated amorphous pharmaceuticals of the present invention maintain their amorphous state and, therefore, their solubility over extended periods of time, relative to uncoated pharmaceuticals.

Inhibiting surface enhanced crystallization of amorphous pharmaceuticals with ultrathin coatings

A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices. The method relies on the detection of the dissolution endpoint of a drug/polymer mixture prepared by cryomilling.

Method for evaluating the solubility of a crystalline substance in a polymer

The present invention provides vapor deposition methods that overcome the kinetic restrictions imposed by more conventional vapor deposition processes and liquid-cooling techniques to form amorphous molecular solids with greatly enhanced stabilities. The present methods produce amorphous molecular solids having stabilities, as measured by fictive temperature, that cannot be achieved using liquid-cooling methods.

Unusually stable glasses and methods for forming same

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Madison, WI, United States of America

Lian Yu