Small-Scale Manufacture of Modified-Release Coated Beads For Preclinical Drug Discovery Research

Modified-release technologies are used early in discovery to

• enable mechanism/target testing of molecules with non-ideal pharmacokinetics,

• reduce dosing frequency,

• reduce stress to animals, and

• enable target validation requiring prolonged plasma levels.

 

The objective was to develop a “micro-scale” fluid-bed system that met the following criteria to enable these discovery studies:

• ~0.5- to 1-g batches (using ~100 mg of API),

• quick turnaround,

• a platform applicable to a wide range of API,

• tunable release with close to zero-order kinetics, and

• predictable release rate, based on API properties.

Topics: 
Modified & Targeted Release