How Much Do You Know about Good Oral Candidates?

1. All poor oral exposure issues can be mitigated by optimizing the solid for m of the drug substance and/or the formulation.

1. True
2. False

2. What is the T50% of gastric emptying of a glass of water (240 ml)?

1. Approximately 15 min.
2. Approximately 20 min.
3. Approximately 30 min.

3. Which of the following is false:

1. Primary active transporters are directly coupled to an energy yielding process.
2. Secondary active transporters are indirectly coupled to the free energy yielding process via the utilization of the voltage or ion gradients generated by a primary active transporter.
3. Na+ symporters are frequent in eukaryotic cells and are an example of secondary active transporters.
4. All carrier-mediated transport is active transport.

4. High intrinsic hepatic clearance always translates into high in vivo hepatic clearance. No need to consider differences in microsomal and plasma protein binding.

1. True
2. False

5. In early discovery, a series of compounds within a chemotype exhibited poor bioavailability in rats. Which of the following studies would shed light on the underlying factors?

1. Assessment of solubility in simulated gastric and intestinal media
2. Studies in portal vein cannulated rats looking at portal and systemic drug concentrations
3. Studies in aminobenzotriazole-treated rats (inhibits CYP-mediated metabolism)
4. All of the above

6. What is not a method for producing amorphous dispersion formulations?

1. Hot melt extrusion
2. Solvent casting
3. Spray drying
4. Flash freezing

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ANSWERS: B, A, D, B, D, D