Lecture 14

Question 1

US Life Expectancy

Answer 1

• increase in expectancy is based on drug development and better treatment by doctors
• experienced a dip in almost a year due to COVID-19
• Female is higher than male

Question 2

AntiViral Drugs and Solubility

Answer 2

• antiviral drugs are typically insoluble

Question 3

Solutions to Insolubility

Answer 3

Prodrug
- drug substance that is inactive in the intended pharmacological actions and is converted into active agent by metabolical transformation

Formulation
- Melt Extrusion
- Spray Drying

Question 4

Sofosbuvir

Answer 4

• prodrug
• converted to triphosphate and inhibits NS5B polymerase

Question 5

Antiviral Drugs Statistics

Answer 5

• 75% of molecules failed in preclinical
• 25% of molecules make it to Phase 1

Reasons
- 39% of Poor Bioavailability
- 30% Low Efficacy
- 11% High toxicity
- 10% Adverse Effects
- 10% Other

Question 6

Melt Extrusion

Answer 6

• creates an amorphous dosage form
• Place API and Polymer to destroy crystal of antiviral drug
• Melt the formulation
• mix the formulation
• homogenous dispersion

FORMS PELLETS THAT ARE PLACED IN CAPSULES

Question 7

Results of Melt Extrusion

Answer 7

• crystalline form is completely insoluble
• high gains in solubility with addition of polymer and API as well as the melting stage

Question 8

Spray Drying

Answer 8

• spray a solution of drug into a hot environment and the crystals are placed into a powder that are then processed
• disadvantage: large machine

Question 9

Results of Spray Drying

Answer 9

• crystalline has a small amount of blood level
• when spray dried, high gains in solubility as more of drug is seen in the blood plasma

Question 10

Conclusion of AntiViral Drugs

Answer 10

• needs to make a molecule that will inhibit the virus
• molecule must have little effect on normal cells and nontoxic
• formulations play at critical role in making these drugs soluble