Lecture 14 Flashcards
1
Q
US Life Expectancy
A
- 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
2
Q
AntiViral Drugs and Solubility
A
- antiviral drugs are typically insoluble
3
Q
Solutions to Insolubility
A
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
4
Q
Sofosbuvir
A
- prodrug
- converted to triphosphate and inhibits NS5B polymerase
5
Q
Antiviral Drugs Statistics
A
- 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
6
Q
Melt Extrusion
A
- 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
7
Q
Results of Melt Extrusion
A
- crystalline form is completely insoluble
- high gains in solubility with addition of polymer and API as well as the melting stage
8
Q
Spray Drying
A
- spray a solution of drug into a hot environment and the crystals are placed into a powder that are then processed
- disadvantage: large machine
9
Q
Results of Spray Drying
A
- 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
10
Q
Conclusion of AntiViral Drugs
A
- 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
