BME 6210 Small Molecule Stability -
Formulation Test With Solution
Experimental formats are used to... - ANSWER Determine drug stability.
A perfect world would want... - ANSWER 5 year expiration, "shelf life".
"Shelf-life" is defined by the FDA in two ways: - ANSWER 1. Product at least
90% potent from the manufacturing date.
2. Product must look and act as the day it was manufactured.
How to measure drug potency and stability? - ANSWER By adding stressors
to the formulation.
Different examples of stressors: - ANSWER 1. Temperature - Rate of reaction
increases with increasing temperature.
2. Humidity - Rate of reaction increases with increasing humidity.
3. Physical stress - Products tend to be crystals with different lattice energies.
Most common degradation reactions: - ANSWER 1. Hydrolysis - Adding
water across a bond.
2. Oxidation
, 3. Photolysis - Light
Zero Order Reactions: - ANSWER A ---(k0)---> B
-d[A]/dt = k0 for a zero order reaction - ANSWER [A] = [A]0 - k0t
Graph with a straight line for zero order reactions... - ANSWER [A] versus t
The slope of a zero order reaction is... - ANSWER k0
t50 for a zero order reaction is... - ANSWER t50 = (0.5[A]0) / k0
We care about t90 (90% potency) which is... - ANSWER t90 = (0.1[A]0) / k0
Example of a pseudo-zero order: - ANSWER Drug suspensions
- Solid, very slow degradation
- Not in equilibrium, the solid state amount will change
- Will plateau once all the solids dissolve
- Molecule that degrades is replaced by a non-degraded one
- Take dissolved ones out by degradation
Formulation Test With Solution
Experimental formats are used to... - ANSWER Determine drug stability.
A perfect world would want... - ANSWER 5 year expiration, "shelf life".
"Shelf-life" is defined by the FDA in two ways: - ANSWER 1. Product at least
90% potent from the manufacturing date.
2. Product must look and act as the day it was manufactured.
How to measure drug potency and stability? - ANSWER By adding stressors
to the formulation.
Different examples of stressors: - ANSWER 1. Temperature - Rate of reaction
increases with increasing temperature.
2. Humidity - Rate of reaction increases with increasing humidity.
3. Physical stress - Products tend to be crystals with different lattice energies.
Most common degradation reactions: - ANSWER 1. Hydrolysis - Adding
water across a bond.
2. Oxidation
, 3. Photolysis - Light
Zero Order Reactions: - ANSWER A ---(k0)---> B
-d[A]/dt = k0 for a zero order reaction - ANSWER [A] = [A]0 - k0t
Graph with a straight line for zero order reactions... - ANSWER [A] versus t
The slope of a zero order reaction is... - ANSWER k0
t50 for a zero order reaction is... - ANSWER t50 = (0.5[A]0) / k0
We care about t90 (90% potency) which is... - ANSWER t90 = (0.1[A]0) / k0
Example of a pseudo-zero order: - ANSWER Drug suspensions
- Solid, very slow degradation
- Not in equilibrium, the solid state amount will change
- Will plateau once all the solids dissolve
- Molecule that degrades is replaced by a non-degraded one
- Take dissolved ones out by degradation
