Class material

Question 1

draw an amine group

Answer 1

R-NH2

Question 2

draw an alcohol group

Answer 2

R-OH

Question 3

another name for alkene

Answer 3

olefine

Question 4

structure of ketone

Answer 4

R2C=O

Question 5

thiol structure

Answer 5

R-SH

Question 6

aldehyde structure

Answer 6

RHC=O

Question 7

amine structure

Answer 7

R-NH2

Question 7

ester structure

Answer 7

RC=O, C-OR

Question 8

carboxylic acid structure

Answer 8

RCOOH

Question 9

amide structure

Answer 9

RC=O, C-NR2

Question 10

formula for keq

Answer 10

[products]/[reactants]

Question 11

what does keq > 1 mean

Answer 11

products favored

Question 12

exothermic/endothermic reactions produce heat

Answer 12

exothermic reactions produce heat

Question 13

what sign represents energy difference between products and reactants?

Answer 13

Gibbs free energy (ΔG)

Question 14

two formula for Gibbs free energy

Answer 14

1. ΔH - TΔS
2. -RTln(keq)

Question 15

do things want to be in high or low energy state

Answer 15

low energy state

Question 16

Amino acids with nucleophile side chains

Answer 16

Cysteine, Lysine

Question 17

Amino acids with electrophile side chains

Answer 17

DEN Q
Aspartic acid, Glutamic acid, asparagine, glutamine

Question 18

Define two criteria used to determine shelf life

Answer 18

1. 90% potency of API
2. Product should look and perform as when first manufactured

Question 19

3 tests used for drug stability

Answer 19

1. Temperature
   *rxn’s double per +10C
2. Moisture
3. Ball milling

Question 20

Name 3 main drug degradation mechanism

Answer 20

Hydrolysis, Oxidation, Photolysis (photo degradation)

Question 21

Formulation stability concerns

Answer 21

1. Buffer
2. Antioxidants
3. Excipients (anything other than API)

Question 22

Different unit cells have different _____

Answer 22

properties

Question 23

What are generic drugs and how do they differ from their brand-name counterparts?

Answer 23

Same API, same dosage, different excipients

Question 24

Define polymorph

Answer 24

Same chemical composition, different unit cell

Question 25

What sort of structures are fast-dissolving tablets?

Answer 25

Amorphous structures (no unit cell, no 3D structure). High energy state

Question 26

3 characteristics of amorphous structures

Answer 26

1. Hydroscopic (absorb H2O) 2. Very hard to stabilize 3. Shorter shelf-life

Question 27

What is oxidation catalyzed by? How to prevent oxidation?

Answer 27

Fe, Cu, Light. Add antioxidants such as vitamin C or chelators

Question 28

(T/F) formulation stability can be affected by hydrolysis and oxidation

Answer 28

True

Question 29

Product of aspirin and acetaminophen

Answer 29

salicylic acid and acetoacetaminophen

Question 30

Analysis tools (5)

Answer 30

X-ray diffraction Differential scanning calorimetry IR Raman spectroscopy NMR

Question 31

(T/F) chemical stability includes formation and breaking of bonds

Answer 31

True

Question 32

Describe process associated with physical stability of proteins

Answer 32

denaturation of proteins/aggregation

Question 33

5 factors affecting chemical stability

Answer 33

Temperature Humidity pH Backbone flexibility Neighboring amino acids

Question 34

(T/F) Deamidation and hydrolysis are different

Answer 34

False. Deamidation is a type of hydrolysis

Question 35

Opaque meaning

Answer 35

Blurry; opposite of transparent

Question 36

4 factors influencing conformational stability

Answer 36

1. Vortex 2. Temperature 3. pH 4. Other excipients

Question 37

Define isoelectric point

Answer 37

Net electrical charge = 0 pH at which protein has equal number of positive and negative charge

Question 38

pH > pI means protein is _____ charged (vice versa)

Answer 38

negatively charged (deprotonated)

Question 39

Tablets vs Capsules

Answer 39

Tablets - cheaper to make - more stable

Question 40

Which has better bioavailability - tablets vs capsules

Answer 40

Capsules (higher SA)

Question 41

When are capsules used?

Answer 41

When API not compatible with compression

Question 42

What filters out anything bigger than 200 nm

Answer 42

Liver

Question 43

What filters out anything smaller than 200 nm

Answer 43

Kidneys

Question 44

First pass effect

Answer 44

Drug gets metabolized before getting to site of action

Question 45

2 major sites of drug metabolism

Answer 45

Intestines + liver

Question 46

Mechanisms of drug transport

Answer 46

1. Passive absorption - via concentration gradient 2. Active transport - via peptide transporters

Question 47

Drug release formulae

Answer 47

du/dt = dv/dt*Cs dv/dt = KA/h*D

Question 48

2 advantages of pulmonary delivery 2 disadvantages

Answer 48

1. Lower dosage required 2. Direct access to target organ -> can avoid first pass effect, lower dose 1. Expensive 2. Not compatible with all