Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmaceutics > T2 - Week 3 > Flashcards

T2 - Week 3 Flashcards

1
Q

What are the categories of stability within drug development?

A
  1. Stability of the drug substance
  2. Stability of the drug substance in drug product
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is a drug product?

A

The finished dosage form that contains a drug substance in association with other active or inactive ingredients

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the identifications of instability?

A
  1. Physical
  2. Chemical
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are indicators of physical instability of a drug?

A
  1. Change in physical properties such as color, odor, taste, or texture
  2. Microbiological instability when a product grows signs of microbial growth (molds)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are indicators of chemical instability?

A

The integrity of the chemical structure of the active ingredient is degraded

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What might occur with the drug if it has been chemically degraded?

A
  1. Loss in efficacy
  2. Toxicity concerns
  3. Therapeutic and toxicological instability
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What kind of reaction is degradation?

A

Decomposition

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What factors affect the rate of a decomposition reaction?

A
  1. Concentration of reactants
  2. Reaction temperature
  3. Presence of catalysts
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are catalysts?

A

Speeds up chemical reaction by lowering activation energy (threshold)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the factors that can cause instability of a drug?

A
  1. Moisture and water
  2. Temperature
  3. Light
  4. Excipients
  5. pH of the environment
  6. Oxygen
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What reactions cause water to destabilize the drug in a drug product?

A
  1. Hydrolysis
  2. Isomerization (Racemization)
  3. Polymerization
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What reactions cause temperature to destabilize the drug in a drug product?

A
  1. Hydrolysis
  2. Oxidation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What reactions cause light to destabilize the drug in a drug product?

A
  1. Photolysis
  2. Oxidation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What reactions cause pH to destabilize the drug in a drug product?

A
  1. Hydrolysis
  2. Oxidation
  3. Isomerization (Racemization)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What reactions cause oxygen to destabilize the drug in a drug product?

A

Oxidation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is the most common drug degradation pathway?

A

Hydrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is hydrolysis?

A

When the OH group of a water molecule provides a nucleophile attack with a susceptible functional group on a drug molecule to degrade the drug (typically C=O groups)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What catalyzes hydrolysis?

A

H+ (acids) and OH- (base)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What are the susceptible functional groups for hydrolysis?

A
  1. Esters
  2. Amides
  3. Lactone
  4. Lactam
  5. Carbamate
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What are common drugs that can be effected by hydrolysis?

A
  1. Aspirin (ester linkages)
  2. Penicillins (Lactam ring)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are methods to control hydrolysis?

A
  1. Reduce or eliminate water from formulation
  2. Control pH with buffers, HCl or NaOH
22
Q

How do we reduce or eliminate water from a formulation?

A
  1. Using co-solvents
  2. Suspension of drug in a non-aqueous vehicle
  3. Protection from humidity by applying a waterproof coating
  4. Supply the drug product in a dry powder for reconstitution
  5. Suppress degradation by making the drug less soluble
23
Q

How do we determine what buffer to select from?

A
  1. Determine the optimum pH and adjust at which pH the drug is most stable.
  2. Design buffers based on the pKa, route and compatibility with the other ingredients in the formulation.
24
Q

What are the storage conditions to prevent hydrolysis?

A
  1. Dry environment: 40-60% humidity not in refrigerator
  2. Low temperature can stabilize liquid dosage forms
25
How should drugs be packaged to prevent hydrolysis?
Keep in a tightly closed container
26
What is oxidation?
Involves either the removal of an electropositive atom (hydrogen), radical or electron, or the addition of an electronegative atom (oxygen) or radical
27
What are the concurrent reactions caused by autooxidation?
1. Initiation 2. Propagation 3. Termination
28
What functional groups can be degraded by oxidation?
1. Aldehydes 2. Alcohols 3. Phenols 4. Sugars 5. Alkaloids 6. Unsaturated fats and oils
29
What are example drugs that can be influenced by oxidation?
1. Steroids (hydrocortisone) 2. Polyunsaturated fatty acids 3. Thiamine 4. Catecholamines
30
What are the methods to control oxidation?
1. Using chelating agents that trap trace metals from being oxidized 2. Using antioxidants 3. Replacing air with nitrogen gas or carbon dioxide to remove dissolved O2 4. Controlling pH by buffering because most drug oxidized at acidic pH in protonated form
31
What are examples of antioxidants used for aqueous products?
Sulfites
32
What are examples of antioxidants used for oleaginous products?
1. Alpha-tocopherol 2. Ascorbyl palmitate
33
How do we store drugs prone to oxidation?
Low temperature because activity of metal ions and hydroxyl ions are reduced
34
How do we package drug prone to oxidation?
1. Light resistant or opaque containers cause light can catalyze oxidations 2. Solid oral forms have sealed bottles with foil before dispensing
35
What happens if a drug is degraded by light?
1. Loss in potency 2. Discoloration 3. Formation of precipitate
36
What causes the photochemical reaction of a drug?
1. The wavelength of the incident light is within the range of absorption of the drug so the drug absorbs radiation and degrades 2. Absorption of radiation by excipients in the formulation (photo-sensitizers) which transfer the absorbed energy to the drug, causing it to degrade.
37
How can photodecomposition occur after a drug is applied?
Sunlight can penetrate skin to a certain depth causing photo-degradation of drugs circulating in the surface capillaries or in the eyes of patients receiving the drug
38
How do we control photolysis?
Coating tablets with vinyl acetate (polymer) containing oxybenzone an UV absorbers reducing discoloration and degradation
39
How do we package drugs sensitive to photolysis?
1. The use of colored glass containers and storage in a dark. 2. Amber glass excludes light of wavelength <470 nm and so affords considerable protection of compounds sensitive to ultraviolet light.
40
What is isomerization/racemization?
The process of conversion of a drug into its optical or geometric isomers
41
How can isomers affect the probability for degradation?
1. Conversions can result in a loss of therapeutic activity due to isomerization/racemization 2. Loss of activity of solutions of adrenaline at low pH. 3. In acidic conditions, tetracyclines undergo epimerization to toxic epimer.
42
What are methods of controlling isomerization/racemization?
1. Reducing or eliminating water from formulation 2. Control pH with buffers, HCl, or NaOH
43
What is polymerization?
The process by which two or more identical drug molecules combine together to form a complex long-chain molecule
44
What is an example drug that is effected by polymerization?
Aminopenicillins (ampicillin sodium) in concentrated aqueous solutions
45
What is the temperature spec for cold?
<8C or <46F
46
What is the temperature spec for refrigerator?
2-8C or 36-46F
47
What is the temperature spec for freezer?
-10- -20C or 14- -4F
48
What is the temperature spec for cool?
8-15C or 46-59F
49
What is the temperature spec for room temperature?
20-25C or 68-77F
50
What is drug stability?
The extent to which a product retains, within specified limits, and throughout its period of storage and use the same properties and characteristics that it possessed at the time of its manufacture or compounding
51
What the keys of pre-formulation studies?
1. Solubility analysis 2. Dissolution rate 3. Stability 4. pKa 5. Partition coefficient (Log P)

Pharmaceutics (27 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions