Dosage Form Design

Question 1

Definition of Drug

Answer 1

An agent intended for use in the diagnosis, mitigation, treatment cure or prevention of disease in humans/animals

Question 2

Chemical syntheses is the major source of drug for most compounds due to what?

Answer 2

Advancements in chemistry, purification and engineering

Question 3

What are the four main sources of drug compounds?

Answer 3

Chemical syntheses
Plants
Animals
Humans

Question 4

Define drug delivery

Answer 4

Development of the most appropriate dosage form (preparation, formulations) that allow for patient to take the medication in the most convenient and acceptable manner

Question 5

Define “Dosage Forms”

Answer 5

Any physical form that consists of both active ingredients and pharmaceutical excipients

Question 6

How many medication doses do most dosage forms usually contain?

Answer 6

One

Question 7

What are the 6 major reasons to make appropriate dosage forms out of drug compounds?

Answer 7

1) To prevent active ingredients from degradation (physical/chemical/biological, in vitro and in vivo)
2) To conceal unpleasant flavor, taste or odor of active ingredients or pharmaceutical excipients
3) To facilitate mass industrial production of drug products
4) To use accurate dose of active ingredients
5) To provide various product choices to patients and consumers
6) To enhance therapeutic compliance and outcome

Question 8

What is the major goal of drug delivery?

Answer 8

To obtain the highest drug effects in the simplest administration way

Question 9

Routes of drug administrations:

Answer 9

Oral, parenteral, transdermal, nasal, buccal, sublingual, ophthalmics, pulmonary, rectal, topical, etc.

Question 10

Therapeutic effects can be either:

Answer 10

Systemic or Site-specific

Question 11

True or False: Systemic products can only have systemic effects

Answer 11

False: systemic formulations can have site specific effects and topical formulations can have systemic effects

Question 12

What are the 6 stages in drug discovery that must be done before becoming a product for human application?

Answer 12

1) New Chemical Entity
2) Preclinical Studies
3) Investigational New Drug Application
4) Clinical Trials
5) New Drug Application
6) Post-marketing

Question 13

The finding of a compound as a potential drug candidate is apart of what stage?

Answer 13

1) New chemical entity

Question 14

What is entailed in finding a New Chemical Entity?

Answer 14

Syntheses, extraction, separation and purification

Question 15

What do Preclinical Studies determine?

Answer 15

The suitability of an NCE as a therapeutic agent

Question 16

What do preclinical studies investigate?

Answer 16

Early stage: physical/chemical characterization, pharmacological/toxicological evaluations and in vivo behaviours.
Late stage: long term toxicity, formulation development/assessment, and prep for new drug product launch.

Question 17

When can clinical trials on human subjects begin?

Answer 17

After the health authority has reviewed the Investigational New Drug application and approved it for safety.

Question 18

Describe the three phases of clinical trials.

Answer 18

1) drug safety in 20-100 subjects
2) drug efficacy in 100’s of people
3) drug efficacy and evaluation in 1000’s of people

Question 19

What is involved in the New Drug Application?

Answer 19

Submission of complete information of a chemical entity for review by the health authorities, including everything from physiochemical characterization, pharmacology, toxicology, clinical results, to formation, production and quality control.

Question 20

How long does it take for a new drug product to go through whole process?

Answer 20

5-10 years

Question 21

What are the two major areas that are explored completely before final decision is made to market?

Answer 21

Drugs In vitro

Drugs In vivo

Question 22

In vitro drug testing includes:

Answer 22

Assessing basic characteristics of chemical compounds (physical and chemical properties, interaction with other dugs, stability)

Question 23

What are the four biological stages in vivo that all drugs undergo?

Answer 23

Absorption
Distribution
Metabolism
Excretion

Question 24

Bioavailability is one of the principle criteria to evaluate effectiveness of dose form, define it.

Answer 24

The rate and extent of an active ingredient from a formulation to the site of action

Question 25

The comparison of bioavailability of different formulations, batches or products with the same active ingredient

Answer 25

Bioequivalence

Question 26

What causes differences in bioequivalence between the same product from different drug companies?

Answer 26

Different:
Manufacturing processes
Excipients used
Quality Control measures of company

Question 27

What is the formulation goal?

Answer 27

Make most optimal dosage form for specific purpose

Question 28

What administration route achieves the fastest onset?

Answer 28

Parenteral

Question 29

What is the most commonly used and most accepted dosage formulation?

Answer 29

Oral

Question 30

Formulation with the longest effect, easiest application but slower onset?

Answer 30

Transdermal

Question 31

What are the benefits of modifying the drug release rate through excipients?

Answer 31

• sustaining absorption in GI
• prolonging systemic effects of drug
• decreasing administration frequency
• decreasing potential adverse effects

Question 32

Four factors to consider in drug development.

Answer 32

Physiochemical properties
Biological characteristics
Route of administration
Excipients properties

Question 33

What are some common excipients?

Answer 33

Suspending agents (stability, dose accuracy)
Binders (disintegration, dissolution, bioavailability)
Emulsifiers (particle size, O/W or W/O, stability)
Lubricants (dissolution, bioavailability)

Question 34

True or False: Excipients only have positive effects on formulation, such as enhancing appearance, concealing unfavourable taste/smell,and increasing bioavailability.

Answer 34

False. They can also have negative effects on the formulation.

Question 35

What does MEC and MTC stand for?

Answer 35

MEC- minimal effective concentration
MTC- minimal toxic concentration
Blood concentrations should be in between these two.

Question 36

What needs to be considered for optimal drug therapy?

Answer 36

Drug interactions
Subject situation
Drug tolerance
Patient compliance

Question 37

Where is the future going in drug formulation?

Answer 37

More personalized medications and bioavailability improvements