4 - Preformulation

Question 1

Preformulation

Answer 1

gathering info regarding drug properties which may have a bearing on product formulation

Question 2

What are organoleptic properties?

Answer 2

Description of drug substance including:
color
odor
taste

Question 3

Organoleptic properties:

How do you fix objectionable colours?

Answer 3

• colouring agent may be included

- tablets may be coated

Question 4

Organoleptic properties:

How do you fix objectionable odors?

Answer 4

• contain the odor in a coating

- inclusion of an aromatic excipient

Question 5

Organoleptic properties:

How do you fix objectionable taste?

Answer 5

• masked by flavoring agent, coating

- use of an insoluble salt form

Question 6

5 tastes recognized

Answer 6

bitter
sour
sweet
salty
umami (protein taste)

Question 7

Bitter taste is associated with ____ groups

Answer 7

amine

Question 8

Sour taste associated with ____

Answer 8

acids

Question 9

Sweet taste associated with ____ groups

Answer 9

hydroxyl

Question 10

Salty taste associated with _____ ____

Answer 10

inorganic salts

Question 11

Umami associated with some ____ ___

Answer 11

amino acids

Question 12

What are micromeretics?

Answer 12

particle size
shape
surface area

Question 13

_____ crosses membranes better

Answer 13

unionized

Question 14

_____ dissolves better

Answer 14

ionized

Question 15

What is the formula for partition coefficient?

Answer 15

P = [organic]/[aqueous]

often expressed as log P

Question 16

larger P value means?

Answer 16

it has more affinity for the organic phase

Question 17

smaller P value means?

Answer 17

it has more affinity for the aqueous phase

Question 18

What is a Franz cell used for?

Answer 18

measure passive diffusion through membrane

sample how much drug has crossed the membrane

Question 19

Generally _____ form is more soluble

Answer 19

amorphous

more soluble that identifiable definite shape

Question 20

When is a polymorph transformation reported?

Answer 20

after milling, granulation, drying and compression

Question 21

Granulation can also cause the formation of?

Answer 21

solvates or hydrates

Question 22

Drying may cause transformation to ??

Answer 22

anhydrous crystalline or amorphous forms

Question 23

Properties that influence stability

Answer 23

pKa
solubility
melting point
crystal habit and form
equilibrium moisture content

Question 24

Most common factors for instability are ?

Answer 24

light
heat
oxygen
moisture

Question 25

Data is analyzed using ___

Answer 25

MLR

multiple linear regression

Question 26

In the presence of moisture many drugs ?

Answer 26

hydrolyze
react with excipients
oxidize

Question 27

How do you measure how moisture affects certain drugs?

Answer 27

• keep constant temperature

- measure different samples and different humidity levels

Question 28

Other factors important to the formulator are?

Answer 28

density
hygroscopicity
flow properties
compressibility

Question 29

Density

Answer 29

• provide a rough idea of the size of the finished product

- density affects flow properties

Question 30

Hygroscopicity

Answer 30

• moisture content

- can affect flow and compression properties

Question 31

Flow properties

Answer 31

• good flow properties essential for blending, granulation and compression
• angle of repose measures flow (prefer angle between 25 and 45 degrees)