Preformulation 1

Question 1

What is preformulation?

Answer 1

it is the first step in the rational development of dosage forms of a drug into a medicine. it involves characterising the physical and chemical properties of the active pharmaceutical ingredients

Question 2

what is the aim of preformulation exercise?

Answer 2

To generate mathematical and statistical data for use in developing an efficient, effective and stable dosage form. and to produce a model for drug behaviour.
can also reduce development time and costs.

Question 3

what are poorly soluble drugs in aqueous solutions generally referred as?

Answer 3

Brick DUST

Question 4

what is the optimal solubility for solid medicines?

Answer 4

greater than 10mg/ml. if the solubility of the drug is less than 1mg/ml then the salt form of the drug if possible is indicated

Question 5

what are pharmaceutical salts?

Answer 5

if a drug has poor solubility and is weak base/acid then it’s converted to a salt form

Question 6

Factors affecting dissolution rate

Answer 6

Diffusion coefficient
surface area of the drug
Thickness of boundary layer
solubility and conc in bulk solvent

Question 7

Common strategies to address low drug solubility

Answer 7

SALTS
POLY MORPHS
Co solvents
surfactants

Question 8

ADVANTAGES of pharmaceutical salts??????

Answer 8

Enhance solubility 
Increased dissolution rate 
better taste 
Higher bio availability 
Higher melting point

Question 9

DISADVANTAGES OF pharmaceutical salts

Answer 9

decrease percentage of drug 
increased hygoscopcity 
increased toxicity 
decreased chemical stability 
increased number of polymorphs