Exam 1: Kwon

Question 1

Elements of drug delivery

Answer 1

Drug, excipients, packaging

Question 2

Preformulation drug personalities

Answer 2

Solubility, partition coefficient, dissolution rate, physical form, stability

Question 3

Excipient characteristics

Answer 3

Promote manufacturability, stability, bioavailability, accurate dosing, patient patience and convenience

Mostly inert

Question 4

Main phases of drug action

Answer 4

Dose –> Bioavailability –> Drug Available for Action –> Effect

Question 5

What is bioavailability?

Answer 5

Rate and extent of active drug absorbed and available at site of action to yield a therapeutic response

Question 6

Fick’s First Law

Answer 6

Rate of diffusion

Question 7

Physicochemical properties influencing drug absorption

Answer 7

Lipid solubility (K)
pKa (Henderson-Hasslbach)
Molecular weight and volume (Stokes-Einstein)
Aqueous solubility
Chemical stability

Question 8

Lipinski’s Rule of 5

Answer 8

Oral drug must have:
Molecular weight > 500g/mol 
Log K > 5
Hydrogen bond donors > 5
Hydrogen bond acceptors > 10

Question 9

Drug absorption pathways

Answer 9

Transcellular (most common)
Paracellular (less common)
Efflux pump (PGP)

Question 10

Epithelia at sites of drug delivery

Answer 10

Oral: Simple columnar
Nasal: Pseudostratified ciliated columnar
Skin: Stratified squamous

Question 11

Epithelial types

Answer 11

Simple squamous
Simple cuboidal
Simple columnar
Ciliated columnar
Pseudostratified ciliated columnar
Stratified squamous
Transitional

Question 12

Common drug problems

Answer 12

Poor solubility, tissue damage, rapid breakdown, unfavorable PK, poor biodistribution