Knipp 1

Question 1

drug performance 1

Answer 1

ability of drug to elicit therapeutic response
pharmacokinetics: how body responds to drugs
pharmacodynamics: therapuetic response

Question 2

global formulation

Answer 2

to transfer therapeutic compound, it requires a reproducible dosage form.
same drug each each batch

Question 3

ADME

Answer 3

absorption, distribution, metabolism, excretion

Question 4

drugability

Answer 4

discovery stage, ability of NCEs to bind to drug target, in vivo models are assessed
druggable protein: proteins that can bind drug like compounds with high affinity and candidates that perform best advance

Question 5

developability

Answer 5

drug product performance, evaluating properties that allow proper therapeutic response. pharamcokinetics and pharmacodynamics determine safe and efficacious use

Question 6

**drug formulation design

Answer 6

physicochemical properties of the drug, physicochemical properties and composition of the formulation, biological factors that influence performance (ADME and toxicity)

Question 7

drug performance

Answer 7

ability of drug to elicit therapeutic response, safe therapeutic range, lack of toxic/non efficacious response, described by pharmacokinetics and pharmacodynamics, function of drug and formulation

Question 8

physicochemical properties that affect absorption

Answer 8

solubility, stability in solution, molecular size & shape, pka, lipophilicity, physical state (amorphous or crystalline)

Question 9

solubility

Answer 9

depends on molecular structure, physical state, composition of solvents, measurement methods

Question 10

partitioning coefficient

Answer 10

ratio of concentrations of two immiscible solvents

Question 11

pH partition hypothesis

Answer 11

for drugs absorbed by passive transcellular mechansim, permeability transport depends on the fraction of unionized drug at intestinal pH

Question 12

extra+intracellular pH effects drug transport

Answer 12

organelle pH can result in the trapping of a molecule in a cell

Question 13

**overcoming effects of pH partition hypothesis

Answer 13

functionalize compound-change pka,
prodrug strategy (modify moeity and molecule to be recognize by transporter),
salt selection (ion pairing effective, salt form can alter unionized fraction)
drug delivery system

Question 14

formulation factors affecting absorption

Answer 14

dosage form design
rates of drug release from the dosage form
residence time at absorption site

Question 15

excipients

Answer 15

not inert, but pharmacologically inert, inactive therapeutic

Question 16

common excipients

Answer 16

cellulose, sugars, starch, synthetic, inorganic, magnesium

Question 17

factors for excipient selection

Answer 17

origin, quality and purity, stability, cost, toxicological considerations

Question 18

**ingredients affecting bioavailability, stability, marketing considerations

Answer 18

disintegrates enhance rate of disintegration/dissolution
coatings-control release
flavors/sweeteners mask drug taste
colors-recognition
miscellaneous ingredients

Question 19

common methods for excipient compatibility testing

Answer 19

mechanical stress
tablets processed by wet granulation
using amorphous drug
suspension or solution of excipients

Question 20

**organoleptic senses to consider when coating/blinding clinical trials

Answer 20

sight, smell, sound, taste, touch

Question 21

solid dosage form requirements

Answer 21

must have content uniformity (each tablet has approx 85%-115% API, or tighter control)
have good organoleptic properties
need to be stable for 2 year shelf life
reproducible release metrics as measured by dissolution for batch release
must not be friable (does not break)