Core Concepts (5)

Question 1

Amorphous and Metastable are (more or less) soluble than their stable counterparts.

Answer 1

More

Question 2

Hydrophilic substituents such as hydroxyl group, are (more or less) water soluble

Answer 2

more

Question 3

____ of the molecule can be more important than the substituents. Corticosteriod Ring has hydrophilic substituents, but the solubility is still low.

Answer 3

Bulk

Question 4

The size of lipophilic molecules matter regarding water solubility, if the molecule is large and has water-soluble substituents than the molecule is (more or less) water soluble.

Answer 4

less

Question 5

(Ionized or nonionized) form of drug is generally most water-soluble.

Answer 5

Ionized

Question 6

Henderson-Hasselbalch equation: The degree of ionization is a function of medium pH and can be measured by the dissociation constant =____

Answer 6

pKa

Question 7

Weak base the drug will be ionized at 3 pH (below or above) its pKa

Answer 7

below

Question 8

Two approaches to altering the solute for solubility proposes are creating ____

Answer 8

salts and prodrugs

Question 9

_____ is a very common method of altering a drug’s properties. (can increase or decrease water solubility)

Answer 9

Salt formation

Question 10

Salt formation can (increase or decrease) water-solubility if there is a greater degree of ionic dissociation of salt molecules. (Drug is charged)

Answer 10

increase

Question 11

Salt formation can (increase or decrease) water-solubility if the solid drug is more chemically stable than drug in solution.

Answer 11

Decrease

more stable- less likely to dissociate

Question 12

Prodrugs (increase or decrease) solubility by increasing lipophilicity. To increase solubility prodrug must have phosphate group.

Answer 12

decrease

Question 13

Two approaches in altering solvent for solubility purposes are…

Answer 13

pH and Polarity

Question 14

Functional groups susceptible to hydrolysis are..

Answer 14

esters, amides, lactam (cyclic amide), and lactones (cyclic ester)

Question 15

Functional groups susceptible to oxidation are…

Answer 15

phenols, catechols, thiols, tertiary amines, polyunsaturated hydrocarbons

Question 16

Most common photolytic mechanism is _____- light help create initiating radicals. Photolysis is the chemical breakdown of light and different molecules have susceptibilities to different types of light (UV, fluorescent etc.)

Answer 16

photooxidation

Question 17

Increased ______ (tendency of substance to take up atmospheric moisture) can lead to deliquescence and uptake of water by a solid drug can accelerate the drug’s chemical degradation.

Answer 17

hygroscopicity

Question 18

pH of maximum stability is the point where K is the (highest or lowest).

Answer 18

Lowest

Question 19

A 10 degree Celsius rise in temperature produce a ____ fold decay rate increase.

Answer 19

2-5

Question 20

____ equation determine the effect of temperature on degradation rates and useful for accelerated stability studies.

Answer 20

Arrhenius Equation -

Question 21

Factors that can delay emptying include ____ meals and drugs with ____activity

Answer 21

high fat, anticholinergic

Question 22

____ are emptied faster than digested and undigested solids.

Answer 22

Liquids and Small particles

Question 23

Food can delay emptying of (large or small) particles

Answer 23

large

Question 24

____ +____ generally not significantly delayed by food

Answer 24

Fine particles + disintegrated tablets

Question 25

For optimal absorption, the drug must have adequate residence time in the ____

Answer 25

duodenum

Question 26

Increased motility can decrease residence time and (increase or decrease) drug absorption.

Answer 26

decrease

Question 27

Efficient drug absorption requires removal by capillaries and lymphatics perfusing GI tract. GI tract receives more than 25% cardiac output and this is increased with meals. So (more or less) blood flow in GI increases the removal of food and drug

Answer 27

more

Question 28

Bioavailability of drug is better in fasted state (alone) with ___ oz of water to help wash drug through esophagus and contribute as medium for dissolution.

Answer 28

8

Question 29

Disease can cause GI anatomical or physiological changes can affect drug absorption. And ____ can be inter-individual difference in uptake transporters, efflux pumps, and drug metabolism.

Answer 29

genetic variation

Question 30

Drugs with _____ properties can reduce gastric acid secretion, gastric emptying, and GI motility.

Answer 30

anticholinergic

Question 31

____ drugs those with calcium, magnesium, or aluminum can reduce drug bioavailability and increase gastric pH to affect drug dissolution (decrease dissolution in weak base)

Answer 31

Antacids

Question 32

____ major site for passive drug absorption due to presence of folds, villi (inc. surface area) and high perfusion.

Answer 32

Duodenum

Question 33

Low pH can enable (slow or rapid) dissolution of weak base drugs

Answer 33

rapid favors ionization

Question 34

eating (increases or decreases) the pH

Answer 34

increase (more basic)

Question 35

Food, liquid, and medications are emptied into the small intestines by the opening of the _____

Answer 35

pyloric sphincter