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DDS > Core Concepts (5) > Flashcards

Core Concepts (5) Flashcards

1
Q

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

A

More

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2
Q

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

A

more

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3
Q

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

A

Bulk

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4
Q

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.

A

less

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5
Q

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

A

Ionized

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6
Q

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

A

pKa

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7
Q

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

A

below

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8
Q

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

A

salts and prodrugs

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9
Q

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

A

Salt formation

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10
Q

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

A

increase

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11
Q

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

A

Decrease

more stable- less likely to dissociate

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12
Q

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

A

decrease

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13
Q

Two approaches in altering solvent for solubility purposes are…

A

pH and Polarity

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14
Q

Functional groups susceptible to hydrolysis are..

A

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

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15
Q

Functional groups susceptible to oxidation are…

A

phenols, catechols, thiols, tertiary amines, polyunsaturated hydrocarbons

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16
Q

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.)

A

photooxidation

17
Q

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.

A

hygroscopicity

18
Q

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

A

Lowest

19
Q

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

A

2-5

20
Q

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

A

Arrhenius Equation -

21
Q

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

A

high fat, anticholinergic

22
Q

____ are emptied faster than digested and undigested solids.

A

Liquids and Small particles

23
Q

Food can delay emptying of (large or small) particles

A

large

24
Q

____ +____ generally not significantly delayed by food

A

Fine particles + disintegrated tablets

25
Q

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

A

duodenum

26
Q

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

A

decrease

27
Q

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

A

more

28
Q

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.

A

8

29
Q

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.

A

genetic variation

30
Q

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

A

anticholinergic

31
Q

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

A

Antacids

32
Q

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

A

Duodenum

33
Q

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

A

rapid

favors ionization

34
Q

eating (increases or decreases) the pH

A

increase (more basic)

35
Q

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

A

pyloric sphincter

DDS (29 decks)

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