Topic 1: Stability and Incompatibilities

Question 1

Problem which could occur as a result of interaction between two or more drugs or chemicals

Answer 1

Incompatibilities

Question 2

Physical or chemical interaction that leads to visible recognizable change

Answer 2

Physical Incompatibilities

Question 3

Physical Incompatibilities includes

Answer 3

Incomplete Solution
Precipitation from solution
Polymorphism
Liquefaction of Solid Ingredients
Sorption and leaching
Evaporation
Loss of water

Question 4

Insolubility of components
Immiscibility of components

Answer 4

Incomplete Solution

Question 5

In Precipitation from Solution, for ____, will cause therapeutic failure or toxicity

Answer 5

For oral or topical solution

Question 6

In Precipitation from Solution, for ____, insoluble particles can lodge in capillaries and block them causing severe consequences or even death

Answer 6

For IV solutions

Question 7

Alteration in the degree of ionization

Answer 7

pH effects

Question 8

is freely soluble in water

Answer 8

Phenobarbital Na

Question 9

is slightly soluble to water

Answer 9

Phenobarbital

Question 10

Control pH at desired level

Answer 10

Handling solutions of weak electrolytes

Question 11

In Handling solutions of weak electrolytes, for oral or topical solutions, use a ___ that will keep the free drug in a solution or prepare a suspension

Answer 11

cosolvent

Question 12

In incomplete solution, For oral or topical product, make ____

Answer 12

suspension or emulsion

Question 13

In Handling solutions of weak electrolytes, for ____, Check the product insert and consult references

Answer 13

parenteral products

Question 14

In Handling solutions of weak electrolytes, for ____, be aware of the possible problems if product will be used or administered at a different temperatures

Answer 14

For oral or topical solution

Question 15

a competitive process wherein the molecule of a substance compete for the water in solution forming precipitate

Answer 15

Salting out

Question 16

Remedy in handling solutions sensitive to change in temperature

Answer 16

Use another solvent

Question 17

Change in crystalline form

Answer 17

Polymorphism

Question 18

Different polymorphs will exhibit different physical properties, such as

Answer 18

melting point and dissolution rates = affects bioavailability

Question 19

example of polymorphism

Answer 19

cocoa butter

Question 20

cocoa butter melting point

Answer 20

not greater than 34ᵒC

Question 21

Liquefaction of Solid Ingredients examples

Answer 21

Efflorescent powders
Hygroscopic and deliquescent drugs

Question 22

Efflorescent powders examples

Answer 22

morphine acetate
ferrous sulfate
codeine
caffeine atropine sulfate

Question 23

Hygroscopic and deliquescent drugs examples

Answer 23

Ephedrine sulfate
potassium citrate
Phenobarbital Na
Sodium iodide

Question 24

molecules are concentrating at the interface

Answer 24

Adsorption

Question 25

The molecules being absorbed are penetrating into the capillary spaces of the absorbing surface

Answer 25

Absorption

Question 26

sorption commonly occurs in __ due to plasticizer

Answer 26

polyvinyl chloride (PVC) containers

Question 27

Drugs that are poor water-soluble or lipophilic that have greater tendency to sorb to PVC to dissolve in its plasticizer

Answer 27

Lorazepam diazepam nitroglycerin nicardipine ISDN

Question 28

container substitutes to prevent leaching

Answer 28

glass polyvinyl polyethylene polyurethane

Question 29

vaporization aka

Answer 29

volatilization

Question 30

liberation of the active ingredients

Answer 30

vaporization

Question 31

Common in liquid dosage forms

Answer 31

Loss of Water

Question 32

phase inversions in O/W emulsions

Answer 32

Emulsions

Question 33

↑ potency

Answer 33

Suspensions and solutions

Question 35

Occurs as a result of chemical interaction among the ingredients of a given prescription.

Answer 35

Chemical Incompatibility

Question 36

Visible change in the reaction is not necessarily observed but can be determined by

Answer 36

analytical method

Question 37

Chemical Incompatibility includes

Answer 37

Oxidation Reduction Hydrolysis Evolution of Gas Complexation Racemization Epimerization

Question 38

Occurs when one drug losses electron to the other

Answer 38

Oxidation

Question 39

Triggered by light, heavy metals, oxygen, oxidizing agents

Answer 39

Oxidation

Question 40

Drugs susceptible to oxidation includes:

Answer 40

Catecholamine e.g. epinephrine Phenolics e.g phenylephrine, morphine Phenothiazines, chlorpromazine Thiols e.g captopril Others: Amphotericin B, tetracycline, furosemide, etc.

Question 41

Most common type of incompatibility and drug degradation

Answer 41

Hydrolysis

Question 42

Triggered by presence of water, acids, bases, catalyst e.g. dextrose

Answer 42

Hydrolysis

Question 43

example of hydrolysis

Answer 43

dextrose

Question 44

Drugs susceptible to hydrolysis

Answer 44

Amides especially with lactam rings – penicillins and cephalosporins Esters – procaine, tetracaine, aspirin, belladonna

Question 45

In hydrolysis, for ___, control exposure to moisture by using light containers and desiccants

Answer 45

for solids

Question 46

Commonly caused by NaHCO3 and carbonate buffers = effervescence

Answer 46

Evolution of Gas

Question 47

example of Evolution of Gas

Answer 47

Alka seltzer

Question 47

Desired use in some powders and tablets

Answer 47

Evolution of Gas

Question 48

Forming inactive complex

Answer 48

Complexation

Question 49

example of Complexation

Answer 49

tetracycline with multivalent ions

Question 50

The conversion of one enantiomer to a racemate

Answer 50

Racemization

Question 51

the I-enantiomer is approximately 15-20x more active than d-enantiomer

Answer 51

Epinephrine

Question 52

Other drugs involve in racemization

Answer 52

esomeprazole bupivacaine omeprazole levalbuterol albuterol

Question 53

Formation the pair of diasteriomers that differ only in the configuration about one carbon atom

Answer 53

Epimerization

Question 54

one carbon atom

Answer 54

epimers

Question 55

undergoes reversible epimerization to epitetracycline (of little antibacterial activity) in a solution

Answer 55

Tetracycline

Question 56

example of epimerization

Answer 56

tetracycline

Question 57

A problem that occurs when two or more drugs are administered to a patient

Answer 57

Therapeutic Incompatibilities

Question 58

Therapeutic Incompatibilities aka

Answer 58

drug interaction

Question 59

one drug alters the effect of another drug

Answer 59

drug interaction

Question 60

therapeutic incompatibilities

Answer 60

Pharmacokinetic Pharmacodynamic

Question 61

Undesirable pharmacological interactions between two or more ingredients that lead to:

Answer 61

Additive or potentiated therapeutic effects Antagonistic or destruction of the effect

Question 62

may cause toxicity or death

Answer 62

Additive or potentiated therapeutic effects

Question 63

sub-therapeutic or lack of effect

Answer 63

Antagonistic or destruction of the effect