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Pharmaceutics II FINAL > Chapter 9 - Solid Oral Modified Release Dosage Forms and Drug Delivery Systems > Flashcards

Chapter 9 - Solid Oral Modified Release Dosage Forms and Drug Delivery Systems Flashcards

1
Q

true or false

all drugs are suitable for controlled release

A

false

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2
Q

how many modified release dosage forms are there?
name them

A

7

SR - sustained release
SA - sustained action
PA - prolonged action
CR - controlled release
ER - extended release
TR - timed release
LA - long acting

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3
Q

SR

A

sustained release

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4
Q

PA

A

prolonged acting

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5
Q

CR

A

controllled release

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6
Q

LA

A

long acting

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7
Q

TR

A

timed release

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8
Q

SA

A

sustained action

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9
Q

true or false

a disadvantage of modified release dosage forms is that they are more likely to cause more adverse side effects

A

false - there is actually a reduction in adverse side effects bc of fewer blood level peaks that are outside therapeutic range (and into toxic range)

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10
Q

true or false

adverse side effects are less frequent in modified release dosage forms

A

true

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11
Q

true or false

in modified release dosage forms, there is LESS fluctuation in blood drug levels

A

true

controlling the release rate eliminates the peaks and valleys in drug blood levels

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12
Q

true or false

an advantage of modified release dosage forms is that there is a reduction on overall healthcare costs

A

true

initial cost is greater, but there is enhanced therapeutic benefit and fewer side effects. also, healthcare personnel don’t have to dispense and administer the drugs as often and monitor the patients as often – saving money

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13
Q

true or false

modified release dosage forms require more frequent administration

A

false - less frequent

extended release products frequently deliver more than a single dose - thus taken less than conventional dosage forms

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14
Q

explain how modified release dosage forms leads to enhanced compliance and convenience

A

enhanced patient compliance because there is less frequent dosing

enhanced conveniene with day and night administration – not midday

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15
Q

what is the difference between SR and SA

A

sustained release - related to how much drug comes out

sustained action - related to the therapeutic effect

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16
Q

enteric coating is an example of what kind of modified release

A

timed release - want to release in small intestine and not stomach or delayed release

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17
Q

define modified release

A

the drug-release is based on the time, course, and/or location designed to accomplish therapeutic objectives or convenience objectives that are not offered by conventional or immediate release forms

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18
Q

define extended release

A

allows a reduction in dosing frequency

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19
Q

define delayed release

A

designed to release the drug at a time other than promptly after administration

ie - based on environmental factors like the low gastric pH

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20
Q

what are repeat action dosage forms?

A

contain 2 single doses of medication - one for immediate release and the 2nd for delayed release

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21
Q

true or false

enteric coating is an example of providing extended release

A

false - delayed release

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22
Q

what is targeted release

A

drug gets released at receptor site and not in circulation

ie: chemo drugs we dont want to get released in circulation so they are loaded in a nano particle and released at the receptor compartment

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23
Q

in modified release dosage forms, what has solvent action on the coated drug particles and thus controls the amount of drug released out?

A

the biologic fluids

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24
Q

the release rate of osmotic systems is controlled by what?

A

the diffusion of biologic fluids through a polymer

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25
Q

the release rate of erodible systems is controlled by…

A

the erosion of a polymeric matrix

ie: if polymer doesnt erode, the drug won’t come out

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26
Q

the release rate of diffusion systems is controlled by what?

A

the diffusion of the drug through a polymeric membrane or a monolithic matrix

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27
Q

true or false

in modified release dosage forms, chemical interactions can control the release of certain drugs

A

true

ie: interaction between the drug and site-specific biologic fluids (pH)

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28
Q

for oral rate-controlled products, a good drug candidate must have what kind of absorption and excretion and why?

A

neither very slow nor very fast absorption and secretion

not very slow because this drug would already be long acting and exhibit sustained release, so there’s no point

cannot be very fast because we would need an extremely high dose to provide a rate-controlled product and this tablet would be way too big to swallow

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29
Q

true or false

a good candidate for extended release products must be uniformly absorbed from the GI tract

A

true

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30
Q

a good drug candidate for extended release dosage form should be administered in relatively ____ doses

A

small doses

if it was large doses, tablet would be too big to swallow

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31
Q

why must drugs that are being considered to be made into extended release have a good margin of safety

A

technology limits and patient misuse

technology for extended release cannot realistically be so precise. thus, using a drug with a narrow therapeutic index would be dangerous

if pt chews on accident - immediately toxic

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32
Q

drugs that are good candidates for extended release products must treat what kind of conditions and why?

A

chronic conditions

acute conditions require more dosing adjustment by the physician and ER products can’t provide this

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33
Q

drugs with _ half lives are not good candidates for extended release dosage form

A

short

large quantity of drug would be required for formulation - too big to swallow

34
Q

to be a good candidate for extended release dosage form, do we want it to exhibit active or passive absorption and why?

A

PASSIVE bc it will cover the entire GI tract

active only takes place in the duodenum

35
Q

what should be the dose size for a drug to be a good candidate for extended release dosage form

A

0.5-1g

total daily dose can’t be higher than 1 g

36
Q

to be a good candidate for extended release, what should the solubility of the drug NOT be

A

no less than 0.01mg/mL

the variation of the drug will be huge - sometimes release fast and sometimes slow

37
Q

name 3 factors that affect GI transit time

A

floating systems
bioadhesives
penetration enhancers

38
Q

what is a multitablet system?

A

small spheroid compressed tablets 3-4mm in diameter prepared to have varying drug release characteristics.

8-10 of these spheroid minitablets contained in a capsule with a gelatin shell. some of these minitablets are uncoated for immediate release and others are coated for extended release

39
Q

the multitablet system is an extended release technology for the oral dosage form.
it consists of ___ inside ____

A

8-10 minitablets inside a capsule

40
Q

what is the commercial name for repeat action tablets?
explain what they are

A

repetabs

initial drug dose is released from the tablet SHELL and then a second dose is released from the inner core of the tablet at a later time

type of extended release oral technology

41
Q

what are “coated beads, granules, and microspheres”?

A

a type of extended release technology for the oral dosage form.

consists of either beads or granules. some are uncoated (immediate release and water soluble)

and some are coated with a LIPID MATERIAL (beeswax) and CELLULOSIC MATERIAL (ethylcellulose) in different thicknesses - comprises the SUSTAINED RELEASE DOSE

these coated beads or granules are either placed in to capsules or compressed into tablets

42
Q

in coated beads/granules/microspheres extended release systems, the sustained release beads/granules consist of what material?

A

a lipid material like beeswax and cellulosic material like ethylcellulose in different thicknesses

43
Q

give 4 examples of coated beads/granules/microspheres in the market

what is similar with all of them?

A

Toprol-XL (metoprolol succinate) tablets

Indocin SR (Indomethacin) capsules

Compazine (prochlorperazine) Spansule capsules

Adderall XR (amphetamine) capsules

they all contain 2 kinds of beads/granules: sustained release and immediate release

44
Q

true or false

in the system with coated beads/granules/microspheres, the immediate release dose is coated with a hydrophilic material

A

FALSE - IT IS UNCOATED, but it is hydrophilic. that’s how it’s able to give immediate release

45
Q

what is a micro-encapsulated drug?

A

an extended release technology for oral dosage form

solids, liquids, or gasses can be encapsulated into microscopic particles by the formation of thin coatings of wall material around the substance

(similar to an emulsion)

46
Q

give 4 examples of the wall materials that can be used to coat the solid/liquid/gasses to form a microencapsulated drug for oral extended release

A

gelatin
PVA (polyvinyl alcohol)
ethylcellulose
polyvinyl chloride

47
Q

give 3 examples of commercial products that give an extended release profile by using microencapsulation technology

A

Micro-K
K-dur
effexor XR (venlafaxine)

48
Q

a form of technology for oral extended release is to embed the drug in…..

A

a slowly eroding or hydrophilic matrix system

49
Q

in the technology of embedding the drug into a slow eroding or hydrophilic matrix system, explain how it works to given extended release

A

the IR dose is untreated and the sustained release dose is combined with a lipid or cellulosic material and processed into granules.

both of these portion are either placed into capsules, or compressed into 2 or 3 layered tablets

50
Q

give 4 examples of extended release products on the market that use the technology of embedding the drug in a slowly eroding or hydrophilic matrix system

A

Slow-K
Depakote ER (divalproex sodium)
Quinidex (Quinidine Sulfate)
Oramorph SR (morphine sulfate)

51
Q

True or false

a hydrophilic matrix system is unable to provide extended release

A

false - it can

52
Q

in the extended release technology method of embedding the drug in a slowly eroding or hydrophilic matrix system, what type of erosions can occur and which is preferred?

A

surface erosion and bulk erosion

surface erosion - entire system gets smaller and smaller

bulk erosion - system breaks into smaller systems

surface erosion is preferred

53
Q

technology: embedding drug in inert plastic matrix to provide extended release

explain how it works

A

the drug is combined with an inert polymer (PVA, polyethylene, and polymethacrylate) and processed into GRANULES

these granules are compressed into tablets.

The drug releases by a DIFFUSION MECHANISM through the polymer matrix

this is like solid dissolved in solid

54
Q

technology: embedding drug into inert plastic material to provide extended release

give 3 examples of what this inert plastic material can be

A

PVA - polyvinyl acetate
polyethylene
polymethylacrylate

55
Q

give 2 examples of extended release products that use the technology of embedding the drug in an inert plastic matrix

A

Gradumet
Procanabid

56
Q

true or false

the extended release technology of embedding the drug in an inert plastic matrix is different from the other technologies in that the mechanism is via diffusion across the hydrophobic polymer matrix

A

true

the matrix is hydrophobic so it will not undergo dissolution (dissolve) in the body fluids

57
Q

in the extended release technology of embedding the drug in an inert plastic matrix, what can you say about the solubility of the drug in the polymer?

A

should be water soluble enough to be able to diffuse into body fluids, but also be soluble enough in the polymer that enough drug can be loaded into it

58
Q

explain the “complex formation” extended release oral technology

A

the drug is chemically combined with another agent like CYCLODEXTRIN to form a chemical complex

the hydrophobic drug (or hydrophobic portion of it) is maintained in the hydrophobic core of cyclodextrin.

the drug gets released into body fluids due to pH. ionization will take place in the core – which causes the hydrophobic properties of the core to decrease

the drug is released bc it doesn’t wanna stay in the ionized core – HAPPENS SLOWLY (extended release)

THE DRUG MUST COME OUT OF THE COMPLEX TO HAVE THERAPEUTIC EFFECT

59
Q

give 4 examples of drugs that use complex formation technology in order to have extended release

are these drugs totally maintained in the hydrophobic core?

A

only the hydrophobic portion of these drugs is in the core and the hydrophilic portion is outside of it

ampicillin
progesterone
estradiol
prostaglandin F

60
Q

what are ion exchange resins?

A

an oral extended release technology

61
Q

explain how ion exchange resins work to provide extended release

A

a cationic or anionic drug (doesnt matter just has to be ionized) is combined with an ion exchange resin to form a resin-drug complex. this complex is encapsulated or tableted.

the electrolyte concentration and pH in the GI tract causes drug release into body fluids

62
Q

in ion exchange resins, generally, drug release is greater…….

A

greater in the stomach than in the intestine

63
Q

give 2 examples of products that use ion exchange resins in order to give extended release

A

Tussionex and Ionamin

64
Q

if the drug is cationic, what will the resin be made of?

if the drug is anionic, what will the resin be made of?

A

cationic - SO3-

anionic - N(CH3)3+

65
Q

what are the drug-resin complex particle treated with?

A

polyethylene glycol

66
Q

what is the coating around the entire ion exchange resin?

A

ethylcellulose coating

67
Q

if the drug is cationic, explain its release via ion exchange resin

A

extended release

the drug will be released by the effect of pH and electrolyte concentration in GI fluids. Drug will be released and hydrogen ions will go in

ion exchanged for ion

68
Q

if a drug is anionic, explain its release via an ion exchange resin

A

extended release

drug will be released from the resin due to electrolyte conc and pH in GI tract.

anionic drug will be released and exchanged for chloride

69
Q

what does OROS stand for

A

osmotic controlled release oral delivery system

70
Q

what is the OROS system composed of?

A

a core tablet with a semipermeable coating.

there is a 0.4mm diameter hole for the drug to exit the tablet

71
Q

in an osmotic pump, what is the drug release dependent on?
what is it independent on?

A

dependent on osmotic pressure

INDEPEDENT of the pH of biologic fluids

72
Q

true or false

an osmotic pump is technology that is able to provide oral extended release

A

truw

73
Q

in an osmotic pump, what is drug release CONTROLLED BY

A

the surface area
nature of the membrane
the diameter of the drug release orifice

74
Q

true or false

zero order release is not attainable for an osmotic pump

A

FALSE - it is

75
Q

name 3 advantages of osmotic pumps

A

the release is INDEPENDENT of the environment

for different drugs, reformulation is NOT required

can provide zero order drug release

76
Q

name 2 disadvantages of an osmotic pump

A

these systems can be very expensive

quality control is more extensive

77
Q

what is the diameter for the orifice where the drug is released in an osmotic pump

A

0.4mm

78
Q

give 4 examples of products that use an osmotic pump to provide oral extended release

A

acutrim
Procardia XL
Glucotrol XL (glipizide)
Covera HS (verapamil)

79
Q

osmotic pumps have similar technology to…..

A

transdermal delivery systems
somehwat replaced them

80
Q
A

Pharmaceutics II FINAL (11 decks)

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