PHAR124 > Tablets > Flashcards

Tablets Flashcards

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1
Q

What is the most frequently used dosage form?

A

tablets

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2
Q

What are the advantages of tablets?

A

economical dosage form
easy to prepare
variety of size and shapes
mostly oral but there are other routes of administration
easy to package, ship, dispense
good stability, especially if coated
accurate doses
portable
relatively tasteless, especially if coated

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3
Q

What are the two methods that tablets are prepared?

A

compressing or molding

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4
Q

What are the most common excipients you will find in a tablet?

A

binder
disintegrant
lubricants and glidants
coatings
diluents
colorants
flavoring agents

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5
Q

What are compressed tablets? How are they prepared?

A

tablets formed by compression with no special coating
prepared with machines capable of exerting great pressure in compacting the powdered or granulated material
powders–>compression–>tablets
the basis for many different types of tablets

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6
Q

What is the problem with compressed tablets?

A

simple powders may have poor flow and compression characteristics
-they require tremendous pressure

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7
Q

What is the solution to the poor flow and compression characteristics of compressed tablets?

A

modification such as formation of granules which impart both cohesiveness and flow properties

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8
Q

Which substances can undergo direct compression?

A

granular chemicals with free-flowing and cohesive properties:
-potassium chloride
-microcrystalline cellulose
-compressible starch

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9
Q

What are some issue that can arise with tablets made from compression?

A

capping
splitting
laminating
due to air entrapment

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10
Q

What is granulation?

A

the process of particle size enlargement of powdered ingredients (agglomeration)
-wet granulation
-dry granulation

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11
Q

Which method of dry granulation is preferred and why?

A

roller compaction is preferred due to improved hardness and friability

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12
Q

When are lubricants added during wet granulation?

A

added at the end to the dry granules

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13
Q

What is the purpose of diluents in tablets?

A

acts as a vehicle for the drug
increases bulk
improves or maintains uniformity
diluents make up as little as 5% to 80% of the tablet

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14
Q

What are the diluents used in tablets that we have to know?

A

lactose
dextrose
microcrystalline starch
starch
mannitol

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15
Q

What is often considered the most important ingredient in tablets?

A

binders

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16
Q

What is the purpose of binders in tablets?

A

impart cohesiveness to powders, providing necessary bonding
varies from 1-20%

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17
Q

What will happen to your tablet if you have too little binder? What about if you have too much binder?

A

too little: fragile tablets (fall apart)
too much: excessive hardness (slow disintegration and dissolution and therefore poor bioavailability)

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18
Q

What are the binders used in tablets that we have to know?

A

starch
gelatin
glucose
polyvinylpyrrolidone

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19
Q

True or false: tablet excipients may often perform more than one function

A

true

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20
Q

Give examples of tablet excipients performing more than one function.

A

dextrose, sucrose, and lactose exhibit binding properties
starch and MCC have binding and disintegrant properties
lactose and sucrose impart hardness
starch, kaolin, and dextrose add softness
mannitol, lactose, and sorbitol exhibit cooling effect

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21
Q

What are the three properties of lubricants in tablets?

A

glidant effect by coating and lubricating particle surfaces
-improves flow properties
provide anti-adhesive effects
-prevents adhesion of materials to punches and dies
act as lubricant between walls of die cavity and tablet
-facilitating tablet ejection

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22
Q

What are the two types of lubricants?

A

water insoluble: magnesium stearate, stearic acid, talcum
water soluble

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23
Q

Which item is usually added last to tablets?

A

lubricants

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24
Q

What is the purpose of disintegrants in tablets?

A

facilitates break-up of tablet after administration
causes tablet to rupture when it contacts GI fluids
facilitates disintegration, dispersion, and dissolution

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25
What is the mechanism of disintegrants?
draws gastric fluids into tablet, causing porosity in the tablet or swelling and finally break up due to hydrostatic pressure
26
What are the disintegrants used in tablets that we have to know?
starch celluloses (MCC) tartaric acid (used for effervescent tablets)
27
What is the function of coloring agents in tablets?
esthetics identification
28
When are sweeteners and flavoring agents required for tablets?
chewable and effervescent tablets not required for standard compressed tablets
29
True or false: a tablet can be made if the excipients are not compatible with the rest of the formulation
false one must ensure that the excipients are compatible with the rest of the formulation
30
What is the basic mechanical unit for tablet compression?
punch and die -lower punch -upper punch -die
31
What is the purpose of tablet coatings?
smooth surface product identification mask drug taste improve drug stability (protect against air or humidity) defined characteristics of drug release -functional coatings: enteric-coating, controlled/sustained release
32
What are the three types of tablet coatings?
film coating sugar coating functional coatings
33
What are the potential problems with sugar coating?
many steps involve tumbling, tablet must be hard enough to withstand it must mix uniformly or coating goes on unevenly resulting in tablets of different sizes and weights
34
What is the most common coating?
film coating
35
What is a film coating?
thin coating of a plastic like material over the compressed tablets the basic component is cellulose derivatives like HPMC
36
What are the processes for film coating?
coating pan spray in a fluidized stream press coating
37
Describe pan coating.
mixing of tablet mass: -pan shape, rotational speed and loading affect the mixing of tablets and coating -uniform mixing is essential to deposit the same quantity of film on each tablet, poor tablet movement causes errors
38
Describe press coating.
compaction of a dry coat around a tablet core, produced on the same tableting machine avoids the use of solvents can be used to separate incompatible drugs in the same tablet, making a layered tablet
39
What are the challenges of aqueous film coating process?
slow evaporation of water orange peel effect covering of score line disfiguration of the core tablet
40
Why is the organic film process not preferred?
expensive and sometimes not environmentally friendly
41
What is enteric coating?
allows for disintegration in the intestine rather than the stomach does not dissolve in the acidic pH of the stomach protects drug from acid hydrolysis
42
What is functional coating?
allows for timed release -can have particles coated with varying thicknesses of coating so drug is released gradually from the dosage unit
43
What are molded tablets?
prepared by molding rather than compression soft, soluble, and designed for rapid dissolution
44
Which excipients will you not find in molded tablets?
disintegrants lubricants coating
45
When are molded tablets not appropriate?
potent drugs -due to difficulties with content uniformity
46
What are the most common diluents found in molded tablets?
mannitol lactose dextrose
47
What are chewable tablets? Who are they intended for?
tablets intended to disintegrate in the mouth primarily intended for children who prefer chewing a flavoured medication rather than swallowing
48
What are the advantages of chewable tablets?
pleasant taste no bitter or unpleasant aftertaste convenience and patient acceptance (esp kids and geriatrics) rapid onset of bioactivity (no disintegration)
49
What are the disadvantages of chewable tablets?
limitations on # of drugs that can be put in drug material is bitter and flavouring is difficult
50
What is a widely used excipient in chewable tablets? Why is it so widely used in chewable tablets?
mannitol -70% sweetness compared to sucrose -cool taste and mouth-feel -non-hygroscopic
51
Which excipient is commonly used in chewable tablets when you want the tablet to be sugar free?
xylitol
52
Why is color added to chewable tabblets?
appeal of the tablet correlate with flavour
53
Which excipient is not required in chewable tablets?
disintegrants
54
What is an important counselling point in regards to chewable tablets?
do not swallow whole, chew to break the tablet
55
Which anticonvulsant is commonly found as a chewable tablet for kids?
carbamazepine
56
What are effervescent tablets?
large wafer-like tablets which dissolve rapidly in water large surface area allows for faster rate of solution
57
What facilitates the breakup of effervescent tablets?
release of CO2 generated from sodium bicarbonate and citric or tartaric acid chemical rxn is initiated when tablet is placed in water; water solubilizes the reagents so reaction can take place
58
What are important considerations to keep in mind with effervescent tablets?
binders, fillers, and lubricants are water soluble moisture excluded during manufacturing package in moisture-proof containers to avoid degradation flavoured & sweetened
59
What are important counselling points for effervescent tablets?
dissolve in water at room temperature once effervescence stops, wait >5 min and stir solution for about 10s and then drink store away from humid conditions
60
What is the difference between sublingual and buccal tablets?
sublingual: placed under tongue buccal: between cheek and gum
61
What are sublingual and buccal tablets designed to produce?
designed to produce immediate systemic effect by enabling drug to be directly absorbed through the oral mucosa
62
Which excipient do sublingual and buccal tablets not have?
disintegrant
63
What is the physical design of sublingual and buccal tablets?
small soft flat may be molded or compressed (lightly)
64
In terms of dissolving, what is the difference between sublingual and buccal tablets?
sublingual: dissolve promptly to provide rapid effects buccal: erode relatively slowly
65
What are ODTs?
solid dosage form which disintegrates rapidly, usually within a matter of seconds, when placed on tongue
66
How are ODTs different from sublingual and buccal tablets?
ODTs dissolve in seconds, may not result in faster therapeutic onset sublingual and buccal require more than a minute to dissolve
67
What are other names used for ODTs?
oro-disperse mouth dissolving quick-dissolve fast-melt freeze-dried wafers
68
What are the advantages of ODTs?
enhance clinical effects through pre-gastric absorption increases bioavailability
69
What must always be added to ODTs?
flavours and sweeteners
70
What are important counselling points with ODTs?
do not administer with wet hands store in dry place may cause burning or tingling on tongue
71
What are the major challenges associated with sublingual, buccal, and ODTs?
drug loading (only good for small doses) taste masking and palatability (shouldnt be gritty) friability (balance between soft and hard) extra cost of packaging (require individual blistering)
72
What are lozenges designed to do?
promote saliva flow, which is soothing may be used for systemic effect if the drug is well absorbed through the buccal lining they contain one or more medications, usually sweetened
73
Who are lozenges good for?
patients who have difficulty swallowing -pediatrics -geriatrics -patients with GI blockage
74
Who are lozenges a potential danger to?
kids they look and taste like candy
75
What are some drugs in lozenge form?
fentanyl nicotine sore throat flurbiprofen zinc
76
How are lozenges prepared?
molding (gelatin, fused sucrose or sorbitol base) OR compression of sugar-based tablets
77
Molded lozenges are sometimes referred to as ____, harder lozenges are sometimes referred to as ___.
pastilles troches
78
What are the basic properties of a good lozenge?
slow uniform dissolution or erosion over 5-10 minute period smooth surface texture pleasant flavour masking drug taste
79
Which excipient will you find in a hard lozenge, soft lozenge, and chewable lozenge?
hard lozenge: sucrose soft lozenge: polyethylene glycol chewable lozenge: gelatin
80
What is the composition of hard lozenges?
solid syrups or sugars -typically 55-65% sucrose and about 35-45% corn syrup -needs a low moisture content (0.5-1.5%)
81
How are hard lozenges made?
heating sugars and other ingredients together and then pouring the mixture into a mold -the molds can shape the mixture to look like a sucker/lollipop
82
How are soft lozenges made?
can be hand rolled and then cut into pieces (because of soft texture) more convenient: pour the warm mass into a plastic troche mold
83
What is the typical composition of soft lozenges?
polyethene glycol 1000 or 1450 chocolate sugar-acacia base
84
What is the benefit of adding acacia or silica gel to soft lozenges?
acacia: adds texture and smoothness silica gel: suspending agent to keep materials from settling to the bottom of the mold
85
If using PEG for a soft lozenge, what should be done during the filling process?
cavitities of the troche mold should be overfilled before the material has solidified, use the spatula to level and even out the mass -chocolate does not shrink as it cools so filling is unecessary
86
Which group of patients are chewable lozenges popular with?
pediatrics
87
What is the composition of chewable lozenges?
most formulations are based on the glycerinated gelatin suppository formular which consists of glycerin, gelatin, and water
88
What is the flavour of chewable lozenges?
fruit flavoured may have a slightly acidic taste to cover the acrid taste of the glycerin
89
What is the rule of thumb for adding flavouring to lozenges?
prepare the lozenges without any drug present and flavor these blank lozenges to taste then when drug is added, start with 5-10 times the amount of flavoring used in the blank lozenges
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