solid dosage forms, compressed with the aid of suitable pharmaceutical ingredients and processing
tablets
most tablets are intended for ______ administration
oral
most tablets are prepared by ________ using ________
compression , rotary tablet presses
what is tablet scoring
helps tablet to be easily split in 2 halves to be taken as divided doses
functional vs nonfunctional modifications
functional modifies release profile and nonfunctional does not
monograms (embossing or debasing) on the tablets are dependent on the etching on the punches. punching can be ________ to prevent ________ in letters containing ______
pre picked, picking, islands
force of pressing determines ______________
hardness
Tablet routes of administration (4)
oral, sublingual, buccal, vaginal
Release profiles (4)
immediate, delayed, sustained, controlled release
Multiple compressed tablets (2)
multiple layers (bi- tri- penta-) or tablet within a tablet
Coated tablets (4)
sugar coated, film coated, gelatin coated, enteric coated
sugar coated tablets- compressed tablets coated with colored or uncolored sugar layer
long, labor intensive process
film coated tablets (non functional coat)- coated with a thin layer of ________. Usually colored. More _______ and less ______ than sugar coating
polymer, durable, bulky
gelatin coated tablets- capsule shaped tablet dipped in gelatin that is _________ than a capsule filled with equivalent amount of powder
1/3 smaller
enteric coated tablets- coated with ____ sensitive _______ that do not ________________
e.g Eudragit, HMPC, polyvinyl acetate phthalate, diethyl phthalate and cellulose phthalate
pH , polymers, dissolve in gastric pH
buccal and sublingual tablets are for drugs
1.
2.
3.
drugs that are not stable in gastric medium
drugs that are poorly soluble in the GI tract
drugs that bypass 1st pass
sublingual tablets are intended to be __________ and dissolve instantly to provide rapid drug action
dissolved under the tongue
Buccal tablet are intended to be dissolved in the buccal cavity for ________ effect
erode _____ for drug absorption through oral mucosa; lozenges and troches
local or systemic
slowly
chewable tablets
meant to be chewed for tablet _______ and ______ in the mouth
usually have a creamy base of ________ that gives a cool mouth feel
also contain other sweetness such as sorbitol, lactose, dextrose, glucose, aspartame
colorants and flavoring
disintegration and dissolution
mannitol
T/F : chewable tablets contain disintegrating agents
F. chewing is the disintegrating
chewable tablets are usually prepared by __________ and direct compression using only _________ compression force to make soft tablets
wet granulation , some
chewable tablets are useful for children and adults having __________________
difficulty swallowing solid dosage forms
effervescent tablets
- compresses with ________ that release _____ when in contact with water
usually containing sodium bicarb and citric acid/tartaric acids
effervescent salts, CO2
effervescent tablets are __________
rapidly dissolving
RDT's and ODT's disintegrate and dissolve in less than ______, most in ______ or less
1 minute, 15-30 secs
2 ways to manufacture RDT's and ODT's
lyophilization
soft direct compression
lyophilization
- tablets prepared by a foaming mixture of gelatin , sugars, and the drug, poured into a mold, which is also the dispensing package
- the foam is then lyophilized (freeze-dried) and packaged
...
Disadvantages to lyophilization
1.
2.
difficulty taste making
removing from package due to soft nature
soft direct compression
- prepared using very water soluble excipients and usually ________ that wick water into the tablet for rapid disintegration eg. Dimetapp ND OTD (loratadine, Schering)
superdisintegrants
advantages of RDT's
1.
2.
good for patients who have trouble swallowing
more convienent to carry, and requires little to no water to be taken for oral administration
Disadvantages od RDT's
1.
2
3
1. drug loading
2. taste masking
3. friability
molded tablets - soft and soluble, designed for rapid dissolution.
usually contains a mix of _____ and ______ which results in less brittle tablets
do not contain any ________, _________, or ______ that might slower their dissolution
lactose and sucrose
disintegrates, lubricants, coating
Durasolv and oralsolv
rapidly disintegrating tablets
tablet triturates
- small cylindrical tablets, prepared by _____ or _____ usually containing small amounts of ______
molding or compression
potent drugs
tablet triturates must be readily and completely _________
soluble in water
tablet triturates
- a combination of lactose and sucrose helps in making _______ tablets with minimal _________
often inserted into capsules or dissolved in liquid to provide accurate dosing of potent drugs
harder, minimal compression
Hypodermic tablets
- no longer available
-previously used for extemporaneous preparation of parenteral solutions
-stopped due to sterility issues
...
Dispensing tablets
- no longer used
-these used to large tablets of potent drugs, previously used by compounding pharmacies to make smaller and multiple doses
...
T/F immediate release tablets do not contain any release rate-controlling features, such as polymer coatings
true
T/F extended and controlled release tablets are designed to have an undetermined drug release profile
false
vaginal inserts
-uncoated bullet shaped or ovoid tablets to be inserted into the vagina
-usually contain antibacterials for vaginitis or antifungals for candidiasis
...
lozenges
- can be compressed or molded
-hard, meant for slow dissolution in the mouth
-should be heat stable
lollipops
-sugar based lozenges on a stick meant to be sucked by the mouth for local or systemic actions
can be systemic
Besides their API(s), a compressed tablet may contain
-diluents or fillers
-binders or adhesives
-disintegrants
-anti-aherents, glidnats, lubricants
-colors, flavors, coatings
...
Povidone, HPMC, methyl cellulose, carboxymethyl cellulose, PVP are examples of
binders/adhesives
lactose, MCC, calcium phosphate, and starch are examples of
diluents or fillers
corsscarmellose sodium, sodium starch glycolate, starch 1500, crosspovidone, alginic acid are examples of
disintegrates
T/F disintegrants can be only intracellular
false
talc is a
anti-adhesive
colloidal silicone dioxide is a
glidant or flow aid
magnesium iterate, stearic acid, sodium stearyl fumarate are examples of
lubricants
compressed tablets can be made by 3 methods
1.
2.
3.
wet granulation followed by compression
dry granulation followed by compression
direct compression
Wet granulation
- dont under wet or over wet
-over wetting with make hard granules
-underwetting will make soft granules prone to crumbling
- more _______ in the final blend can cause tablet weight variability and content uniformity issues during tabletin
fines
roller compactor is a _______ process
continuous
_______ compression is the easiest and _______ . no granulation step. MCC commonly used
direct , cheapest
problems associated with tableting
1.
2.
3.
4.
5.
1. capping
2. lamination
3. sticking
4. picking
5. splitting
capping
- entire top of surface of the tablet separates from the rest of the tablet
- due to air entrapment in the powder being compressed
- due to higher amount of fines in the granulation (10-20% is ideal to fill void spaces)
-due to punches not being c
...
lamination
- horizontal striations
-when press speed is too high
...
sticking
- granulation sticks to the punches
-when the material is sticky or too much lubrication
-happens with _____ punches
both
picking
- the upper punch picks up a portion of the tablet while retracting
-happens when compression is too low
- happens with ______ punch
upper
splitting
- can happen due to improper storage aging
...
solid dosage forms, compressed with the aid of suitable pharmaceutical ingredients and processing
tablets
most tablets are intended for ______ administration
oral
most tablets are prepared by ________ using ________
compression , rotary tablet presses
what is tablet scoring
helps tablet to be easily split in 2 halves to be taken as divided doses
functional vs nonfunctional modifications
functional modifies release profile and nonfunctional does not
monograms (embossing or debasing) on the tablets are dependent on the etching on the punches. punching can be ________ to prevent ________ in letters containing ______
pre picked, picking, islands
force of pressing determines ______________
hardness
Tablet routes of administration (4)
oral, sublingual, buccal, vaginal
Release profiles (4)
immediate, delayed, sustained, controlled release
Multiple compressed tablets (2)
multiple layers (bi- tri- penta-) or tablet within a tablet
Coated tablets (4)
sugar coated, film coated, gelatin coated, enteric coated
sugar coated tablets- compressed tablets coated with colored or uncolored sugar layer
long, labor intensive process
film coated tablets (non functional coat)- coated with a thin layer of ________. Usually colored. More _______ and less ______ than sugar coating
polymer, durable, bulky
gelatin coated tablets- capsule shaped tablet dipped in gelatin that is _________ than a capsule filled with equivalent amount of powder
1/3 smaller
enteric coated tablets- coated with ____ sensitive _______ that do not ________________
e.g Eudragit, HMPC, polyvinyl acetate phthalate, diethyl phthalate and cellulose phthalate
pH , polymers, dissolve in gastric pH
buccal and sublingual tablets are for drugs
1.
2.
3.
drugs that are not stable in gastric medium
drugs that are poorly soluble in the GI tract
drugs that bypass 1st pass
sublingual tablets are intended to be __________ and dissolve instantly to provide rapid drug action
dissolved under the tongue
Buccal tablet are intended to be dissolved in the buccal cavity for ________ effect
erode _____ for drug absorption through oral mucosa; lozenges and troches
local or systemic
slowly
chewable tablets
meant to be chewed for tablet _______ and ______ in the mouth
usually have a creamy base of ________ that gives a cool mouth feel
also contain other sweetness such as sorbitol, lactose, dextrose, glucose, aspartame
colorants and flavoring
disintegration and dissolution
mannitol
T/F : chewable tablets contain disintegrating agents
F. chewing is the disintegrating
chewable tablets are usually prepared by __________ and direct compression using only _________ compression force to make soft tablets
wet granulation , some
chewable tablets are useful for children and adults having __________________
difficulty swallowing solid dosage forms
effervescent tablets
- compresses with ________ that release _____ when in contact with water
usually containing sodium bicarb and citric acid/tartaric acids
effervescent salts, CO2
effervescent tablets are __________
rapidly dissolving
RDT's and ODT's disintegrate and dissolve in less than ______, most in ______ or less
1 minute, 15-30 secs
2 ways to manufacture RDT's and ODT's
lyophilization
soft direct compression
lyophilization
- tablets prepared by a foaming mixture of gelatin , sugars, and the drug, poured into a mold, which is also the dispensing package
- the foam is then lyophilized (freeze-dried) and packaged
...
Disadvantages to lyophilization
1.
2.
difficulty taste making
removing from package due to soft nature
soft direct compression
- prepared using very water soluble excipients and usually ________ that wick water into the tablet for rapid disintegration eg. Dimetapp ND OTD (loratadine, Schering)
superdisintegrants
advantages of RDT's
1.
2.
good for patients who have trouble swallowing
more convienent to carry, and requires little to no water to be taken for oral administration
Disadvantages od RDT's
1.
2
3
1. drug loading
2. taste masking
3. friability
molded tablets - soft and soluble, designed for rapid dissolution.
usually contains a mix of _____ and ______ which results in less brittle tablets
do not contain any ________, _________, or ______ that might slower their dissolution
lactose and sucrose
disintegrates, lubricants, coating
Durasolv and oralsolv
rapidly disintegrating tablets
tablet triturates
- small cylindrical tablets, prepared by _____ or _____ usually containing small amounts of ______
molding or compression
potent drugs
tablet triturates must be readily and completely _________
soluble in water
tablet triturates
- a combination of lactose and sucrose helps in making _______ tablets with minimal _________
often inserted into capsules or dissolved in liquid to provide accurate dosing of potent drugs
harder, minimal compression
Hypodermic tablets
- no longer available
-previously used for extemporaneous preparation of parenteral solutions
-stopped due to sterility issues
...
Dispensing tablets
- no longer used
-these used to large tablets of potent drugs, previously used by compounding pharmacies to make smaller and multiple doses
...
T/F immediate release tablets do not contain any release rate-controlling features, such as polymer coatings
true
T/F extended and controlled release tablets are designed to have an undetermined drug release profile
false
vaginal inserts
-uncoated bullet shaped or ovoid tablets to be inserted into the vagina
-usually contain antibacterials for vaginitis or antifungals for candidiasis
...
lozenges
- can be compressed or molded
-hard, meant for slow dissolution in the mouth
-should be heat stable
lollipops
-sugar based lozenges on a stick meant to be sucked by the mouth for local or systemic actions
can be systemic
Besides their API(s), a compressed tablet may contain
-diluents or fillers
-binders or adhesives
-disintegrants
-anti-aherents, glidnats, lubricants
-colors, flavors, coatings
...
Povidone, HPMC, methyl cellulose, carboxymethyl cellulose, PVP are examples of
binders/adhesives
lactose, MCC, calcium phosphate, and starch are examples of
diluents or fillers
corsscarmellose sodium, sodium starch glycolate, starch 1500, crosspovidone, alginic acid are examples of
disintegrates
T/F disintegrants can be only intracellular
false
talc is a
anti-adhesive
colloidal silicone dioxide is a
glidant or flow aid
magnesium iterate, stearic acid, sodium stearyl fumarate are examples of
lubricants
compressed tablets can be made by 3 methods
1.
2.
3.
wet granulation followed by compression
dry granulation followed by compression
direct compression
Wet granulation
- dont under wet or over wet
-over wetting with make hard granules
-underwetting will make soft granules prone to crumbling
- more _______ in the final blend can cause tablet weight variability and content uniformity issues during tabletin
fines
roller compactor is a _______ process
continuous
_______ compression is the easiest and _______ . no granulation step. MCC commonly used
direct , cheapest
problems associated with tableting
1.
2.
3.
4.
5.
1. capping
2. lamination
3. sticking
4. picking
5. splitting
capping
- entire top of surface of the tablet separates from the rest of the tablet
- due to air entrapment in the powder being compressed
- due to higher amount of fines in the granulation (10-20% is ideal to fill void spaces)
-due to punches not being c
...
lamination
- horizontal striations
-when press speed is too high
...
sticking
- granulation sticks to the punches
-when the material is sticky or too much lubrication
-happens with _____ punches
both
picking
- the upper punch picks up a portion of the tablet while retracting
-happens when compression is too low
- happens with ______ punch
upper
splitting
- can happen due to improper storage aging
...