Tablet Manufacturing Technique.ppt
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Jul 14, 2023
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About This Presentation
The most common tablet manufacturing process techniques are wet granulation, dry granulation, and direct compression.
Your active pharmaceutical ingredients’ (APIs) physical and chemical stability influences manufacturing.
For successful tablet manufacturing, you need granulators, mixing equipment...
Slide Content
By-
Prof. Vedanshu R. Malviya
M.Pharm (Pharmaceutics)
Dr. Rajendra Gode Institute of
Pharmacy, Amravati
Prof. Vedanshu R. Malviya
M.Pharm (Pharmaceutics)
Dr. Rajendra Gode Institute of
Pharmacy, Amravati
Tabletsare solid dosage
forms consisting of active
ingredient(s) and suitable
pharmaceutical excipients.
They may vary in size,
shape, weight, hardness,
thickness, disintegration
and dissolution
characteristics, and in other
aspects. They may be
classyfied, according to the
method of manufacture, as
compressed tablets or
molded tablets.
forms consisting of active
ingredient(s) and suitable
pharmaceutical excipients.
They may vary in size,
shape, weight, hardness,
thickness, disintegration
and dissolution
characteristics, and in other
aspects. They may be
classyfied, according to the
method of manufacture, as
compressed tablets or
molded tablets.
Production aspect
◦Large scale production at
lowest cost
◦Easiest and cheapest to
package and ship
◦High stability
User aspect (doctor,
pharmacist, patient)
◦Easy to handling
◦Lightest and most
compact
◦Greatest dose precision &
least content variability
◦Large scale production at
lowest cost
◦Easiest and cheapest to
package and ship
◦High stability
User aspect (doctor,
pharmacist, patient)
◦Easy to handling
◦Lightest and most
compact
◦Greatest dose precision &
least content variability
Some drugs resist
compression into dense
compacts
Drugs with poor wetting,
slow dissolution,
intermediate to large
dosages may be difficult or
impossible to formulate and
manufacture as a tablet that
provide adequate or full
drug bioavailability
Bitter taste drugs, drugs
with an objectionable odor,
or sensitive to oxygen or
moisture may require
encapsulation or
entrapment prior to
compression or the tablets
may require coating
compression into dense
compacts
Drugs with poor wetting,
slow dissolution,
intermediate to large
dosages may be difficult or
impossible to formulate and
manufacture as a tablet that
provide adequate or full
drug bioavailability
Bitter taste drugs, drugs
with an objectionable odor,
or sensitive to oxygen or
moisture may require
encapsulation or
entrapment prior to
compression or the tablets
may require coating
1)compressed tablets
2)sugar coated tablets
3)film coated tablets
4)enteric coated tablets
5)effervescent tablets
6)chewable tablets
7)dispersible tablets
8)sustained release tablets
2)sugar coated tablets
3)film coated tablets
4)enteric coated tablets
5)effervescent tablets
6)chewable tablets
7)dispersible tablets
8)sustained release tablets
9)multilayer tablets
10)sublingual tablets
11)toroches
12)buccal tablets
13)implant tablets
14)hypodermic tablets
15)solution tabletc
16)vaginal tablets
10)sublingual tablets
11)toroches
12)buccal tablets
13)implant tablets
14)hypodermic tablets
15)solution tabletc
16)vaginal tablets
Compressed tabletsusuallycontainanumberof
pharmaceuticaladjuncts,knownasexcipients,in
additiontothemedicinalsubstance.Theuseof
appropriateexcipientsisimportantinthedevelopment
oftheoptimumtablets.Excipientsdeterminethebulkof
thefinalproductindosageformssuchastablet,
capsule,etc.,thespeedofdisintegration,rateof
dissolution,releaseofdrug,protectionagainstmoisture,
stabilityduringstorage,andcompatibility.Excipients
shouldhavenobioactivity,noreactionwiththedrug
substance,noeffectonthefunctionsofotherexcipients,
andnosupportofmicrobiologicalgrowthintheproduct.
pharmaceuticaladjuncts,knownasexcipients,in
additiontothemedicinalsubstance.Theuseof
appropriateexcipientsisimportantinthedevelopment
oftheoptimumtablets.Excipientsdeterminethebulkof
thefinalproductindosageformssuchastablet,
capsule,etc.,thespeedofdisintegration,rateof
dissolution,releaseofdrug,protectionagainstmoisture,
stabilityduringstorage,andcompatibility.Excipients
shouldhavenobioactivity,noreactionwiththedrug
substance,noeffectonthefunctionsofotherexcipients,
andnosupportofmicrobiologicalgrowthintheproduct.
Diluents increase the volume to a formulation
to prepare tablets of the desired size.
Widely used fillers are lactose, dextrin,
microcrystalline cellu-lose starch,
pregelatinized starch, powdered sucrose,
and calcium phosphate.
to prepare tablets of the desired size.
Widely used fillers are lactose, dextrin,
microcrystalline cellu-lose starch,
pregelatinized starch, powdered sucrose,
and calcium phosphate.
The diluent is selected based on various factors, such as
the experience of the manufacturer in the preparation
of other tablets, its cost, and compatibility with other
formulation ingredients. For example, in the
preparation of tablets or capsules of tetracycline
antibiotics, a calcium salt should not be used as a
diluent since calcium interferes with absorption of the
antibiotics from the GI tract.
the experience of the manufacturer in the preparation
of other tablets, its cost, and compatibility with other
formulation ingredients. For example, in the
preparation of tablets or capsules of tetracycline
antibiotics, a calcium salt should not be used as a
diluent since calcium interferes with absorption of the
antibiotics from the GI tract.
Binders promote the adhesion of particles of the
formulation. Such adhesion enables preparation
of granules and maintains the integrity of the
final tablet.As listed in the Table, Commonly
used binding agents include: starch, gelatin and
sugars (sucrose, glucose, dextrose, and lactose).
formulation. Such adhesion enables preparation
of granules and maintains the integrity of the
final tablet.As listed in the Table, Commonly
used binding agents include: starch, gelatin and
sugars (sucrose, glucose, dextrose, and lactose).
Carboxymethylcellulose, sodiumKaraya gum
Cellulose,microcrystalline(Avicel®)Starch, pregelatinized
Ethylcellulose Tragacanth gum
Hydroxypropyl methylcellulosePoly(acrylic acid)
Methylcellulose Polypvinylpyrrolidone
Acacia gum Gelatin
Agar Dextrin
Alginacid Glucose
Guar gum Molasses
Cellulose,microcrystalline(Avicel®)Starch, pregelatinized
Ethylcellulose Tragacanth gum
Hydroxypropyl methylcellulosePoly(acrylic acid)
Methylcellulose Polypvinylpyrrolidone
Acacia gum Gelatin
Agar Dextrin
Alginacid Glucose
Guar gum Molasses
Lubricant is a substance capable of reducing or
preventing friction, heat, and wear when introduced as
a film between solid surfaces. It works by coating on the
surface of particles, and thus preventing adhesion of
the tablet material to the dies and punches.
Glycerylmonostearate(USP/NFCH2(OH)CH(OH)CH2O2CC
17H35) is one example of a lubricant. Lubricants play
more than one role in the preparation of tablets as
described below.
preventing friction, heat, and wear when introduced as
a film between solid surfaces. It works by coating on the
surface of particles, and thus preventing adhesion of
the tablet material to the dies and punches.
Glycerylmonostearate(USP/NFCH2(OH)CH(OH)CH2O2CC
17H35) is one example of a lubricant. Lubricants play
more than one role in the preparation of tablets as
described below.
1. Lubricants improve the flow of granules in the
hopper to the die cavity.
2. Lubricants prevent sticking of tablet formulation
to the punches and dies during formulation.
3. Lubricants reduce the friction between the tablet
and the die wall during the tablet’s ejection from
the tablet machine.
4. Lubricants give a sheen to the finished tablets.
hopper to the die cavity.
2. Lubricants prevent sticking of tablet formulation
to the punches and dies during formulation.
3. Lubricants reduce the friction between the tablet
and the die wall during the tablet’s ejection from
the tablet machine.
4. Lubricants give a sheen to the finished tablets.
Commonly used lubricants include: talc,
magnesium stearat, calcium stearate
,stearic acid, hydrogenated vegetable oils
and (PEG).
magnesium stearat, calcium stearate
,stearic acid, hydrogenated vegetable oils
and (PEG).
The breakup of the tablets to smaller particles is important for
dissolution of the drug and subsequent bioavailability.
Disintegrators promote such breakup. To rupture or breakup
of tablets, disintegrating agents must swell or expand on
exposure to aqueous solution. Thus, the most effective
disintegrating agents in most tablet systems are those with the
highest wa-ter uptake property. In general, the more
hydrophilic, the better disinte-grating agents are therefore
highly hydrophilic. A list of typical disinte-grants is tabulated
in Table
dissolution of the drug and subsequent bioavailability.
Disintegrators promote such breakup. To rupture or breakup
of tablets, disintegrating agents must swell or expand on
exposure to aqueous solution. Thus, the most effective
disintegrating agents in most tablet systems are those with the
highest wa-ter uptake property. In general, the more
hydrophilic, the better disinte-grating agents are therefore
highly hydrophilic. A list of typical disinte-grants is tabulated
in Table
Water molecules attract each other equally in all directions. Water
molecules on the surface, however, can only be pulled into the
bulk water by water molecules underneath, since there are no
water molecules to pull in the opposite direction. The surface
tension of water is strong enough to support the weight of tiny
insects such as water striders. The surface ten-sion in action can
be visualized by placing a small drop of alcohol on a thin layer of
water. Alcohol with lower surface tension mixes with water
causing reduction in the surface tension in the local region.
Owing to the higher surface tension of water in the neighbor,
water is pulled from the alcohol dropped region into the
neighbor, and this leads to the formation of a dry spot in the
middle of the water layer.
molecules on the surface, however, can only be pulled into the
bulk water by water molecules underneath, since there are no
water molecules to pull in the opposite direction. The surface
tension of water is strong enough to support the weight of tiny
insects such as water striders. The surface ten-sion in action can
be visualized by placing a small drop of alcohol on a thin layer of
water. Alcohol with lower surface tension mixes with water
causing reduction in the surface tension in the local region.
Owing to the higher surface tension of water in the neighbor,
water is pulled from the alcohol dropped region into the
neighbor, and this leads to the formation of a dry spot in the
middle of the water layer.
•The classification of manufacturing methods
wet granulation: suitable for drugs that are stable to moisture
and heat
dry granulation: suitable for drugs that are sensitive to
moisture and heat
powder compression: suitable for drugs that are sensitive
to moisture and heat, fill material possessing, good flowability
and compressibility
granulation
direct
compression
crystal compression：suitable for drugswith proper
crystal form and good flowability
wet granulation: suitable for drugs that are stable to moisture
and heat
dry granulation: suitable for drugs that are sensitive to
moisture and heat
powder compression: suitable for drugs that are sensitive
to moisture and heat, fill material possessing, good flowability
and compressibility
granulation
direct
compression
crystal compression：suitable for drugswith proper
crystal form and good flowability
drug
excipients
sieving
adhesive
prilling
dry
processing
granule
lubricant
mix press
wet granulation
excipients
sieving
adhesive
prilling
dry
processing
granule
lubricant
mix press
wet granulation
dry granulation
drug
excipient
smashsievingmix
press
cake
smash
processing
granule
adhesive
mix press
drug
excipient
smashsievingmix
press
cake
smash
processing
granule
adhesive
mix press
drugs
excipients
smash sievingmix
adhesive
mix press
powder compression
excipients
smash sievingmix
adhesive
mix press
powder compression
crystal compression
drugs
excipients
smash sieving
mix
mix press
adhesive
drugs
excipients
smash sieving
mix
mix press
adhesive
wet granulation technology
(一)wet granulation methods and equipment:
1.Extrusion grain methods and equipment: first
prescription drug powder and the auxiliary
materials mixed evenly to join adhesive soft
material system, then with soft material
compulsory extrusion way through has a certain
size screen hole and granulating method.
(一)wet granulation methods and equipment:
1.Extrusion grain methods and equipment: first
prescription drug powder and the auxiliary
materials mixed evenly to join adhesive soft
material system, then with soft material
compulsory extrusion way through has a certain
size screen hole and granulating method.
The steps of wet granulation
weighing and blending the ingredients(disintegrant)
preparing a damp mass
screening the damp mass into pellets or granules
drying the granulation
sizing the granulation by dry screening
adding lubricant and disintegrant, and blending
tableting by compression
(liquid binder)
Internal(内加法)
External(外加法)
weighing and blending the ingredients(disintegrant)
preparing a damp mass
screening the damp mass into pellets or granules
drying the granulation
sizing the granulation by dry screening
adding lubricant and disintegrant, and blending
tableting by compression
(liquid binder)
Internal(内加法)
External(外加法)
Tablet presses:
a.single-punch presses
b.multi-station rotary presses
a.single-punch presses
b.multi-station rotary presses
Core components:
die
lower punch
upper punch
die
lower punch
upper punch
a) filling material
b) scraping away the excessive
granulation
c) forming a tablet by
compression
d) pushing up the tablet to stage
surface
e) shoving the tablet aside
b) scraping away the excessive
granulation
c) forming a tablet by
compression
d) pushing up the tablet to stage
surface
e) shoving the tablet aside
hopper
feed-frame
head: upper turret, lower turret, die table
upper turret
die table
lower turret
feed-frame
head: upper turret, lower turret, die table
upper turret
die table
lower turret
A: upper punch
B: die cavity
C: die
D: lower punch
The compression
is applied by both
the upper punch
and the lower
punch.
The compression cycle of a rotary tablet press
B: die cavity
C: die
D: lower punch
The compression
is applied by both
the upper punch
and the lower
punch.
The compression cycle of a rotary tablet press
Suitable for
1) granular chemicals possessing free flowing and
cohesive properties
e.g. potassium chloride
2) chemicals added with special pharmaceutical
excipients which impart the necessary qualities for
the production of tablets by direct compression
1) granular chemicals possessing free flowing and
cohesive properties
e.g. potassium chloride
2) chemicals added with special pharmaceutical
excipients which impart the necessary qualities for
the production of tablets by direct compression
The direct compression tableting excipients include:
a) fillers, as spray-dried lactose, microcrystals of
alphamonohydrate lactose, sucroseinvert ,sugar –corn starch
mixtures, microcrystalline cellulose, crystalline malt and
dicalcium phosphate;
d) disintegrants, as direct-compression starch, sodium
carboxymethyl starch, cross-linked carboxymethylcellulose
fiber, and cross-linked polyvinylpyrrolidone;
c) lubricants, as magnesium stearate and talc;
d) glidants, fumed silicon dioxide
a) fillers, as spray-dried lactose, microcrystals of
alphamonohydrate lactose, sucroseinvert ,sugar –corn starch
mixtures, microcrystalline cellulose, crystalline malt and
dicalcium phosphate;
d) disintegrants, as direct-compression starch, sodium
carboxymethyl starch, cross-linked carboxymethylcellulose
fiber, and cross-linked polyvinylpyrrolidone;
c) lubricants, as magnesium stearate and talc;
d) glidants, fumed silicon dioxide
Sophora Alopecuruldes L．Seed Tablet
optimization
optimization
powder of sophora
AIopecuroides L．Seed
mix 制软材
prilling 、
processing
granule
mix
press
excipient
1％Magnesium
stearate
AIopecuroides L．Seed
mix 制软材
prilling 、
processing
granule
mix
press
excipient
1％Magnesium
stearate
formula 1 2 3 4
adhesive 10%
Starch
10%PVP
（water）
10%CMC-Na10%PVP
(Ethanol)
Hardness
（Kg）
0.68 0.83 0.75 particles
deformed
adhesive 10%
Starch
10%PVP
（water）
10%CMC-Na10%PVP
(Ethanol)
Hardness
（Kg）
0.68 0.83 0.75 particles
deformed
formula 5 6 7 8
fillersstarchPregelati
nized
starch
lactose
10%PVP
( Ethanol)
Hardnes
s（Kg）
0.68 0.77 3.14 3.55
fillersstarchPregelati
nized
starch
lactose
10%PVP
( Ethanol)
Hardnes
s（Kg）
0.68 0.77 3.14 3.55
Factor
level
A [The amount of Microcrstalline
cellulose(g)]
80 120 160
A [Concentration of PVP
solution（%，g/ml)]
10 15 20
level
A [The amount of Microcrstalline
cellulose(g)]
80 120 160
A [Concentration of PVP
solution（%，g/ml)]
10 15 20
Table4:Result of Orthogonal test
Test NO. A B
A×B Result
1 2
Ⅰ Ⅱ
Total
1
2
3
4
5
6
7
8
9
K1
K2
K3
1
1
1
2
2
2
3
3
3
17.8
24.2
24.4
1
2
3
1
2
3
1
2
3
23.0
21.8
21.6
1
2
3
2
3
1
3
1
2
21.4
22.5
22.5
1
2
3
3
1
2
2
3
1
22.2
22.0
22.2
3.1 2.9 6.0
2.8 3.1 5.9
3.2 2.7 5.9
4.1 4.4 8.5
4.0 4.1 8.1
4.2 3.4 8.5
4.0 3.8 7.8
3.9 4.2 8.1
R×6 6.6 1.4
1.1 0.2
0.6
Test NO. A B
A×B Result
1 2
Ⅰ Ⅱ
Total
1
2
3
4
5
6
7
8
9
K1
K2
K3
1
1
1
2
2
2
3
3
3
17.8
24.2
24.4
1
2
3
1
2
3
1
2
3
23.0
21.8
21.6
1
2
3
2
3
1
3
1
2
21.4
22.5
22.5
1
2
3
3
1
2
2
3
1
22.2
22.0
22.2
3.1 2.9 6.0
2.8 3.1 5.9
3.2 2.7 5.9
4.1 4.4 8.5
4.0 4.1 8.1
4.2 3.4 8.5
4.0 3.8 7.8
3.9 4.2 8.1
R×6 6.6 1.4
1.1 0.2
0.6
variance sourceSS V MS F P
total variance5.658
A 4.6982 2.349 33.562 0.0001
B 0.1912 0.096 1.366 0.3034
A×B 0.1394 0.035 0.993 0.4077
error 0.6309 0.070
total variance5.658
A 4.6982 2.349 33.562 0.0001
B 0.1912 0.096 1.366 0.3034
A×B 0.1394 0.035 0.993 0.4077
error 0.6309 0.070
Comparison
group
differenc
e
between
two
means
standard
value of q
error
Number
of
group
α =0.05α= 0.01
P
A1andA3-1.1 0.1074-10.2413 4.346.33<0.01
A1andA2-1.0 0.1074-9.310 2 3.465.24<0.01
A2andA3-0.1 0.1074-9.310 2 3.465.24>0.05
q threshold
group
differenc
e
between
two
means
standard
value of q
error
Number
of
group
α =0.05α= 0.01
P
A1andA3-1.1 0.1074-10.2413 4.346.33<0.01
A1andA2-1.0 0.1074-9.310 2 3.465.24<0.01
A2andA3-0.1 0.1074-9.310 2 3.465.24>0.05
q threshold
The reasons for tablet coating
1) to protect the medicinal agent against destructive exposure
to air and/or humidity;
2) to mask the taste of the drug;
3) to provide special characteristics of drug release;
4) to provide aesthetics or distinction to the product;
5) to prevent inadvertent contact by nonpatients with the drug
substance
1) to protect the medicinal agent against destructive exposure
to air and/or humidity;
2) to mask the taste of the drug;
3) to provide special characteristics of drug release;
4) to provide aesthetics or distinction to the product;
5) to prevent inadvertent contact by nonpatients with the drug
substance
The general methods involved in coating tablets are as follows
1) sugarcoating tablets
2) film-coating tablets
3) enteric coating
4) pan coating
5) fluid-bed or air suspension coating
6) compression coating
1) sugarcoating tablets
2) film-coating tablets
3) enteric coating
4) pan coating
5) fluid-bed or air suspension coating
6) compression coating
The sugarcoating of tablets may be divided into the
following steps:
1) waterproofing and sealing (if needed)
2) subcoating
3) smoothing and final rounding
4) finishing and coloring (if desired)
5) polishing
following steps:
1) waterproofing and sealing (if needed)
2) subcoating
3) smoothing and final rounding
4) finishing and coloring (if desired)
5) polishing
Chip——Cladding Isolation——Powder Coating Layer——sugar coating
layer——colored icing——Light up
layer——colored icing——Light up
1) waterproofing and sealing (if needed)
aim: to prevent the components from being adversely
affected by moisture; one or more coats; shellac , zein ,
or a polymer as cellulose acetate phthalate
2) Subcoating aim: to bond the sugar coating to the
tablet and provide rounding
a) 3 to 5 subcoats of a sugar-based syrup are applied.
The sucrose and water syrup also contains gelatin,
acacia, or PVP.
aim: to prevent the components from being adversely
affected by moisture; one or more coats; shellac , zein ,
or a polymer as cellulose acetate phthalate
2) Subcoating aim: to bond the sugar coating to the
tablet and provide rounding
a) 3 to 5 subcoats of a sugar-based syrup are applied.
The sucrose and water syrup also contains gelatin,
acacia, or PVP.
b) When the tablets are partially dry they are
sprinkled with a dusting powder, usually a mixture
of powdered sugar and starch but sometimes talc,
acacia, or precipitated chalk as well.
c) Then drying the tablets. Repetition (15 to 18 times)
the subcoating process until the tablets are of the
desired shape and size.
sprinkled with a dusting powder, usually a mixture
of powdered sugar and starch but sometimes talc,
acacia, or precipitated chalk as well.
c) Then drying the tablets. Repetition (15 to 18 times)
the subcoating process until the tablets are of the
desired shape and size.
3) smoothing and final rounding
aim: to complete the rounding and smooth the
coatings
5 to 10 additional coatings of a thick syrup; This syrup
is sucrose-based with or without additional
components as starch and calcium carbonate.
4) finishing and coloring
aim: to attain final smoothness and the appropriate
color
several coats of a thin syrup containing the desired
colorant
aim: to complete the rounding and smooth the
coatings
5 to 10 additional coatings of a thick syrup; This syrup
is sucrose-based with or without additional
components as starch and calcium carbonate.
4) finishing and coloring
aim: to attain final smoothness and the appropriate
color
several coats of a thin syrup containing the desired
colorant
5) imprinting
aim: to impart identification codes and other distinctive
symbols to the product
The imprint may be debossed, embossed, engraved, or printed
on the surface with ink.
6) polishing
aim: to render the tablets the desired sheen/gloss/luster
a) pans lined with canvas cloth impregnated with carnauba
waxand/or beeswax
b) Pieces of wax may be placed in a polishing pan
c) light-spraying of the tablets with wax dissolved in a
nonaqueous solvent
aim: to impart identification codes and other distinctive
symbols to the product
The imprint may be debossed, embossed, engraved, or printed
on the surface with ink.
6) polishing
aim: to render the tablets the desired sheen/gloss/luster
a) pans lined with canvas cloth impregnated with carnauba
waxand/or beeswax
b) Pieces of wax may be placed in a polishing pan
c) light-spraying of the tablets with wax dissolved in a
nonaqueous solvent
1) The disadvantages of sugarcoating process
a) time-consuming
b) requiring the expertise of highly skilled technicians
c) doubling the size and weight of the original uncoated
tablets
d) may vary in size from batch to batch and within a batch
e) large tablets are not as easily swallowed as are small
tablets.
a) time-consuming
b) requiring the expertise of highly skilled technicians
c) doubling the size and weight of the original uncoated
tablets
d) may vary in size from batch to batch and within a batch
e) large tablets are not as easily swallowed as are small
tablets.
2) The advantages of film-coating process
a) coated tablets having essentially the same weight, shape,
and size as the originally compressed tablet
b) The coating is thin enough to reveal any identifying
monograms.
c) far more resistant to destruction by abrasion than are
sugar-coated tablets
d) the coating may be colored to make the tablets attractive
and distinctive.
a) coated tablets having essentially the same weight, shape,
and size as the originally compressed tablet
b) The coating is thin enough to reveal any identifying
monograms.
c) far more resistant to destruction by abrasion than are
sugar-coated tablets
d) the coating may be colored to make the tablets attractive
and distinctive.
3) The components of nonaqueous film-coating solutions:
a) film former: e.g. CAP
b) alloying substance: to provide water solubility or
permeability to the film e.g. PEG
c) plasticizer: to render flexibility and elasticity to the coating
e.g. castor oil
d) surfactant: to enhance spreadability of the film e.g.
polyoxyethylene sorbitan derivatives
e) opaquants and colorants: e.g. titanium dioxide, FD&C or
D&C dyes
f) sweeteners, flavors, and aromas: saccharin, vanillin
g) glossant: beeswax
h) volatile solvent: alcohol-acetone mixture
a) film former: e.g. CAP
b) alloying substance: to provide water solubility or
permeability to the film e.g. PEG
c) plasticizer: to render flexibility and elasticity to the coating
e.g. castor oil
d) surfactant: to enhance spreadability of the film e.g.
polyoxyethylene sorbitan derivatives
e) opaquants and colorants: e.g. titanium dioxide, FD&C or
D&C dyes
f) sweeteners, flavors, and aromas: saccharin, vanillin
g) glossant: beeswax
h) volatile solvent: alcohol-acetone mixture
4) The components of a typical aqueous film-coating
solutions:
a) film-forming polymer (7-18%): e.g. cellulose
ether polymers as HPMC, HPC and MC
b) plasticizer (0.5-2.0%): e.g. glycerin, propylene
glycol, PEG, diethyl phthalate, and dibutyl
subacetate
c) colorant and opacifier (2.5-8%): FD&C or D&C
lakes and iron oxide pigments
d) water
solutions:
a) film-forming polymer (7-18%): e.g. cellulose
ether polymers as HPMC, HPC and MC
b) plasticizer (0.5-2.0%): e.g. glycerin, propylene
glycol, PEG, diethyl phthalate, and dibutyl
subacetate
c) colorant and opacifier (2.5-8%): FD&C or D&C
lakes and iron oxide pigments
d) water
5) Some problems with aqueous film-coating
a) picking and peeling the appearance of small amounts or
large amounts of film fragments flaking from the tablet
surface
b) orange peel effect roughness of the tablet surface due to
failure of spray droplets to coalesce
c) mottling an uneven distribution of color on the tablet
surface
d) bridging
filling-in of the score-line or indented logo on the tablet by
the film
e) tablet erosion
disfiguration of the core tablet
a) picking and peeling the appearance of small amounts or
large amounts of film fragments flaking from the tablet
surface
b) orange peel effect roughness of the tablet surface due to
failure of spray droplets to coalesce
c) mottling an uneven distribution of color on the tablet
surface
d) bridging
filling-in of the score-line or indented logo on the tablet by
the film
e) tablet erosion
disfiguration of the core tablet
5) Some problems with aqueous film-coating
a) picking and peeling the appearance of small amounts or
large amounts of film fragments flaking from the tablet
surface
b) orange peel effect roughness of the tablet surface due to
failure of spray droplets to coalesce
c) mottling an uneven distribution of color on the tablet
surface
d) bridging
filling-in of the score-line or indented logo on the tablet by
the film
e) tablet erosion
disfiguration of the core tablet
a) picking and peeling the appearance of small amounts or
large amounts of film fragments flaking from the tablet
surface
b) orange peel effect roughness of the tablet surface due to
failure of spray droplets to coalesce
c) mottling an uneven distribution of color on the tablet
surface
d) bridging
filling-in of the score-line or indented logo on the tablet by
the film
e) tablet erosion
disfiguration of the core tablet
The reasons for capping,
splitting or laminating of
tablets
1) air entrapment
2) not immaculately cleaned or not
perfectly smoothed punches
3) too great a proportion of fine powder
4) Tablets have aged or have been
stored improperly
splitting or laminating of
tablets
1) air entrapment
2) not immaculately cleaned or not
perfectly smoothed punches
3) too great a proportion of fine powder
4) Tablets have aged or have been
stored improperly
The apparent physical features of compressed tablets:
1) shape: round, oblong, unique 2) thickness: thick or thin
3) diameter: large or small 4) flat or convex
5) unscored or scored in halves, thirds and quadrants
6) engraved or imprinted with an identifying symbol and/or code
number
7) coated or uncoated 8)colored or uncolored 9) number of layer.
The die and punches determine the physical features of
compressed tablets.
1) shape: round, oblong, unique 2) thickness: thick or thin
3) diameter: large or small 4) flat or convex
5) unscored or scored in halves, thirds and quadrants
6) engraved or imprinted with an identifying symbol and/or code
number
7) coated or uncoated 8)colored or uncolored 9) number of layer.
The die and punches determine the physical features of
compressed tablets.
Other physical specifications and quality standards:
tablet weight weight variation
content uniformity tablet thickness
tablet hardness tablet disintegration
drug dissolution
in-process controls
verification after the production
tablet weight weight variation
content uniformity tablet thickness
tablet hardness tablet disintegration
drug dissolution
in-process controls
verification after the production
Chp weight variation:
sample amount 20
tablets
Tablets should comply
with the following
requirements stated in
the table below.
Average
weight
Weight
variation
limit
Less than
0.3 g
±7.5%
0.3 g or
more
±5%
sample amount 20
tablets
Tablets should comply
with the following
requirements stated in
the table below.
Average
weight
Weight
variation
limit
Less than
0.3 g
±7.5%
0.3 g or
more
±5%
Electronic weighing instrument
The procedure of weight variation determination in Chp:
Weigh accurately 20 tablets and calculate the average
weight, then weigh individually each of the 20 tablets.
Compare the weight of each tablet with the labelled
tablet (if no labelled weight is stated, compare the
weight of each tablet with the average weight
calculated). No more than 2 of the individual weights
exceed the weight variation limit stated in the table
above and none doubles the limit.
Weigh accurately 20 tablets and calculate the average
weight, then weigh individually each of the 20 tablets.
Compare the weight of each tablet with the labelled
tablet (if no labelled weight is stated, compare the
weight of each tablet with the average weight
calculated). No more than 2 of the individual weights
exceed the weight variation limit stated in the table
above and none doubles the limit.
Tablet hardness
1)The greater the pressure applied, the harder the tablets.
2) The hardness required by different tablets
a) lozenges and buccal tablets: hard (dissolve slowly)
b) the tablets for immediate drug release: soft
3) measurement
a) special dedicated hardness testers
b) multifunctional equipment
1)The greater the pressure applied, the harder the tablets.
2) The hardness required by different tablets
a) lozenges and buccal tablets: hard (dissolve slowly)
b) the tablets for immediate drug release: soft
3) measurement
a) special dedicated hardness testers
b) multifunctional equipment
applys to potent drug of low dose.
USP method, 10 tablets are individually assayed for
their content.
The amount of active ingredient in each tablet lies
within the range of 85% to 115% of the label claim
and the RSD is less than 6.0%.
USP method, 10 tablets are individually assayed for
their content.
The amount of active ingredient in each tablet lies
within the range of 85% to 115% of the label claim
and the RSD is less than 6.0%.
Friability
1) It is used to determine a tablet’s durability
2) Method: allowing the tablets to roll and fall within
the rotating apparatus (friabilator); determine the
loss in weight;
3) requirement: weight loss ≤1%
1) It is used to determine a tablet’s durability
2) Method: allowing the tablets to roll and fall within
the rotating apparatus (friabilator); determine the
loss in weight;
3) requirement: weight loss ≤1%
Hardness
Tester
Tester
Tablet Friability Tester
1) The importance of in vitrodissolution test
a) to guide the formulation and product development
process toward product optimization
b) to monitor the performance of manufacturing process
c) to assure bioequivalence from batch to batch
d) as a requirement for regulatory approval for product
marketing for products registered with the FDA and
regulatory agencies of other countries.
a) to guide the formulation and product development
process toward product optimization
b) to monitor the performance of manufacturing process
c) to assure bioequivalence from batch to batch
d) as a requirement for regulatory approval for product
marketing for products registered with the FDA and
regulatory agencies of other countries.
2) The goal of in vitro dissolution is to
provide a reasonable prediction of the
product’s in vivo bioavailability.
Basis: The combinations of a drug’s solubility
and its intestinal permeability are supposed
as a basis for predicting the likelihood of
achieving a successful in vivo –in vitro
correlation (IVIVC).
provide a reasonable prediction of the
product’s in vivo bioavailability.
Basis: The combinations of a drug’s solubility
and its intestinal permeability are supposed
as a basis for predicting the likelihood of
achieving a successful in vivo –in vitro
correlation (IVIVC).
Considered are drugs determined to have:
a) high solubility and high permeability
(IVIVC may be expected.)
b) low solubility and high permeability
(IVIVC may be expected.)
c) high solubility and low permeability
d) low solubility and low permeability
a) high solubility and high permeability
(IVIVC may be expected.)
b) low solubility and high permeability
(IVIVC may be expected.)
c) high solubility and low permeability
d) low solubility and low permeability
3) The formulation and manufacturing factors
affecting the dissolution of a tablet
a) the particle size of the drug substance
b) the solubility and hygroscopicity of the
formulation
c) the type and concentration of the
disintegrant, binder, and lubricant used
d) the manufacturing method, particularly,
the compactness of the granulation and the
compression force
e) the in-process variables
affecting the dissolution of a tablet
a) the particle size of the drug substance
b) the solubility and hygroscopicity of the
formulation
c) the type and concentration of the
disintegrant, binder, and lubricant used
d) the manufacturing method, particularly,
the compactness of the granulation and the
compression force
e) the in-process variables
4) Test method
a) A volume of the dissolution medium is placed in
the vessel and allowed to come to 37℃±0.5℃.
b) The stirrer is rotate at the specified speed.
c) At stated intervals, samples of the medium are
withdrawn for chemical analysis
5) Requirement for rate of dissolution
The specific required rates of dissolution are
different for tablets containing different medicinal
agents.
e.g. not less than 85% of the labeled amount is
dissolved in 30 minutes
a) A volume of the dissolution medium is placed in
the vessel and allowed to come to 37℃±0.5℃.
b) The stirrer is rotate at the specified speed.
c) At stated intervals, samples of the medium are
withdrawn for chemical analysis
5) Requirement for rate of dissolution
The specific required rates of dissolution are
different for tablets containing different medicinal
agents.
e.g. not less than 85% of the labeled amount is
dissolved in 30 minutes
6) Inconsistencies in dissolution
occur not between dosage units from the same
production batch, but rather between batches or
between products from different manufacturers.
Pooled dissolution testing has emerged. This
process recognizes the concept of batch
characteristics and allows pooled specimens to be
tested.
occur not between dosage units from the same
production batch, but rather between batches or
between products from different manufacturers.
Pooled dissolution testing has emerged. This
process recognizes the concept of batch
characteristics and allows pooled specimens to be
tested.
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